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LY-2857785

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 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

LY-2857785 用途與合成方法

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。

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

MSDS信息

更新日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價(jià)格
2025/02/08HY-12293LY-2857785
LY2857785
1619903-54-61 mg774元
2025/02/08HY-12293LY-2857785
LY2857785
1619903-54-62mg1100元

LY-2857785 上下游產(chǎn)品信息

"LY-2857785"相關(guān)產(chǎn)品信息
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