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Miltefosine/米替福新 {[allProObj[0].p_purity_real_show]}

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。

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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+
Miltefosine/米替福新 化学结构 CAS号:58066-85-6
Miltefosine/米替福新 化学结构
CAS号:58066-85-6
Miltefosine/米替福新 3D分子结构
CAS号:58066-85-6
Miltefosine/米替福新 化学结构 CAS号:58066-85-6
Miltefosine/米替福新 3D分子结构 CAS号:58066-85-6
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Miltefosine/米替福新 纯度/质量文件 产品仅供科研

货号:A288826 标准纯度: {[allProObj[0].p_purity_real_show]}
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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。

Miltefosine/米替福新 生物活性

靶点
  • Akt

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].

Miltefosine/米替福新 细胞实验

Cell Line
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.

Miltefosine/米替福新 动物实验

Species
Animal Model
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.

Miltefosine/米替福新 动物研究

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
Animal Rats[6]
Dose 10 mg/kg
Administration i.v. or p.o.
T1/2 82.5 h (i.v.)
84.3 h (p.o.)
Vz 1.07 L/kg (i.v.)
Tmax 24.0 h (p.o.)
CL 0.15 ml/min/kg (i.v.)
Vss 0.96 L/kg (i.v.)
AUC 1104180 ng·h ml (i.v.)
904533 ng·h ml (p.o.)

Miltefosine/米替福新 参考文献

[1]Eissa MM, El-Moslemany RM, et al. Miltefosine Lipid Nanocapsules for Single Dose Oral Treatment of Schistosomiasis Mansoni: A Preclinical Study. PLoS One. 2015 Nov 17;10(11):e0141788.

[2]Chugh P, Bradel-Tretheway B, et al. Akt inhibitors as an HIV-1 infected macrophage-specific anti-viral therapy. Retrovirology. 2008 Jan 31;5:11.

[3]Botschuijver S, van Diest SA, et al. Miltefosine treatment reduces visceral hypersensitivity in a rat model for irritable bowel syndrome via multiple mechanisms. Sci Rep. 2019 Aug 29;9(1):12530.

[4]Bhatt AP, Bhende PM, et al. Dual inhibition of PI3K and mTOR inhibits autocrine and paracrine proliferative loops in PI3K/Akt/mTOR-addicted lymphomas. Blood. 2010 Jun 3;115(22):4455-63.

[5]Manna L, Corso R, et al. Long-term follow-up of dogs with leishmaniosis treated with meglumine antimoniate plus allopurinol versus miltefosine plus allopurinol. Parasit Vectors. 2015 May 28;8:289.

[6]Miltefosine

[7]Pinto-Martinez AK, Rodriguez-Durán J, Serrano-Martin X, Hernandez-Rodriguez V, Benaim G. Mechanism of Action of Miltefosine on Leishmania donovani Involves the Impairment of Acidocalcisome Function and the Activation of the Sphingosine-Dependent Plasma Membrane Ca2+ Channel. Antimicrob Agents Chemother. 2017 Dec 21;62(1):e01614-17.

[8]Dorlo TP, Balasegaram M, Beijnen JH, de Vries PJ. Miltefosine: a review of its pharmacology and therapeutic efficacy in the treatment of leishmaniasis. J Antimicrob Chemother. 2012 Nov;67(11):2576-97.

[9]Uberall F, Oberhuber H, Maly K, Zaknun J, Demuth L, Grunicke HH. Hexadecylphosphocholine inhibits inositol phosphate formation and protein kinase C activity. Cancer Res. 1991 Feb 1;51(3):807-12.

[10]Pachioni Jde A, Magalhães JG, Lima EJ, Bueno Lde M, Barbosa JF, de Sá MM, Rangel-Yagui CO. Alkylphospholipids - a promising class of chemotherapeutic agents with a broad pharmacological spectrum. J Pharm Pharm Sci. 2013;16(5):742-59.

Miltefosine/米替福新 实验方案

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

Miltefosine/米替福新 技术信息

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

配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
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