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NSC781406
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NSC781406图片
CAS NO:1676893-24-5
规格:98%
分子量:627.68
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
NSC781406是高效的PI3K和mTOR抑制剂,对PI3Kα的IC50值为2nM。
CAS:1676893-24-5
分子式:C29H27F2N5O5S2
分子量:627.68
纯度:98%
存储:Store at -20°C

Background:

NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.


NSC781406 demonstrates potent PI3K inhibition (PI3Kα IC50=2.0 nM) that translates into BEL-7404 cells proliferation inhibition (IC50=20 nM). NSC781406 displays reasonable liver microsome stability. NSC781406 demonstrates cytotoxic activities against leukemia, non-small cell, lung cancer, colon cancer, central nervous system cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, and breast cancer. It is potent against 60 cancer cell lines with a mean GI50 value of 65 nM, and with a GI50 value less than 10 nM against four cancer cell lines[1].


In the xenograft models, treatment with 30 mg/kg of NSC781406 results in statistically significant antitumor activity, with a mean reduction in relative tumor volume ratio of 52%. Sorafenib displays an inhibition ratio of 44% at 50 mg/kg. NSC781406 is well tolerated at 30 mg/kg, with no observed mortality or significant reduction of body weight[1].


[1]. Chen Y, et al. Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinoma. Bioorg Med Chem. 2016 Mar 1;24(5):957-66.