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SGX-523

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Chemical Structure| 1022150-57-7 同义名 : -
CAS号 : 1022150-57-7
货号 : A263510
分子式 : C18H13N7S
纯度 : 99%+
分子量 : 359.408
MDL号 : MFCD16660190
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(83.47 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

0.5% methylcellulose+0.2% Tween 80+water 30 mg/mL suspension

生物活性
描述 Hepatocyte growth factor (HGF) receptor, c-Met, is the prototypic member of a family of receptor tyrosine kinases unique to deuterostomes and has emerged as an important target for the development of novel cancer therapeutics. SGX523 is a novel, ATP-competitive and selective c-Met inhibitor with an IC50 of 4 nM and a Ki of 2.7 nM. In the gastric cancer cell line GTL16, c-Met gene amplification led to constitutive signaling, which was abolished by SGX523 with an IC50 of 0.04 μM. SGX523 also abrogated HGF induced signaling in A549 lung cancer cells with an IC50 of 0.012 μM for the inhibition of c-Met autophosphorylation. Further, SGX523 inhibited the growth of gastric and lung cancer cell lines with amplification of the c-Met gene. In vivo, SGX523 significantly retarded the growth of preestablished GTL16 tumors when administered orally at doses of ≥10 mg/kg twice daily. Moreover, SGX523 (10 mg/kg; twice daily) potently inhibited U87MG tumor growth; SGX523 (30 mg/kg; twice daily) led to clear regression of U87MG tumors[3].
作用机制 SGX-523 binds to the ATP site of an inactive conformation[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.78mL

0.56mL

0.28mL

13.91mL

2.78mL

1.39mL

27.82mL

5.56mL

2.78mL
参考文献

[1]Shen A, Wang L, et al. c-Myc alterations confer therapeutic response and acquired resistance to c-Met inhibitors in MET-addicted cancers. Cancer Res. 2015 Nov 1;75(21):4548-59.

[2]Buchanan SG, Hendle J, et al. SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo. Mol Cancer Ther. 2009 Dec;8(12):3181-90.

[3]Buchanan SG, Hendle J, Lee PS, et al. SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo. Mol Cancer Ther. 2009 Dec;8(12):3181-90