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1619903-54-6

中文名稱 LY-2857785
英文名稱 LY2857785
CAS 1619903-54-6
分子式 C26H36N6O
分子量 448.6
MOL 文件 1619903-54-6.mol
更新日期 2023/03/20 15:41:27
1619903-54-6 結(jié)構(gòu)式 1619903-54-6 結(jié)構(gòu)式

基本信息

中文別名
CDK9,CDK8和CDK7抑制劑(LY2857785)
英文別名
LY2857785
LY2857785 (LY 2857785
1,4-Cyclohexanediamine, N1-[4-[2-methyl-3-(1-methylethyl)-2H-indazol-5-yl]-2-pyrimidinyl]-N4-(tetrahydro-2H-pyran-4-yl)-, trans-
所屬類別
生物化工:激動劑抑制劑

物理化學性質(zhì)

沸點671.0±65.0 °C(Predicted)
密度1.29±0.1 g/cm3(Predicted)
儲存條件Keep in dark place,Sealed in dry,2-8°C
溶解度insoluble in H2O; ≥13.87 mg/mL in EtOH with gentle warming; ≥2.63 mg/mL in DMSO with gentle warming and ultrasonic
酸度系數(shù)(pKa)10.05±0.40(Predicted)
形態(tài)粉末
顏色White to off-white
LY-2857785價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-12293LY-2857785
LY2857785
1619903-54-62mg1100元
2024/11/08HY-12293LY-2857785
LY2857785
1619903-54-65mg1800元
2024/11/08HY-12293LY-2857785
LY2857785
1619903-54-610 mM * 1 mLin DMSO2073元

常見問題列表

生物活性
LY2857785 是一種I型可逆的 ATP 競爭性的 CDK9,CDK8 和 CDK7 抑制劑,IC50 分別為 11 nM,16 nM 和 246 nM。
靶點

CDK9

0.011 μM (IC 50 )

CDK8

0.016 μM (IC 50 )

CDK7

0.246 μM (IC 50 )

體外研究

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.

體內(nèi)研究

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.

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