| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| N654532-1ml |
1ml |
期货  |
|
| 规格或纯度 | 10mM in DMSO |
|---|---|
| 英文名称 | NSC781406 |
| 生化机理 | NSC781406 是一种高效的 PI3K 和 mTOR 抑制剂，对 PI3Kα 的 IC 50 为 2 nM。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 产品介绍 |
NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC 50 of 2 nM for PI3Kα . In Vitro 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target: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 ) |
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | COC1=C(C=C(C=N1)C2=CC3=C(C=CN=C3C=C2)C#CCN4CCN(CC4)S(=O)(=O)C)NS(=O)(=O)C5=C(C=C(C=C5)F)F |
| PubChem CID | 127025628 |
| 分子量 | 627.68 |
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