1676893-24-5
基本信息
NSC-781406
NSC 781406
NSC781406
NSC-781406
NSC 781406
Benzenesulfonamide, 2,4-difluoro-N-[2-methoxy-5-[4-[3-[4-(methylsulfonyl)-1-piperazinyl]-1-propyn-1-yl]-6-quinolinyl]-3-pyridinyl]-
物理化學(xué)性質(zhì)
報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
2024/11/08 | HY-100470 | 1676893-24-5 NSC781406 | 1676893-24-5 | 5mg | 1037元 |
2024/11/08 | HY-100470 | 1676893-24-5 NSC781406 | 1676893-24-5 | 10mM * 1mLin DMSO | 1432元 |
2024/11/08 | HY-100470 | 1676893-24-5 NSC781406 | 1676893-24-5 | 10mg | 1660元 |
常見問題列表
PI3Kα 2 nM (IC 50 ) |
PI3Kγ 2.7 nM (IC 50 ) |
PI3Kβ 9.4 nM (IC 50 ) |
PI3Kδ 14 nM (IC 50 ) |
mTOR 5.4 nM (IC 50 ) |
NSC781406 demonstrates potent PI3K inhibition (PI3Kα IC 50 =2.0 nM) that translates into BEL-7404 cells proliferation inhibition (IC 50 =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 GI 50 value of 65 nM, and with a GI50 value less than 10 nM against four cancer cell lines.
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.