OTS186935

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

OTS186935 

OTS186935 是一种有效的蛋白甲基转移酶 SUV39H2 抑制剂,IC50 值为 6.49 nM。OTS186935 对小鼠异种移植模型的肿瘤生长有明显的抑制作用,且无明显毒性。OTS193320 调节癌细胞中 γ-H2AX 的产生。

OTS186935

OTS186935 Chemical Structure

CAS No. : 2093400-18-9

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OTS186935 的其他形式现货产品:

OTS186935 hydrochloride

生物活性

OTS186935 is a potent protein methyltransferase SUV39H2 inhibitor with an IC50 of 6.49 nM. OTS186935 shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 regulates the production of γ-H2AX in cancer cells[1].

IC50 & Target

IC50: 6.49 nM (SUV39H2)[1]

体外研究
(In Vitro)

OTS186935 inhibits A549 cell growth with an IC50 of 0.67 μM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female NOD.CB17-Prkdcscid/J mice (bearing MDA-MB-231 cells )[1]
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)[1]
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.

分子量

463.96

Formula

C25H26ClN5O2

CAS 号

2093400-18-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Vougiouklakis T, et al. Development of novel SUV39H2 inhibitors that exhibit growth suppressive effects in mouse xenograft models and regulate the phosphorylation of H2AX. Oncotarget. 2018 Aug 7;9(61):31820-31831.

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