货号:A288826
同义名:
HePC; Hexadecyl phosphocholine
Miltefosine是一种多靶点抑制剂,通过抑制 PI3K/Akt 和 PKC 活性表现抗微生物、抗利什曼原虫活性,可用于传染病和癌症的研究。
HazMat Fee + There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
| Type | HazMat fee for 500 gram (Estimated) |
| Excepted Quantity | USD 0.00 |
| Limited Quantity | USD 15-60 |
| Inaccessible (Haz class 6.1), Domestic | USD 80+ |
| Inaccessible (Haz class 6.1), International | USD 150+ |
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |


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| 产品名称 | PKC ↓ ↑ | PKCα ↓ ↑ | PKCβ ↓ ↑ | PKCγ ↓ ↑ | PKCδ ↓ ↑ | PKCε ↓ ↑ | PKCζ ↓ ↑ | PKCη ↓ ↑ | PKCθ ↓ ↑ | 其他靶点 | 纯度 | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Daphnetin |
+
PKC, IC50: 25.01 μM |
EGFR,PKA | 95% | ||||||||||||||||
| Dequalinium Chloride | 99%+ | ||||||||||||||||||
| Quercetin | ✔ | Src,Sirtuin | 95% | ||||||||||||||||
| Myricetrin | ✔ | 96% | |||||||||||||||||
| Go 6983 |
+++
PKCα, IC50: 7 nM |
+++
PKCβ, IC50: 7 nM |
+++
PKCγ, IC50: 6 nM |
+++
PKCδ, IC50: 10 nM |
++
PKCζ, IC50: 60 nM |
99%+ | |||||||||||||
| Go6976 |
+++
PKC, IC50: 7.9 nM |
++++
PKCα, IC50: 2.3 nM |
+++
PKCβ1, IC50: 6.2 nM |
FLT3 | 99%+ | ||||||||||||||
| Bisindolylmaleimide I |
+++
PKCα, IC50: 20 nM |
+++
PKCβ2, IC50: 16 nM PKCβ1, IC50: 17 nM |
+++
PKCγ, IC50: 20 nM |
99%+ | |||||||||||||||
| Lawsone methyl ether | ✔ | 99% | |||||||||||||||||
| Sotrastaurin |
++++
PKCα, Ki: 0.95 nM |
++++
PKCβ1, Ki: 0.64 nM |
++++
PKCδ, Ki: 2.1 nM |
++++
PKCε, Ki: 3.2 nM |
++++
PKCη, Ki: 1.8 nM |
++++
PKCθ, Ki: 0.22 nM |
99%+ | ||||||||||||
| Enzastaurin |
++
PKCα, IC50: 39 nM |
+++
PKCβ, IC50: 6 nM |
+
PKCγ, IC50: 83 nM |
+
PKCε, IC50: 110 nM |
98% | ||||||||||||||
| Midostaurin |
++
PKCα, IC50: 22 nM |
++
PKCβ2, IC50: 31 nM PKCβ1, IC50: 30 nM |
++
PKCγ, IC50: 24 nM |
+
PKCδ, IC50: 330 nM |
+
PKCε, IC50: 1.25 μM |
+
PKCη, IC50: 160 nM |
99% | ||||||||||||
| Ro 31-8220 mesylate |
++++
PKCα, IC50: 5 nM |
+++
PKCβ2, IC50: 14 nM PKCβ1, IC50: 24 nM |
++
PKCγ, IC50: 27 nM |
++
PKCε, IC50: 24 nM |
99%+ | ||||||||||||||
| Staurosporine |
++++
PKCα, IC50: 2 nM |
++++
PKCγ, IC50: 5 nM |
+++
PKCδ, IC50: 20 nM |
++
PKCε, IC50: 73 nM |
++++
PKCη, IC50: 4 nM |
99%+ | |||||||||||||
| Ruboxistaurin HCl |
+
PKCα, IC50: 0.36 μM |
++++
PKCβ2, IC50: 5.9 nM PKCβ1, IC50: 4.7 nM |
+
PKCγ, IC50: 0.3 μM |
+
PKCδ, IC50: 0.25 μM |
++
PKCη, IC50: 0.052 μM |
99%+ | |||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 产品名称 | ALK1 ↓ ↑ | ALK2 ↓ ↑ | ALK3 ↓ ↑ | ALK4 ↓ ↑ | ALK6 ↓ ↑ | Smad3 ↓ ↑ | TGF-β ↓ ↑ | TGFβRI/ALK5 ↓ ↑ | TGFβRII ↓ ↑ | 其他靶点 | 纯度 | ||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| LDN193189 |
++++
ALK1, IC50: 0.8 nM |
++++
ALK2, IC50: 0.8 nM |
+++
ALK3, IC50: 5.3 nM |
+++
ALK6, IC50: 16.7 nM |
99%+ | ||||||||||||||
| LDN-212854 |
++++
ALK1, IC50: 2.4 nM |
++++
ALK2, IC50: 1.3 nM |
+
ALK3, IC50: 85.8 nM |
+
ALK4, IC50: 2133 nM |
+
ALK5, IC50: 9276 nM |
99%+ | |||||||||||||
| ML347 |
++
ALK1, IC50: 46 nM |
++
ALK2, IC50: 32 nM |
98% | ||||||||||||||||
| K02288 |
++++
ALK1, IC50: 1.8 nM |
++++
ALK2, IC50: 1.1 nM |
++
ALK3, IC50: 34.4 nM |
+++
ALK6, IC50: 6.4 nM |
99%+ | ||||||||||||||
| LDN-193189 2HCl |
++++
ALK1, IC50: 0.8 nM |
++++
ALK2, IC50: 0.8 nM |
+++
ALK3, IC50: 5.3 nM |
+++
ALK6, IC50: 16.7 nM |
99% | ||||||||||||||
| LDN-214117 |
++
ALK2, IC50: 24 nM |
98% | |||||||||||||||||
| DMH-1 |
+
ALK2, IC50: 107.9 nM |
99%+ | |||||||||||||||||
| SB-505124 |
+
ALK4, IC50: 129 nM |
++
ALK5, IC50: 47 nM |
99%+ | ||||||||||||||||
| Vactosertib |
+++
ALK4, IC50: 13 nM |
+++
ALK5, IC50: 11 nM |
99%+ | ||||||||||||||||
| Alantolactone | ✔ | 98% | |||||||||||||||||
| (E/Z)-SIS3 free base | ✔ | 97% | |||||||||||||||||
| Pirfenidone | ✔ | 98% | |||||||||||||||||
| Hesperetin | ✔ | 97% | |||||||||||||||||
| RepSox |
++++
TGFβR1(ALK5), IC50: 4 nM |
98% | |||||||||||||||||
| GW788388 |
+++
ALK5, IC50: 18 nM |
98% | |||||||||||||||||
| LY364947 |
++
TGFβRI, IC50: 59 nM |
+
TGFβRII, IC50: 0.4 μM |
98% | ||||||||||||||||
| SD-208 |
++
TGF-βRI (ALK5), IC50: 48 nM |
99% | |||||||||||||||||
| SB-525334 |
+++
TGFβR1(ALK5), IC50: 14.3 nM |
99%+ | |||||||||||||||||
| LY2109761 |
++
TβRI, Ki: 38 nM |
+
TβRII, Ki: 300 nM |
99%+ | ||||||||||||||||
| Galunisertib |
++
TβRI, IC50: 56 nM |
98% | |||||||||||||||||
| SB 431542 |
+
ALK5, IC50: 94 nM |
99%+ | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 产品名称 | Akt ↓ ↑ | Akt1 ↓ ↑ | Akt2 ↓ ↑ | Akt3 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Honokiol | ✔ | MEK | 98% | ||||||||||||||||
| PF-04691502 |
++++
P-Akt (T308), IC50: 7.5 nM P-Akt (S473), IC50: 3.8 nM |
98+% | |||||||||||||||||
| PHT-427 |
+
Akt, Ki: 2.7 μM |
99%+ | |||||||||||||||||
| Deguelin | ✔ | PI3K | 99%+ | ||||||||||||||||
| TIC10 isomer | ✔ | ERK | 98+% | ||||||||||||||||
| Perifosine |
+
Akt, IC50: 4.7 μM |
98% | |||||||||||||||||
| Miltefosine | ✔ | PI3K,PKC | 98% | ||||||||||||||||
| Triciribine |
+
Akt, IC50: 130 nM |
99%+ | |||||||||||||||||
| Uprosertib |
+
Akt1, IC50: 180 nM |
+
Akt2, IC50: 328 nM |
++
Akt3, IC50: 38 nM |
99%+ | |||||||||||||||
| Afuresertib |
++++
Akt1, Ki: 0.08 nM |
++++
Akt2, Ki: 2 nM |
++++
Akt3, Ki: 2.6 nM |
99%+ | |||||||||||||||
| Miransertib |
++++
Akt1, IC50: 5 nM |
++++
Akt2, IC50: 4.5 nM |
++
Akt3, IC50: 16 nM |
98+% | |||||||||||||||
| GSK-690693 |
++++
Akt1, IC50: 2 nM |
+++
Akt2, IC50: 13 nM |
+++
Akt3, IC50: 9 nM |
99%+ | |||||||||||||||
| AT7867 |
++
Akt1, IC50: 32 nM |
++
Akt2, IC50: 17 nM |
++
Akt3, IC50: 47 nM |
PKA | 99%+ | ||||||||||||||
| AKT inhibitor VIII |
++
Akt1, IC50: 58 nM |
+
Akt2, IC50: 210 nM |
+
Akt3, IC50: 2119 nM |
97% | |||||||||||||||
| MK-2206 2HCl |
+++
Akt1, IC50: 8 nM |
+++
Akt2, IC50: 12 nM |
+
Akt3, IC50: 65 nM |
99%+ | |||||||||||||||
| Ipatasertib |
++++
Akt1, IC50: 5 nM |
++
Akt2, IC50: 18 nM |
+++
Akt3, IC50: 8 nM |
99%+ | |||||||||||||||
| AT13148 |
++
Akt1, IC50: 38 nM |
+
Akt2, IC50: 402 nM |
++
Akt3, IC50: 50 nM |
PKA | 95% | ||||||||||||||
| Capivasertib |
++++
Akt1, IC50: 3 nM |
+++
Akt2, IC50: 8 nM |
+++
Akt3, IC50: 8 nM |
99%+ | |||||||||||||||
| A-674563 HCl |
+++
Akt1, Ki: 11 nM |
PKA | 99% | ||||||||||||||||
| CCT128930 |
+++
Akt2, IC50: 6 nM |
PKA | 95% | ||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 产品名称 | C2β ↓ ↑ | p110α ↓ ↑ | p110β ↓ ↑ | p110γ ↓ ↑ | p110δ ↓ ↑ | PI3K ↓ ↑ | Vps34 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| A66 |
+
C2β, IC50: 462 nM |
++
p110α, IC50: 32 nM |
99%+ | ||||||||||||||||
| Taselisib |
+
C2β, IC50: 292 nM |
++++
PI3Kα, Ki: 0.29 nM |
+++
PI3Kβ, Ki: 9.1 nM |
++++
PI3Kγ, Ki: 0.97 nM |
++++
PI3Kδ, Ki: 0.12 nM |
+
hVps34, IC50: 374 nM |
99%+ | ||||||||||||
| Gedatolisib |
++++
PI3Kα, IC50: 0.4 nM |
+++
PI3Kγ, IC50: 5.4 nM |
mTOR | 99% | |||||||||||||||
| HS-173 |
++++
PI3Kα , IC50: 0.8 nM |
99%+ | |||||||||||||||||
| Serabelisib |
+++
PI3Kα, IC50: 21 nM |
99%+ | |||||||||||||||||
| GNE-477 |
++++
PI3Kα, IC50: 4 nM |
mTOR | 99% | ||||||||||||||||
| YM-201636 |
+
p110α, IC50: 3.3 μM |
PIKfyve | 98% | ||||||||||||||||
| AS-252424 |
+
PI3Kα, IC50: 935 nM |
++
PI3Kγ, IC50: 33 nM |
99% | ||||||||||||||||
| Alpelisib |
+++
PI3Kα, IC50: 5 nM |
99%+ | |||||||||||||||||
| AS-604850 |
+
PI3Kα, IC50: 4.5 μM |
+
PI3Kγ, IC50: 0.25 μM |
99% | ||||||||||||||||
| SF2523 |
++
PI3Kα, IC50: 34 nM |
++
PI3Kγ, IC50: 158 nM |
DNA-PK,mTOR | 99%+ | |||||||||||||||
| Inavolisib |
++++
PI3K alpha, IC50: 0.038 nM |
99%+ | |||||||||||||||||
| Bimiralisib |
++++
PI3Kα, Kd: 1.5 nM |
+++
PI3Kβ, Kd: 11 nM |
++
PI3Kγ, Kd: 25 nM |
++
PI3Kδ, Kd: 25 nM |
mTOR | 99%+ | |||||||||||||
| GSK1059615 |
++++
PI3Kα, IC50: 0.4 nM |
++++
PI3Kβ, IC50: 0.6 nM |
+++
PI3Kγ, IC50: 5 nM |
++++
PI3Kδ, IC50: 2 nM |
mTOR | 98% | |||||||||||||
| GSK2636771 | ✔ | 99% | |||||||||||||||||
| Fimepinostat |
+++
PI3Kα, IC50: 19 nM |
++
PI3Kβ, IC50: 54 nM |
++
PI3Kδ, IC50: 39 nM |
99%+ | |||||||||||||||
| VS-5584 |
++++
PI3Kα, IC50: 2.6 nM |
+++
PI3Kβ, IC50: 21 nM |
++++
PI3Kγ, IC50: 3.0 nM |
++++
PI3Kδ, IC50: 2.7 nM |
mTOR | 98% | |||||||||||||
| Dactolisib |
++++
p110α1, IC50: 4 nM |
++
p110β, IC50: 75 nM |
+++
p110γ, IC50: 5 nM |
+++
p110δ, IC50: 7 nM |
98+% | ||||||||||||||
| PI-103 |
++++
p110α, IC50: 2 nM |
++++
p110β, IC50: 3 nM |
+++
p110γ, IC50: 15 nM |
++++
p110δ, IC50: 3 nM |
DNA-PK,mTOR | 99%+ | |||||||||||||
| PI-3065 |
+
p110β, IC50: 1078 nM |
+++
p110δ, IC50: 15 nM |
99%+ | ||||||||||||||||
| Voxtalisib |
++
PI3Kα, IC50: 39 nM |
++
PI3Kβ, IC50: 113 nM |
+++
PI3Kγ, IC50: 9 nM |
++
PI3Kδ, IC50: 43 nM |
DNA-PK,mTOR | 99%+ | |||||||||||||
| AZD-8835 |
+++
PI3Kα, IC50: 6.2 nM |
+
PI3Kβ, IC50: 431 nM |
++
PI3Kγ, IC50: 90 nM |
+++
PI3Kδ, IC50: 5.7 nM |
99% | ||||||||||||||
| Pilaralisib analogue |
++
PI3Kα, IC50: 39 nM |
++
PI3Kβ, IC50: 36 nM |
+++
PI3Kγ, IC50: 23 nM |
++
PI3Kδ, IC50: 36 nM |
99%+ | ||||||||||||||
| ZSTK474 |
+++
PI3Kα, IC50: 16 nM |
++
PI3Kβ, IC50: 44 nM |
++
PI3Kγ, IC50: 49 nM |
+++
PI3Kδ, IC50: 4.6 nM |
++
PI3K, IC50: 37 nM |
98% | |||||||||||||
| AS-605240 |
++
PI3Kα, IC50: 60 nM |
+
PI3Kβ, IC50: 270 nM |
+++
PI3Kγ, IC50: 8 nM |
+
PI3Kδ, IC50: 300 nM |
98% | ||||||||||||||
| TGX-221 |
+++
p110β, IC50: 5 nM |
++
p110δ, IC50: 0.1 μM |
99%+ | ||||||||||||||||
| PF-04691502 |
++++
PI3Kα, Ki: 1.8 nM |
++++
PI3Kβ, Ki: 2.1 nM |
++++
PI3Kγ, Ki: 1.9 nM |
++++
PI3Kδ, Ki: 1.6 nM |
mTOR | 98+% | |||||||||||||
| GDC-0084 |
++++
PI3Kα, Ki app: 2 nM |
++
PI3Kβ, Ki app: 46 nM |
+++
PI3Kγ, Ki app: 10 nM |
++++
PI3Kδ, Ki app: 3 nM |
mTOR | 99%+ | |||||||||||||
| Buparlisib |
++
p110α, IC50: 52 nM |
+
p110β, IC50: 166 nM |
+
p110γ, IC50: 262 nM |
++
p110δ, IC50: 116 nM |
+
Vps34, IC50: 2.4 μM |
mTOR | 98% | ||||||||||||
| LY294002 |
+
p110α, IC50: 0.5 μM |
+
p110β, IC50: 0.97 μM |
+
p110δ, IC50: 0.57 μM |
DNA-PK | 99%+ | ||||||||||||||
| AZD 6482 |
+
PI3Kα, IC50: 870 nM |
+++
PI3Kβ, IC50: 10 nM |
++
PI3Kδ, IC50: 80 nM |
DNA-PK | 99%+ | ||||||||||||||
| Pictilisib |
++++
p110α, IC50: 3 nM |
++
p110β, IC50: 33 nM |
++
p110γ, IC50: 75 nM |
++++
p110δ, IC50: 3 nM |
mTOR | 99%+ | |||||||||||||
| PKI-402 |
++++
PI3Kα, IC50: 2 nM |
+++
PI3Kβ, IC50: 7 nM |
+++
PI3Kγ, IC50: 16 nM |
+++
PI3Kδ, IC50: 14 nM |
mTOR | 98% | |||||||||||||
| Copanlisib |
++++
PI3Kα, IC50: 0.5 nM |
++++
PI3Kβ, IC50: 3.7 nM |
+++
PI3Kγ, IC50: 6.4 nM |
++++
PI3Kδ, IC50: 0.7 nM |
99%+ | ||||||||||||||
| Omipalisib |
++++
p110α, Ki: 0.019 nM |
++++
p110β, Ki: 0.13 nM |
++++
p110γ, Ki: 0.06 nM |
++++
p110δ, Ki: 0.024 nM |
99%+ | ||||||||||||||
| Izorlisib |
+++
PI3Kα, IC50: 14 nM |
++
PI3Kβ, IC50: 0.12 μM |
++
PI3Kγ, IC50: 36 nM |
+
PI3Kδ, IC50: 0.50 μM |
99%+ | ||||||||||||||
| AZD8186 |
++
PI3Kα, IC50: 35 nM |
++++
PI3Kβ, IC50: 4 nM |
+++
PI3Kδ, IC50: 12 nM |
99% | |||||||||||||||
| KU-0060648 |
++++
PI3Kα, IC50: 4 nM |
++++
PI3Kβ, IC50: 0.5 nM |
+
PI3Kγ, IC50: 0.59 μM |
++++
PI3Kδ, IC50: 0.1 nM |
DNA-PK | 98% | |||||||||||||
| Apitolisib |
+++
p110α, IC50: 5 nM |
++
p110β, IC50: 27 nM |
+++
p110γ, IC50: 14 nM |
+++
p110δ, IC50: 7 nM |
mTOR | 98%+ | |||||||||||||
| CZC24832 |
+
PI3Kβ, IC50: 1.1 μM |
++
PI3Kγ, IC50: 27 nM |
98+% | ||||||||||||||||
| BGT226 maleate |
++++
PI3Kα, IC50: 4 nM |
++
PI3Kβ, IC50: 63 nM |
++
PI3Kγ, IC50: 38 nM |
mTOR | 99%+ | ||||||||||||||
| TG 100713 |
++
PI3Kα, IC50: 165 nM |
+
PI3Kβ, IC50: 215 nM |
++
PI3Kγ, IC50: 50 nM |
+++
PI3Kδ, IC50: 24 nM |
98%+ | ||||||||||||||
| PI3K-IN-1 |
++
PI3Kα, IC50: 39 nM |
++
PI3Kβ, IC50: 113 nM |
+++
PI3Kγ, IC50: 9 nM |
++
PI3Kδ, IC50: 43 nM |
DNA-PK,mTOR | 98+% | |||||||||||||
| TG100-115 |
+
PI3Kα, IC50: 1.3 μM |
+
PI3Kβ, IC50: 1.2 μM |
++
PI3Kγ, IC50: 83 nM |
+
PI3Kδ, IC50: 235 nM |
98% | ||||||||||||||
| PIK-90 |
+++
PI3Kα, IC50: 11 nM |
+
PI3Kβ, IC50: 350 nM |
+++
PI3Kγ, IC50: 18 nM |
++
PI3Kδ, IC50: 58 nM |
99%+ | ||||||||||||||
| PIK-294 |
+
p110β, IC50: 490 nM |
++
p110γ, IC50: 160 nM |
+++
p110δ, IC50: 10 nM |
99%+ | |||||||||||||||
| Duvelisib |
++++
PI3Kβ, Ki: 1564 pM |
++
PI3Kγ, Ki: 243 pM |
++++
PI3Kδ, Ki: 23 pM |
99%+ | |||||||||||||||
| GDC-0326 |
++++
PI3Kα, Ki: 0.2 nM |
++
PI3Kβ, Ki: 26.6 nM |
+++
PI3Kγ, Ki: 10.2 nM |
++++
PI3Kδ, Ki: 4 nM |
98% | ||||||||||||||
| Quercetin Dihydrate |
+
PI3Kβ, IC50: 5.4 μM |
+
PI3Kγ, IC50: 2.4 μM |
+
PI3Kδ, IC50: 3.0 μM |
95% | |||||||||||||||
| Quercetin |
+
PI3Kβ, IC50: 5.4 μM |
+
PI3Kγ, IC50: 2.4 μM |
+
PI3Kδ, IC50: 3.0 μM |
Src,Sirtuin,PKC | 95% | ||||||||||||||
| Leniolisib |
+
PI3Kα, IC50: 0.244 μM |
+
PI3Kβ, IC50: 0.424 μM |
+
PI3Kγ, IC50: 2.23 μM |
+++
PI3Kδ, IC50: 0.011 μM |
DNA-PK | 99%+ | |||||||||||||
| PIK-108 | ✔ | 99% | |||||||||||||||||
| Eganelisib |
+++
PI3Kγ, IC50: 16 nM |
99%+ | |||||||||||||||||
| CAY10505 | ✔ | 99% | |||||||||||||||||
| IPI-3063 |
++++
p110δ, IC50: 2.5 nM |
99% | |||||||||||||||||
| Nemiralisib |
++++
PI3Kδ, pKi: 9.9 |
99%+ | |||||||||||||||||
| PF-4989216 |
++++
p110α, IC50: 2 nM |
++
p110γ, IC50: 65 nM |
++++
p110δ, IC50: 1 nM |
99%+ | |||||||||||||||
| PIK-75 HCl |
+++
p110α, IC50: 5.8 nM |
++
p110γ, IC50: 76 nM |
+
p110δ, IC50: 0.51 μM |
DNA-PK | 99%+ | ||||||||||||||
| Tenalisib |
++
PI3Kγ, IC50: 33.2 nM |
++
PI3Kδ, IC50: 24.5 nM |
98% | ||||||||||||||||
| Acalisib |
+++
p110δ, IC50: 14 nM |
99%+ | |||||||||||||||||
| Umbralisib |
+++
PI3Kδ, IC50: 22.2 nM |
99%+ | |||||||||||||||||
| AMG319 |
+
PI3Kγ, IC50: 850 nM |
+++
PI3Kδ, IC50: 18 nM |
99% | ||||||||||||||||
| IC-87114 |
+
PI3Kγ, IC50: 29 μM |
+
PI3Kδ, IC50: 0.5 μM |
99%+ | ||||||||||||||||
| Idelalisib |
++
p110γ, IC50: 89 nM |
++++
p110δ, IC50: 2.5 nM |
98% | ||||||||||||||||
| PIK-293 |
+
p110γ, IC50: 10 μM |
+
p110δ, IC50: 0.24 μM |
99%+ | ||||||||||||||||
| Vps34-PIK-III |
+
PI3Kδ, IC50: 1.2μM |
+++
Vps34, IC50: 0.018μM |
99%+ | ||||||||||||||||
| GSK2292767 | ✔ | 98% | |||||||||||||||||
| Seletalisib |
+
PI3Kγ, IC50: 282 nM |
+++
PI3Kδ, IC50: 12 nM |
99%+ | ||||||||||||||||
| P110δ-IN-1 |
++++
P110δ, IC50: 0.6 nM |
99% | |||||||||||||||||
| PI3Kδ-IN-5 |
++++
PI3Kδ, IC50: 0.9 nM |
99% | |||||||||||||||||
| SRX3207 |
+
PI3K alpha, IC50: 244 nM |
+
PI3K gamma, IC50: 9790 nM |
+
PI3K delta, IC50: 388 nM |
Syk | 98% | ||||||||||||||
| Parsaclisib HCl |
++++
PI3Kδ, IC50: 1 nM |
98% | |||||||||||||||||
| IHMT-PI3Kδ-372 |
+++
PI3Kδ, IC50: 14 nM |
98% | |||||||||||||||||
| Trigonelline | ✔ | Akt | 99%+ | ||||||||||||||||
| Wortmannin |
++++
PI3K, IC50: 3 nM |
MLCK,DNA-PK | 99%+ | ||||||||||||||||
| Samotolisib | ✔ | DNA-PK | 99%+ | ||||||||||||||||
| GNE-317 | ✔ | 99%+ | |||||||||||||||||
| Oroxin B | ✔ | PTEN,Akt | 99%+ | ||||||||||||||||
| NU 7026 |
+
PI3K, IC50: 13 μM |
DNA-PK | 98+% | ||||||||||||||||
| Deguelin | ✔ | Akt | 99%+ | ||||||||||||||||
| Ailanthone | ✔ | CDK,Akt,ATM/ATR | 98% | ||||||||||||||||
| Resibufogenin | ✔ | ROS | 98% | ||||||||||||||||
| KU-57788 |
+
PI3K, IC50: 5 μM |
DNA-PK,mTOR | 99%+ | ||||||||||||||||
| Cinobufagine | ✔ | Akt | 99% | ||||||||||||||||
| α-Linolenic acid | ✔ | 97% (GC) | |||||||||||||||||
| MTX-211 | ✔ | EGFR | 98% | ||||||||||||||||
| PI3K/mTOR Inhibitor-2 |
++++
PI3K, IC50: 3.4 nM |
mTOR | 99%+ | ||||||||||||||||
| SPP-86 | ✔ | 99%+ | |||||||||||||||||
| (E)-Akt inhibitor-IV | ✔ | 98% | |||||||||||||||||
| Vps34-IN-1 |
++
Vps34, IC50: 25 nM |
98% | |||||||||||||||||
| SAR405 |
++++
Vps34, IC50: 1.2 nM |
98+% | |||||||||||||||||
| 3-Methyladenine |
+
PI3Kγ, IC50: 60 μM |
+
Vps34, IC50: 25 μM |
Autophagy | 98% | |||||||||||||||
| Vps34-IN-4 |
+++
VPS34, IC50: 15 nM |
98%+ | |||||||||||||||||
| Autophinib |
+++
Vps34, IC50: 19 nM |
Autophagy | 99% | ||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | Akt/PKB is a crucial protein within the phosphatidylinositol3-kinase/Akt/mammalian target of rapamycin (PI3K/Akt/mTOR) intracellular signalling pathway, which is involved in cell survival. Miltefosine is considered an inhibitor of Akt and is the only oral drug to treat infections caused by L. donovani[7]. Miltefosine belongs to the class of alkylphosphocholine drugs (ALPs), which are phosphocholine esters of aliphatic long-chain alcohols. These alkylphosphocholine compounds are structurally related to the group of alkyl-lysophospholipids, which are synthetic analogues of lysophosphatidylcholines or lysolecithins. From a functional point of view, miltefosine is considered an inhibitor of Akt. The most prominent molecular targets for miltefosine’s anticancer activity are related to the antileishmanial targets, and include the inhibition of phosphatidylcholine biosynthesis and the induction of apoptosis by inhibition of the PI3K/Akt/PKB pathway[8]. The ED50 values of Miltefosine towards inhibiting PI3K/Akt activity are 17.2 μM and 8.1 μM in carcinoma cell lines A431 and HeLa[9]. Miltefosine is approvaled for application in cutaneous metastasis of breast cancer and visceral and cutaneous leishmaniasis. ALPs have also shown in vitro and in vivo activity against Trypanosoma spp., amoebae, Tricomonas vaginalis, Schistosoma mansoni, HIV, and some fungi and bacteria species[10]. |
| 作用机制 | The mechanism of action of ALPs is not fully understood, they interfere with lipid homeostasis which increased degradation of lipid-droplets via lipophagy and prevent plasma membrane recruitment of the PH domain of AKT by disrupting plasma membrane microdomains thus leading to cell apoptosis[10]. |
| Concentration | Treated Time | Description | References | |
| Human eosinophils | 20 µM | 15 min | Inhibited CCL11-stimulated Akt phosphorylation | Br J Pharmacol. 2021 Mar;178(5):1234-1248. |
| Human eosinophils | 20 µM | 15 min | Inhibited CCL24-induced eosinophil chemotaxis | Br J Pharmacol. 2021 Mar;178(5):1234-1248. |
| Mouse bone marrow-derived eosinophils | 20 µM | 1 min | Inhibited CCL24-stimulated intracellular calcium flux by approximately 50%, similar to human eosinophils | Br J Pharmacol. 2021 Mar;178(5):1234-1248. |
| Human eosinophils | 20 µM | 1 min | Inhibited CCL24-stimulated intracellular calcium flux by approximately 50% | Br J Pharmacol. 2021 Mar;178(5):1234-1248. |
| Human eosinophils | 20 µM | 15 min | Suppressed C5a-induced CD63 expression (0.5 nM) but had no effect at high C5a concentration (100 nM) | Br J Pharmacol. 2021 Mar;178(5):1234-1248. |
| Human eosinophils | 20 µM | 15 min | Inhibited CCL24-induced CD11b up-regulation by approximately 50% | Br J Pharmacol. 2021 Mar;178(5):1234-1248. |
| Human eosinophils | 0.5–20 µM | 15 min | Inhibited CCL11-induced eosinophil shape change by approximately 50% at the highest concentration (20 μM) | Br J Pharmacol. 2021 Mar;178(5):1234-1248. |
| Horse erythrocytes | 12 µM | 20 hours | To assess the effect of miltefosine on the hemolytic activity of A. baumannii strains. Results showed that miltefosine significantly reduced the hemolytic activity of all tested strains. | Antimicrob Agents Chemother. 2018 Dec 21;63(1):e01409-18. |
| A549 human alveolar epithelial cells | 12 µM | 20 hours | To assess the effect of miltefosine on the cytolytic activity of A. baumannii strains against A549 cells. Results showed that miltefosine significantly reduced the cytolytic activity of all tested strains. | Antimicrob Agents Chemother. 2018 Dec 21;63(1):e01409-18. |
| RAW264.7 macrophage cell line | 5 µM | 24 hours | Assessment of NO accumulation in macrophages post-infection | EBioMedicine. 2022 Dec;86:104378. |
| Trypanosoma cruzi trypomastigotes | 31.17 µM | 24 hours | Evaluate the trypanocidal activity of MLT on trypomastigotes, results showed low trypanocidal activity of MLT. | Front Cell Infect Microbiol. 2022 Jul 5;12:855119. |
| Trypanosoma cruzi trypomastigotes | 31.17 µM (IC50) | 24 hours | Evaluate the trypanocidal activity of MLT on trypomastigotes, results showed low trypanocidal activity of MLT. | Front Cell Infect Microbiol. 2022 Jul 5;12:855119. |
| Clonorchis sinensis newly excysted juvenile worms (CsNEJs) | 12.5, 25, 50, 100 µM | 24, 48, 72 hours | To assess the larvicidal effect of MLT on CsNEJs. Results showed that MLT significantly reduced the viability of CsNEJs at 50 µM and 100 µM concentrations, with 0% survival after 48 hours. | Antimicrob Agents Chemother. 2024 Sep 4;68(9):e0064224. |
| Clonorchis sinensis metacercariae (CsMC) | 12.5, 25, 50, 100 µM | 24, 48, 72 hours | To assess the larvicidal effect of MLT on CsMC. Results showed that MLT significantly reduced the viability of CsMC at 50 µM and 100 µM concentrations, with 31.3% and 75% reductions in viability after 72 hours, respectively. | Antimicrob Agents Chemother. 2024 Sep 4;68(9):e0064224. |
| Leishmania infantum promastigotes | 10 µM | 3.5 hours or 5.0 hours | Measurement of intracellular miltefosine accumulation levels | EBioMedicine. 2022 Dec;86:104378. |
| CAR-T cells | 15 µM | 4 days | Restores CAR-T cell function, enhances glycolytic metabolism and glucose uptake | Cell Rep Med. 2024 Dec 17;5(12):101869. |
| CCD-18Co | 10 µM | 48 hours | To evaluate the cytotoxic effect of Miltefosine on normal colon cells, results showed that Miltefosine had no significant toxicity on normal cells at higher concentrations. | Clin Transl Med. 2021 Nov;11(11):e552. |
| SW480 | 1 µM | 48 hours | To evaluate the cytotoxic effect of Miltefosine on CRC cells, results showed that Miltefosine significantly inhibited the growth of SW480 cells and induced apoptosis. | Clin Transl Med. 2021 Nov;11(11):e552. |
| DLD1 | 1 µM | 48 hours | To evaluate the cytotoxic effect of Miltefosine on CRC cells, results showed that Miltefosine significantly inhibited the growth of DLD1 cells and induced apoptosis. | Clin Transl Med. 2021 Nov;11(11):e552. |
| HCT116 | 1 µM | 48 hours | To evaluate the cytotoxic effect of Miltefosine on CRC cells, results showed that Miltefosine significantly inhibited the growth of HCT116 cells and induced apoptosis. | Clin Transl Med. 2021 Nov;11(11):e552. |
| HT29 | 1 µM | 48 hours | To evaluate the cytotoxic effect of Miltefosine on CRC cells, results showed that Miltefosine significantly inhibited the growth of HT29 cells and induced apoptosis. | Clin Transl Med. 2021 Nov;11(11):e552. |
| Vero-C76 cells | 0.51 µM | 5 days | Evaluate the inhibitory activity of MLT on intracellular amastigotes, results showed significant inhibition of amastigotes by MLT. | Front Cell Infect Microbiol. 2022 Jul 5;12:855119. |
| Vero-C76 cells | 0.51 µM (IC50) | 5 days | Evaluate the inhibitory activity of MLT on intracellular amastigotes, results showed significant inhibition of amastigotes by MLT. | Front Cell Infect Microbiol. 2022 Jul 5;12:855119. |
| L. donovani intramacrophagic amastigotes | 5.60 µM (EC50) | 72 hours | Evaluate the leishmanicidal effects of NFT and MTF alone and in combination on L. donovani intramacrophagic amastigotes, finding a strong synergistic effect for the NFT/MTF 1/30 combination up to 50% fa. | Int J Mol Sci. 2023 Jan 13;24(2):1635. |
| L. donovani axenic amastigotes | 0.63 µM (EC50) | 72 hours | Evaluate the leishmanicidal effects of NFT and MTF alone and in combination on L. donovani axenic amastigotes, finding a synergistic effect for the NFT/MTF 1/30 combination. | Int J Mol Sci. 2023 Jan 13;24(2):1635. |
| Lomentospora prolificans FMR 3569 | 4 µg/ml | 72 hours | Evaluate the inhibitory effect of Miltefosine on Lomentospora prolificans, results showed effective inhibition of fungal growth | Front Cell Infect Microbiol. 2021 Jul 23;11:698662. |
| Scedosporium dehoogii CBS 117406 | 4 µg/ml | 72 hours | Evaluate the inhibitory effect of Miltefosine on Scedosporium dehoogii, results showed effective inhibition of fungal growth | Front Cell Infect Microbiol. 2021 Jul 23;11:698662. |
| Scedosporium apiospermum CBS 117407 | 4 µg/ml | 72 hours | Evaluate the inhibitory effect of Miltefosine on Scedosporium apiospermum, results showed effective inhibition of fungal growth | Front Cell Infect Microbiol. 2021 Jul 23;11:698662. |
| Scedosporium boydii CBS 120157 | 2 µg/ml | 72 hours | Evaluate the inhibitory effect of Miltefosine on Scedosporium boydii, results showed effective inhibition of fungal growth | Front Cell Infect Microbiol. 2021 Jul 23;11:698662. |
| Scedosporium aurantiacum CBS 136046 | 2–4 µg/ml | 72 hours | Evaluate the inhibitory effect of Miltefosine on Scedosporium aurantiacum, results showed effective inhibition of fungal growth | Front Cell Infect Microbiol. 2021 Jul 23;11:698662. |
| Cryptococcus gattii ATCC 56990 | 1 μg/ml | 72 hours | To evaluate the effects of miltefosine on Cryptococcus cell ultrastructure, results showed thinner cell walls, reduced capsule, and mitochondrial swelling. | Antimicrob Agents Chemother. 2018 Jul 27;62(8):e00312-18. |
| Cryptococcus neoformans H99 | 1 μg/ml | 72 hours | To evaluate the effects of miltefosine on Cryptococcus cell ultrastructure, results showed thinner cell walls, reduced capsule, and mitochondrial swelling. | Antimicrob Agents Chemother. 2018 Jul 27;62(8):e00312-18. |
| Leishmania donovani miltefosine-resistant clone (HePC-R40) promastigotes | 69.1 ± 1.1 µM (IC50) | 72 hours | To assess the effect of miltefosine on the viability of Leishmania donovani resistant clone promastigotes, showing that miltefosine had no cytotoxic effect at concentrations up to 40 μM, but exhibited cytotoxicity at higher doses. | Antimicrob Agents Chemother. 2004 Mar;48(3):852-9. |
| Leishmania donovani wild-type promastigotes | 13.6 ± 2.0 µM (IC50) | 72 hours | To assess the effect of miltefosine on the viability of Leishmania donovani promastigotes, showing that miltefosine inhibits the viability of wild-type promastigotes in a concentration-dependent manner. | Antimicrob Agents Chemother. 2004 Mar;48(3):852-9. |
| Administration | Dosage | Frequency | Description | References | ||
| NPG mice | NCI-H226-luciferase CDX model | Intraperitoneal injection | 10 mg/kg | Once daily, duration as observed | Enhances the solid tumor clearance ability of CAR-T cells | Cell Rep Med. 2024 Dec 17;5(12):101869. |
| NSG mice | CRC xenograft model | Intraperitoneal | 10 mg/kg | Daily for 21 days | To evaluate the antitumor effect of Miltefosine on CRC xenograft models, results showed that Miltefosine significantly inhibited tumor growth and reduced tumor regrowth potential. | Clin Transl Med. 2021 Nov;11(11):e552. |
| Galleria mellonella | G. mellonella infection model | Injection | 12 μM | Single injection, observed for 5 days | To assess the effect of miltefosine on the survival rate of G. mellonella infected with A. baumannii. Results showed that miltefosine significantly reduced the mortality rate of infected larvae. | Antimicrob Agents Chemother. 2018 Dec 21;63(1):e01409-18. |
| BALB/c mice | Eosinophil migration model in IL-5 transgenic mice | Oral | 20 mg/kg | For three consecutive days | Significantly suppressed CCL24-induced eosinophil migration into bronchoalveolar lavage fluid | Br J Pharmacol. 2021 Mar;178(5):1234-1248. |
| Syrian golden hamsters | Clonorchis sinensis infection model | Oral | 20 mg/kg | Administered at 1 and 4 weeks post-infection | To evaluate the larvicidal and adulticidal effects of MLT in vivo against Clonorchis sinensis. Results showed that MLT significantly reduced worm burden by 36.7% and 46.9% when administered at 1 and 4 weeks post-infection, respectively. | Antimicrob Agents Chemother. 2024 Sep 4;68(9):e0064224. |
| Swiss mice | Immunosuppressed murine model of systemic/vascular pythiosis | Oral | 25 mg/kg | Every 24 hours for 14 days | To evaluate the efficacy of miltefosine in treating systemic pythiosis in immunosuppressed mice, results showed miltefosine did not significantly reduce mortality. | Antimicrob Agents Chemother. 2018 Dec 21;63(1):e01385-18 |
| BALB/cJ mice | Acute infection model | Oral | 25, 50, 75, 100 mg/kg/day | Once daily for 20 consecutive days | Evaluate the efficacy of MLT alone or in combination with BZ in acute infection in mice, results showed MLT significantly reduced parasitemia and mortality. | Front Cell Infect Microbiol. 2022 Jul 5;12:855119. |
| Balb/c mice | L. donovani visceral leishmaniasis model | Oral | 10 mg/kg | Daily for 10 days | Evaluate the therapeutic efficacy of the NFT/MTF combination in L. donovani-infected mice, showing significant reduction in parasite load, particularly in thymus and bone marrow. | Int J Mol Sci. 2023 Jan 13;24(2):1635. |
| Dose | Rat: 0.1 mg/kg - 10 mg/kg[3] (p.o.) Mice: 50 mg/kg[4] (i.p.) Dog: 2 mg/kg[5] (p.o.) | ||||||||||||||||||
| Administration | p.o., i.p. | ||||||||||||||||||
| Pharmacokinetics |
|
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.45mL 0.49mL 0.25mL |
12.27mL 2.45mL 1.23mL |
24.54mL 4.91mL 2.45mL |
|
| CAS号 | 58066-85-6 |
| 分子式 | C21H46NO4P |
| 分子量 | 407.57 |
| SMILES Code | O=P(OCC[N+](C)(C)C)(OCCCCCCCCCCCCCCCC)[O-] |
| MDL No. | MFCD00133396 |
| 别名 | HePC; Hexadecyl phosphocholine; Miltefosinum; Miltefosina; Miltefosin; Choline Phosphate Hexadecyl Ester Hydroxide Inner Salt; Miltex; mpavido; Miltefosin CHePCHexadecylphosphocholineHDPCHexadecylphosphorylcholineMiltefosinum; NSC 605583; HPC |
| 运输 | 蓝冰 |
| InChI Key | PQLXHQMOHUQAKB-UHFFFAOYSA-N |
| Pubchem ID | 3599 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Inert atmosphere, store in freezer, under -20°C |
| 溶解方案 |
DMSO: 3 mg/mL(7.36 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO H2O: 30 mg/mL(73.61 mM),配合低频超声,并水浴加热至45℃助溶
|
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