OTS186935 hydrochloride 是一种有效的蛋白甲基转移酶SUV39H2抑制剂,IC50值为 6.49 nM。OTS186935 hydrochloride 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 hydrochloride 调节癌细胞中 γ-H2AX 的产生。
产品描述
OTS186935 hydrochloride is a potent protein methyltransferase SUV39H2 inhibitor with an IC 50 of 6.49 nM. OTS186935 hydrochloride shows significant inhibition of tumor growth in mouse xenograft models without any detectable toxicity. OTS193320 hydrochloride regulates the production of γ-H2AX in cancer cells [1].
体外活性
OTS186935 hydrochloride inhibits A549 cell growth with an IC 50 of 0.67 μM [1].
体内活性
OTS186935 hydrochloride (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]. 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.
分子式
C25H27Cl2N5O2
分子量
522.31
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years