SRX3177是 CDK4/6、PI3K 和 BRD4 的三重抑制剂,IC50 值分别为 33 nM (BRD4 BD1)、89 nM (BRD4 BD2)、79 nM (PI3Kα)、83 nM (PI3Kδ)、3.18 μM (PI3Kγ)、<2.5 nM (CDK4)、3.3 nM (CDK6),对癌细胞具有广泛的细胞毒性,但对正常上皮细胞无害。


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| 产品名称 | BET ↓ ↑ | bromodomain ↓ ↑ | BRPF ↓ ↑ | CBP/beta-catenin ↓ ↑ | p300/CBP ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| MS436 |
++
BRD4 (1), Ki: <0.085 μM BRD4 (2), Ki: 0.34 μM |
99%+ | |||||||||||||||||
| CPI-203 |
+++
BRD4, IC50: 37 nM |
98+% | |||||||||||||||||
| GSK1324726A |
+++
BRD4, IC50: 22 nM BRD2, IC50: 31 nM |
99%+ | |||||||||||||||||
| PFI-1 |
++
BRD4, IC50: 0.22 μM BRD2, IC50: 98 nM |
98% | |||||||||||||||||
| Apabetalone |
+
BD2, IC50: 0.51 μM |
99% | |||||||||||||||||
| (+)-JQ1 |
+++
BRD4 (2), IC50: 33 nM BRD4 (1), IC50: 77 nM |
98% | |||||||||||||||||
| I-BET151 |
+
BRD4, IC50: 0.5 μM BRD3, IC50: 0.25 μM |
98% | |||||||||||||||||
| Molibresib |
+++
BET proteins, IC50: 35 nM |
99%+ | |||||||||||||||||
| I-BRD9 |
+++
BRD9, pIC50: 7.3 BRD4, pIC50: 5.3 |
99%+ | |||||||||||||||||
| BI-7273 |
++++
BRD9, IC50: 19 nM BRD7, IC50: 117 nM |
97% | |||||||||||||||||
| Pelabresib |
+++
BRD4-BD1, IC50: 39 nM |
98% | |||||||||||||||||
| ARV-825 |
+++
BRD4 BD2, Kd: 28 nM BRD4 BD1, Kd: 90 nM |
99%+ | |||||||||||||||||
| Birabresib | 99%+ | ||||||||||||||||||
| BI 2536 |
+++
BRD4, Kd: 37 nM |
c-Myc | 99%+ | ||||||||||||||||
| Bromosporine |
++
BRD9, IC50: 0.122 μM BRD2, IC50: 0.29 μM |
++++
CECR2, IC50: 17 nM |
99%+ | ||||||||||||||||
| XMD8-92 |
++
BRD4 (1), Kd: 170 nM |
99%+ | |||||||||||||||||
| Mivebresib | ✔ | 99%+ | |||||||||||||||||
| BI-9564 |
++++
BRD7, Kd: 73 nM BRD9, Kd: 5.9 nM |
++
CECR2, Kd: 77 nM |
98% | ||||||||||||||||
| AZD5153 6-Hydroxy-2-naphthoic acid |
++++
FL-BRD4, IC50: 5 nM |
99%+ | |||||||||||||||||
| PLX51107 |
++++
BRD3 BD1, Kd: 2.1 nM BRD4 BD2, Kd: 1.7 nM |
99%+ | |||||||||||||||||
| FL-411 |
+
BRD4(1), IC50: 0.43 μM |
99%+ | |||||||||||||||||
| ABBV-744 | ✔ | 99%+ | |||||||||||||||||
| dBET6 |
++++
BRD4, IC50: 14 nM |
99%+ | |||||||||||||||||
| dBET1 |
++++
BRD4, IC50: 20 nM |
99%+ | |||||||||||||||||
| MZ1 |
++++
Brd2(BD2), Kd: 62 nM Brd3(BD2), Kd: 13 nM |
99%+ | |||||||||||||||||
| dBET57 |
+
BRD4BD1, DC50: 500 nM |
99%+ | |||||||||||||||||
| SF2523 |
+
BRD4, IC50: 241 nM |
DNA-PK | 99%+ | ||||||||||||||||
| INCB054329 |
++++
BRD3-BD1, IC50: 9 nM BRD4-BD1, IC50: 119 nM |
99% | |||||||||||||||||
| INCB-057643 | ✔ | 99%+ | |||||||||||||||||
| (E/Z)-ZL0420 |
+++
BRD4 BD1, IC50: 27 nM BRD4 BD2, IC50: 32 nM |
99%+ | |||||||||||||||||
| BMS-986158 | ✔ | 99% | |||||||||||||||||
| BRD4 Inhibitor-10 |
++++
BRD4-BD2, IC50: 41 nM BRD4-BD1, IC50: 5 nM |
97% | |||||||||||||||||
| A1874 | ✔ | 99%+ | |||||||||||||||||
| Y06036 |
++
BRD4 (1), Kd: 82 nM |
99%+ | |||||||||||||||||
| Alobresib | ✔ | NF-κB | 95% | ||||||||||||||||
| ODM-207 | ✔ | 98% | |||||||||||||||||
| GSK778 |
+++
BRD2-BD1, IC50: 75nM BRD4-BD1, IC50: 143 nM |
97% | |||||||||||||||||
| SRX3207 |
+
BRD42, IC50: 3070 nM BRD41, IC50: 3070 nM |
Syk | 98% | ||||||||||||||||
| GSK046 |
+++
BRD4BD2, IC50: 214 nM BRD3BD2, IC50: 98 nM |
98% | |||||||||||||||||
| GSK620 | ✔ | 97% | |||||||||||||||||
| Trotabresib | ✔ | 99% | |||||||||||||||||
| NHWD-870 | ✔ | 98% | |||||||||||||||||
| CFT8634 |
++++
BRD9, DC50: 3 nM |
98% | |||||||||||||||||
| GSK2801 |
++
BAZ2B, Kd: 136 nM BAZ2A, Kd: 257 nM |
99%+ | |||||||||||||||||
| KG-501 | ✔ | 99%+ | |||||||||||||||||
| UNC 669 |
+
L3MBTL4, IC50: 6 μM L3MBTL3, IC50: 35 μM |
99% | |||||||||||||||||
| PFI-3 |
+++
SMARCA2A, Kd: 72 nM SMARCA4, Kd: 55 nM |
99%+ | |||||||||||||||||
| UNC1215 |
+++
L3MBTL3- D274A, IC50: 3.5 μM L3MBTL3, IC50: 120 nM |
99%+ | |||||||||||||||||
| EED226 |
++
PRC2, Kd: 114 nM EED, Kd: 82 nM |
99%+ | |||||||||||||||||
| BRD9539 | ✔ | 98% | |||||||||||||||||
| UNC926 |
+
L3MBTL1, Kd: 3.9 μM |
99% | |||||||||||||||||
| 666-15 |
++
CREB, IC50: 81 nM |
99%+ | |||||||||||||||||
| UNC6852 |
+
EED, IC50: 247 nM |
98% | |||||||||||||||||
| BAZ1A-IN-1 |
+
BAZ1A, Kd: 0.52 μM |
99%+ | |||||||||||||||||
| PFI-4 |
++
BRPF1, IC50: 80 nM BRPF2, IC50: 7.9 μM |
99%+ | |||||||||||||||||
| OF-1 |
++
BRPF2, Kd: 500 nM BRPF1B, Kd: 100 nM |
99%+ | |||||||||||||||||
| GSK-5959 |
++
BRPF3, pIC50: 7.1 BRPF2, pIC50: 5.2 |
99% | |||||||||||||||||
| GSK6853 |
++++
BRPF1, pIC50: 8.1 |
99%+ | |||||||||||||||||
| NI-42 |
++++
BRPF1, IC50: 48 nM BRPF3, IC50: 260 nM |
99%+ | |||||||||||||||||
| E-7386 |
+++
CBP/beta-catenin, IC50: 0.0484 μM |
99% | |||||||||||||||||
| I-CBP112 |
++
p300, Kd: 167 nM CBP, Kd: 151 nM |
98+% | |||||||||||||||||
| Histone Acetyltransferase Inhibitor II |
+
p300, IC50: 5 μM |
98% | |||||||||||||||||
| C646 |
+
p300/CBP, Ki: 400 nM |
99%+ | |||||||||||||||||
| Anacardic Acid |
+
p300/CBP, IC50: 8.5 μM PCAF, IC50: 5 μM |
99%+ | |||||||||||||||||
| SGC-CBP30 |
++++
EP300, IC50: 38 nM CREBBP, IC50: 21 nM |
99%+ | |||||||||||||||||
| Nordihydroguaiaretic acid | ✔ | HER2,IGF-1R | 99%+ | ||||||||||||||||
| Curcumin |
+
p300, IC50: ~25 μM |
Ferroptosis,Nrf2,NF-κB | 98% | ||||||||||||||||
| CPI-637 |
+++
CBP, IC50: 0.03 μM EP300, IC50: 0.051 μM |
99%+ | |||||||||||||||||
| Foscenvivint | ✔ | β-catenin | 99%+ | ||||||||||||||||
| A-485 |
++
p300 HAT, IC50: 0.06 μM |
99%+ | |||||||||||||||||
| GNE-781 |
+
BRD4(1), IC50: 5100 nM |
++++
CBP, IC50: 0.94 nM |
99% | ||||||||||||||||
| NEO2734 |
+++
BET, IC50: <30 nM |
+++
p300/CBP, IC50: <30 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 | Cdc ↓ ↑ | CDK1 ↓ ↑ | CDK19 ↓ ↑ | CDK2 ↓ ↑ | CDK3 ↓ ↑ | CDK4 ↓ ↑ | CDK5 ↓ ↑ | CDK6 ↓ ↑ | CDK7 ↓ ↑ | CDK8 ↓ ↑ | CDK9 ↓ ↑ | CLK ↓ ↑ | 其他靶点 | 纯度 | |||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| XL413 HCl |
++++
Cdc7, IC50: 3.4 nM |
99%+ | |||||||||||||||||
| SU9516 |
+++
CDK1, IC50: 40 nM |
+++
CDK2, IC50: 22 nM |
++
CDK4, IC50: 200 nM |
99%+ | |||||||||||||||
| RO-3306 |
+++
CDK1, Ki: 20 nM |
ERK,SGK | 98% | ||||||||||||||||
| R547 |
++++
CDK1/CyclinB, Ki: 2 nM |
++++
CDK2/CyclinE, Ki: 3 nM |
++++
CDK4/CyclinD1, Ki: 1 nM |
99%+ | |||||||||||||||
| BMS-265246 |
++++
CDK1/CyclinB, IC50: 6 nM |
++++
CDK2/CyclinE, IC50: 9 nM |
+
CDK4/CyclinD, IC50: 230 nM |
99%+ | |||||||||||||||
| NU6027 |
+
CDK1, Ki: 2.5 μM |
+
CDK2, Ki: 1.3 μM |
DNA-PK | 98% | |||||||||||||||
| Purvalanol A |
++++
Cdc2/CyclinB, IC50: 4 nM |
+++
CDK2/CyclinE, IC50: 35 nM CDK2/CyclinA, IC50: 70 nM |
+
CDK4/CyclinD1, IC50: 850 nM |
99%+ | |||||||||||||||
| SCH900776 |
++
CDK2, IC50: 0.16 μM |
99%+ | |||||||||||||||||
| AUZ 454 |
++++
CDK2(C118L), Kd: 18.6 nM CDK2(A144C), Kd: 9.7 nM |
99%+ | |||||||||||||||||
| A-674563 HCl |
++
CDK2, Ki: 46 nM |
PKA | 99% | ||||||||||||||||
| JNJ-7706621 |
++++
CDK1/CyclinB, IC50: 9 nM |
++++
CDK2/CyclinE, IC50: 3 nM CDK2/CyclinA, IC50: 4 nM |
++
CDK3/CyclinE, IC50: 58 nM |
+
CDK4/CyclinD1, IC50: 253 nM |
++
CDK6/CyclinD1, IC50: 175 nM |
99%+ | |||||||||||||
| AT7519 |
++
CDK1/CyclinB, IC50: 210 nM |
++
CDK2/CyclinA, IC50: 47 nM |
+
CDK3/CyclinE, IC50: 360 nM |
++
CDK4/CyclinD1, IC50: 100 nM |
+++
CDK5/p35, IC50: 13 nM |
++
CDK6/CyclinD3, IC50: 170 nM |
++++
CDK9/CyclinT, IC50: <10 nM |
98+% | |||||||||||
| PHA-793887 |
++
CDK1/CyclinB, IC50: 60 nM |
++++
CDK2/CyclinE, IC50: 8 nM CDK2/CyclinA, IC50: 8 nM |
++
CDK4/CyclinD1, IC50: 62 nM |
++++
CDK5/p25, IC50: 5 nM |
++++
CDK7/CyclinH, IC50: 10 nM |
++
CDK9/CyclinT1, IC50: 138 nM |
99%+ | ||||||||||||
| Milciclib |
+
CDK1/CyclinB, IC50: 398 nM |
++
CDK2/CyclinE, IC50: 363 nM CDK2/CyclinA, IC50: 45 nM |
++
CDK4/CyclinD1, IC50: 160 nM |
+
CDK5/p35, IC50: 265 nM |
++
CDK7/CyclinH, IC50: 150 nM |
99%+ | |||||||||||||
| Kenpaullone |
+
CDK1/CyclinB, IC50: 0.4μM |
+
CDK2/CyclinE, IC50: 7.5μM CDK2/CyclinA, IC50: 0.68μM |
+
CDK5/p35, IC50: 0.85μM |
98% | |||||||||||||||
| SNS-032 |
+++
CDK2/CyclinE, IC50: 48 nM CDK2/CyclinA, IC50: 38 nM |
+
CDK5/p35, IC50: 340 nM |
++
CDK7/CyclinH, IC50: 62 nM |
++++
CDK9/CyclinT, IC50: 4 nM |
99%+ | ||||||||||||||
| Dinaciclib |
++++
CDK1, IC50: 3 nM |
++++
CDK2, IC50: 1 nM |
++++
CDK5, IC50: 1 nM |
++++
CDK9, IC50: 4 nM |
99%+ | ||||||||||||||
| PHA-767491 HCl |
++++
Cdc7, IC50: 10 nM |
+
CDK1, IC50: 250 nM |
+
CDK2, IC50: 240 nM |
+
CDK5, IC50: 460 nM |
+++
CDK9, IC50: 34 nM |
MK2 | 99% | ||||||||||||
| (R)-Roscovitine |
+
Cdc2/CyclinB, IC50: 0.65 μM |
+
CDK2/CyclinE, IC50: 0.7 μM CDK2/CyclinA, IC50: 0.7 μM |
++
CDK5/p35, IC50: 0.16 μM |
99%+ | |||||||||||||||
| Narazaciclib |
++++
CDK4/CyclinD1, IC50: 3.87 nM |
++++
CDK6/CyclinD1, IC50: 9.82 nM |
RET | 99%+ | |||||||||||||||
| Palbociclib |
++++
CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM |
+++
CDK6/CyclinD2, IC50: 15 nM |
99% | ||||||||||||||||
| Abemaciclib |
++++
CDK4, IC50: 2 nM |
++++
CDK6, IC50: 10 nM |
99% | ||||||||||||||||
| Ribociclib |
++++
CDK4, IC50: 10 nM |
+++
CDK6, IC50: 39 nM |
98% | ||||||||||||||||
| Palbociclib isethionate |
++++
CDK4/CyclinD1, IC50: 11 nM CDK4/CyclinD3, IC50: 9 nM |
+++
CDK6/CyclinD2, IC50: 15 nM |
99%+ | ||||||||||||||||
| BS-181 HCl |
+++
CDK7, IC50: 21 nM |
99%+ | |||||||||||||||||
| (E/Z)-THZ1 2HCl |
++++
CDK7, IC50: 3.2 nM |
99%+ | |||||||||||||||||
| LDC4297 |
++++
CDK7, IC50: 0.13 nM |
99%+ | |||||||||||||||||
| Senexin A |
+
CDK19, Kd: 0.31 μM |
+
CDK8, Kd: 0.83 μM |
99% | ||||||||||||||||
| MSC2530818 |
++++
CDK8, IC50: 2.6 nM |
99%+ | |||||||||||||||||
| Wogonin | ✔ | 99%+ | |||||||||||||||||
| Riviciclib HCl |
++
CDK1/CyclinB, IC50: 79 nM |
+
CDK2/CyclinE, IC50: 2.54 μM CDK2/CyclinA, IC50: 224 nM |
++
CDK4/CyclinD1, IC50: 63 nM |
+
CDK6/CyclinD3, IC50: 396 nM |
+
CDK7/CyclinH, IC50: 2.87 μM |
+++
CDK9/CyclinT1, IC50: 20 nM |
98% | ||||||||||||
| LDC000067 |
+
CDK2, IC50: 2.441 μM |
++
CDK9, IC50: 44 nM |
98% | ||||||||||||||||
| Flavopiridol |
+++
CDK1, IC50: 40 nM |
+++
CDK2, IC50: 40 nM |
+++
CDK4, IC50: 40 nM |
+++
CDK6, IC50: 40 nM |
+
CDK7, IC50: 300 nM |
+++
CDK9, IC50: 20 nM |
99%+ | ||||||||||||
| LY2857785 |
+
CDK7, IC50: 0.246 μM |
+++
CDK8, IC50: 0.016 μM |
+++
CDK9, IC50: 0.011 μM |
99%+ | |||||||||||||||
| AZD-5438 |
+++
CDK1, IC50: 16 nM |
++++
CDK2, IC50: 6 nM |
+++
CDK9, IC50: 20 nM |
99%+ | |||||||||||||||
| ML167 |
++
Dyrk1B , IC50: 1648 nM CLK4, IC50: 136 nM |
99%+ | |||||||||||||||||
| (E/Z)-TG003 |
+++
mCLK1, IC50: 200 nM mCLK4, IC50: 15 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 | 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 |
PKC,Sirtuin,Src | 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 |
DNA-PK,MLCK | 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。 | |||||||||||||||||||
| 描述 | SRX3177 serves as a multifaceted inhibitor targeting CDK4/6, PI3K, and BRD4, demonstrating IC50s of 33 nM for BRD4 BD1, 89 nM for BRD4 BD2, 79 nM for PI3Kα, 83 nM for PI3Kδ, 3.18 μM for PI3Kγ, less than 2.5 nM for CDK4, and 3.3 nM for CDK6. It exhibits extensive cytotoxic effects on cancerous cells while sparing normal epithelial cells[1]. |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.71mL 0.34mL 0.17mL |
8.55mL 1.71mL 0.86mL |
17.10mL 3.42mL 1.71mL |
|
| CAS号 | 2241237-51-2 |
| 分子式 | C31H32N6O4S |
| 分子量 | 584.69 |
| SMILES Code | O=C(C1=CC2=CN=C(NC3=CC=C(C4=CSC5=C4OC(N6CCOCC6)=CC5=O)C=C3)N=C2N1C7CCCC7)N(C)C |
| MDL No. | N/A |
| 别名 | |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 25 mg/mL(42.76 mM),配合低频超声助溶,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 |
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