OTS186935

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

OTS186935 (OTS-186935) 是一种有效的体内活性蛋白甲基转移酶 SUV39H2 抑制剂，IC50 为 6.49 nM。

OTS186935 (OTS-186935) is a potent, in vivo-active inhibitor of protein methyltransferase SUV39H2 with IC50 of 6.49 nM, inhibits A549 cell growth with IC50 of 0.67 uM; causes a significant growth inhibitory effect in mouse xenograft models using MDA-MB-231 breast cancer cells as well as A549 lung cancer cells, at 25 mg/kg once daily for 14 days yielded a TGI of 60.8%; attenuates the levels of H3K9me3 in A549 xenograft mouse model.

OTS186935 inhibits A549 cell growth with an IC50 of 0.67 μM.

OTS186935 (10 mg/kg or 25 mg/kg; intravenously; once daily for 14 days) exhibits growth suppressive effects in human cancer cell line derived xenograft models. Animal Model:Female NOD.CB17-Prkdcscid/J mice(bearing MDA-MB-231 cells )Dosage:10 mg/kg Administration:Intravenously; once daily for 14 days Result:Tumor growth inhibition of 42.6% on day 14.Animal Model:Female BALB/cAJcl-nu/nu mice (bearing A549 cells)Dosage:25 mg/kg Administration:Intravenously; once daily for 14 days Result:Yielded a tumor growth inhibition of 60.8% without significant body weight loss or toxicity.

OTS-186935 | OTS 186935

Chromatin/Epigenetic

HMTase

HMTase

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——

2093400-18-9

463.966

C25H26ClN5O2

>98% (HPLC)

——

COC1=CC(=C(C=C1C2=CN3C=CC(=CC3=N2)N4CCC(C4)NCC5=CC=NC=C5)Cl)OC

(S)-1-(2-(5-chloro-2,4-dimethoxyphenyl)imidazo[1,2-a]pyridin-7-yl)-N-(pyridin-4-ylmethyl)pyrrolidin-3-amine

(-20℃)

With Ice Pack

≥ 2 years