NSC781406

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NSC781406 是一种高效的 PI3K 和 mTOR 抑制剂（PI3Kα 的 IC50：2 nM）。

NSC781406 is a highly effective inhibitor of PI3K and mTOR (IC50: 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.

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.

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PI3K/Akt/mTOR signaling

mTOR

mTOR|PI3Kα|PI3Kβ|PI3Kγ|PI3Kδ

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1676893-24-5

627.68

C29H27F2N5O5S2

>98% (HPLC)

DMSO:150 mg/mL (238.98 mM)

FC1=CC(F)=CC=C1S(=O)(NC2=CC(C3=CC=C(N=CC=C4C#CCN5CCN(S(C)(=O)=O)CC5)C4=C3)=CN=C2OC)=O

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(-20℃)

With Ice Pack

≥ 2 years