NSC781406

A dual inhibitor of PI3K and mTOR

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库存: 现货

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数量
1mg

￥650.00

520.00

- +
5mg

￥1300.00

1040.00

- +
10mg

￥2175.00

1740.00

- +
50mg

￥6475.00

5180.00

- +
100mg

￥12837.00

10270.00

- +

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Background

NSC 781406 is a dual inhibitor of PI3K and mammalian target of rapamycin (mTOR; IC₅₀s = 2.0, 9.4, 2.7, 14, and 5.4 nM for PI3Kα, PI3Kβ, PI3Kγ, PI3Kδ, and mTOR, respectively).¹ It inhibits cell growth in the NCI-60 panel of cancer cell lines (mean GI₅₀ = 65 nM). NSC 781406 (30 mg/kg) reduces tumor volume in a BEL-7404 hepatic cancer mouse xenograft model.

1.Chen, Y., Zhang, L., Yang, C., et al.Discovery of benzenesulfonamide derivatives as potent PI3K/mTOR dual inhibitors with in vivo efficacies against hepatocellular carcinomaBioorg. Med. Chem.24(5)957-966(2016)

Protocol

Kinase experiment:	IC50 values for inhibition of the PI3K is measured. PI-103 is used as the reference compound. The compounds (NSC781406) are tested in duplicate for 10 concentrations, 100 nM or 500 nM as the top concentration. All reagents are diluted in kinase buffer.Three-fold, ten-point serial compound (NSC781406) dilutions are performed in kinase buffer[1].
Cell experiment:	Cytotoxic effects are tested in the human lung adenocarcinoma cells A549, human colon cancer cells HCT-116, human breast cancer cells MDA-MB-231 and human hepatocellular carcinoma cells BEL-7404. These four tumor cells are diluted to a density of 40,000–50,000 cells/mL in logarithmic phase. After the cells are treated with compounds (NSC781406) for 72 h, MTT solution (5 mg/mL, 20 μL) is added another 4h at 37°C. IC50 values are determined by a nonlinear regression analysis[1].
Animal experiment:	Mice: NSC781406 is orally administered once a day 30 mg/kg for 14 consecutive days or with sorafenib at 50 mg/kg. The relative tumor volume to vehicle-treated control mice is monitored[1].
参考文献: [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.