LY-2857785
中文名稱 | LY-2857785 |
---|---|
中文同義詞 | CDK9,CDK8和CDK7抑制劑(LY2857785);反式-N1-(4-(3-異丙基-2-甲基-2H-吲唑-5-基)嘧啶-2-基)-N4-(四氫-2H-吡喃-4-基)環(huán)己烷-1,4-二胺;化合物L(fēng)Y2857785;化合物L(fēng)Y2857785,10 MM DMSO 溶液 |
英文名稱 | LY2857785 |
英文同義詞 | 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-;trans-N1-(4-(3-Isopropyl-2-methyl-2H-indazol-5-yl)pyrimidin-2-yl)-N4-(tetrahydro-2H-pyran-4-yl)cyclohexane-1,4-diamine;Cyclin dependent kinase,LY 2857785,CDK,Apoptosis,LY2857785,Inhibitor,inhibit,LY-2857785;LY2857785, 10 mM in DMSO |
CAS號 | 1619903-54-6 |
分子式 | C26H36N6O |
分子量 | 448.6 |
EINECS號 | |
相關(guān)類別 | 細(xì)胞生物學(xué)試劑 |
Mol文件 | 1619903-54-6.mol |
結(jié)構(gòu)式 | ![]() |
LY-2857785 性質(zhì)
沸點(diǎn) | 671.0±65.0 °C(Predicted) |
---|---|
密度 | 1.29±0.1 g/cm3(Predicted) |
儲存條件 | 2-8°C(protect from light) |
溶解度 | 不溶于水;溫和加熱時(shí),乙醇溶液中≥13.87 mg/mL; DMSO 中≥2.63 mg/mL,溫和加熱和超聲波 |
形態(tài) | 粉末 |
酸度系數(shù)(pKa) | 10.05±0.40(Predicted) |
顏色 | 白色至米白色 |
CDK9 0.011 μM (IC 50 ) |
CDK8 0.016 μM (IC 50 ) |
CDK7 0.246 μM (IC 50 ) |
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.
安全信息
更新日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價(jià)格 |
---|---|---|---|---|---|
2025/02/08 | HY-12293 | LY-2857785 LY2857785 | 1619903-54-6 | 1 mg | 774元 |
2025/02/08 | HY-12293 | LY-2857785 LY2857785 | 1619903-54-6 | 2mg | 1100元 |