LY-2857785
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- CAS号:
- 1619903-54-6
- 英文名:
- LY2857785
- 英文别名:
- LY2857785;LY2857785
(LY 2857785;Cyclin dependent kinase,LY 2857785,CDK,Apoptosis,LY2857785,Inhibitor,inhibit,LY-2857785;trans-N1-(4-(3-Isopropyl-2-methyl-2H-indazol-5-yl)pyrimidin-2-yl)-N4-(tetrahydro-2H-pyran-4-yl)cyclohexane-1,4-diamine;1,4-Cyclohexanediamine, N1-[4-[2-methyl-3-(1-methylethyl)-2H-indazol-5-yl]-2-pyrimidinyl]-N4-(tetrahydro-2H-pyran-4-yl)-, trans-
- 中文名:
- LY-2857785
- 中文别名:
- 化合物LY2857785;CDK9,CDK8和CDK7抑制剂(LY2857785);反式-N1-(4-(3-异丙基-2-甲基-2H-吲唑-5-基)嘧啶-2-基)-N4-(四氢-2H-吡喃-4-基)环己烷-1,4-二胺
- CBNumber:
- CB02715647
- 分子式:
- C26H36N6O
- 分子量:
- 448.6
- MOL File:
- 1619903-54-6.mol
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LY-2857785化学性质
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沸点:
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671.0±65.0 °C(Predicted)
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密度:
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1.29±0.1 g/cm3(Predicted)
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储存条件:
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2-8°C(protect from light)
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溶解度:
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insoluble in H2O; ≥13.87 mg/mL in EtOH with gentle warming; ≥2.63 mg/mL in DMSO with gentle warming and ultrasonic
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形态:
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Powder
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酸度系数(pKa):
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10.05±0.40(Predicted)
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颜色:
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White to off-white
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LY-2857785性质、用途与生产工艺
LY2857785 是一种I型可逆的 ATP 竞争性的 CDK9,CDK8 和 CDK7 抑制剂,IC50 分别为 11 nM,16 nM 和 246 nM。
CDK9
0.011 μM (IC
50
)
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CDK8
0.016 μM (IC
50
)
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CDK7
0.246 μM (IC
50
)
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LY2857785 shows good selectivity against a panel of 114 protein kinases, with only 5 other protein kinases inhibited with potency (IC
50
) less than 0.1 μM, and a total of 14 kinases less than 1 μM. At the cellular level, LY2857785 inhibits CTD P-Ser2 and CTD P-Ser5 in U2OS cells at IC
50
s 0.089 (n=13) and 0.042 (n=1) μM, respectively. However, LY2857785 only induces a moderate G
2
-M DNA content increase, from 35% to 55%, with EC
50
0.135 μM. LY2857785 shows potent compound exposure- and time-dependent cell proliferation inhibition in MV-4-11, RPMI8226, and L363 cells. When incubated between 4 to 24 hours, the cell growth inhibition potency reaches a maximal effect at 8 hours with IC
50
s 0.04, 0.2, and 0.5 μM for MV-4-11, RPMI8226, and L363 cells, respectively. LY2857785-induced cancer cell apoptosis is also time dependent, reaching maximal potency at 8 hours with IC
50
0.5 μM in L363 cells.
In HCT116 xenograft tumor-bearing mice, LY2857785 demonstrates dose-dependent RNAP II CTD P-Ser2 inhibition potently with TED50 of 4.4 mg/kg and TEC50 of 0.36 μM. LY2857785 also shows significant duration of CTD P-Ser2 inhibition for 3 to 6 hours at TED70 (8 mg/kg) in HCT116 and MV-4-11 nude mice xenograft models. In the nude rat MV-4-11 xenograft model, LY2857785 similarly shows dose-dependent CTD P-Ser2 inhibition for 8 hours at TED70 (7 mg/kg) and TED90 (10 mg/kg). LY2857785 demonstrates the most dramatic tumor regression in the AML MV-4-11 xenograft tumor model either by i.v. bolus in mice or i.v. infusion in rats.
LY-2857785
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
---|
2024/04/30 | HY-12293 | LY-2857785 LY2857785 | 1619903-54-6 | 2mg | 1100元 |
2024/04/30 | HY-12293 | LY-2857785 LY2857785 | 1619903-54-6 | 5mg | 1800元 |
1619903-54-6, LY-2857785 相关搜索:
- 药靶配体
- 细胞生物学试剂
- C26H36N6O
- 化合物LY2857785
- 反式-N1-(4-(3-异丙基-2-甲基-2H-吲唑-5-基)嘧啶-2-基)-N4-(四氢-2H-吡喃-4-基)环己烷-1,4-二胺
- CDK9,CDK8和CDK7抑制剂(LY2857785)
- 1619903-54-6
- Cyclin dependent kinase,LY 2857785,CDK,Apoptosis,LY2857785,Inhibitor,inhibit,LY-2857785
- trans-N1-(4-(3-Isopropyl-2-methyl-2H-indazol-5-yl)pyrimidin-2-yl)-N4-(tetrahydro-2H-pyran-4-yl)cyclohexane-1,4-diamine
- 1,4-Cyclohexanediamine, N1-[4-[2-methyl-3-(1-methylethyl)-2H-indazol-5-yl]-2-pyrimidinyl]-N4-(tetrahydro-2H-pyran-4-yl)-, trans-
- LY2857785
(LY 2857785
- LY2857785