1676893-24-5
1676893-24-5 性质
沸点 | 775.1±70.0 °C(Predicted) |
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密度 | 1.52±0.1 g/cm3(Predicted) |
储存条件 | Store at -20°C |
溶解度 | DMF:10 mg/ml;二甲基亚砜:20 mg/ml; DMSO:PBS (pH 7.2) (1:4): 0.2mg/mL |
形态 | 固体 |
酸度系数(pKa) | 6.23±0.40(Predicted) |
颜色 | 白色至米白色 |
1676893-24-5 用途与合成方法
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.
1676893-24-5 价格(试剂级)
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024-11-08 | HY-100470 | 1676893-24-5 | 1676893-24-5 | 5mg | 1037 |
2024-11-08 | HY-100470 | 1676893-24-5 | 1676893-24-5 | 10mM * 1mLin DMSO | 1432 |