SGX-523

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Chemical Information

Product name：SGX-523	Purity：98% min
CAS NO：1022150-57-7	Solubility：DMSO : ≥ 3.6 mg/mL (10.02 mM)
Molecular Formula：C₁₈H₁₃N₇S	Package：Package according to customer requirements
Molecular Weight：359.408	Storage：Store at -20℃

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Remarks

SGX523 is a novel, ATP-competitive kinase inhibitor remarkable for its exquisite selectivity for MET. SGX523 potently inhibited MET with an IC50 of 4 nmol/L and is >1,000-fold selective versus the >200-fold selectivity of other protein kinases tested in biochemical assays. Crystallographic study revealed that SGX523 stabilizes MET in a unique inactive conformation that is inaccessible to other protein kinases, suggesting an explanation for the selectivity. SGX523 inhibited MET-mediated signaling, cell proliferation, and cell migration at nanomolar concentrations but had no effect on signaling dependent on other protein kinases, including the closely related RON, even at micromolar concentrations.

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Capmatinib; MK-8033; Merestinib; MDK-0264; Tepotinib; NPS-1034; WYE-125132; PHA-665752; SCR-1481B1; SU11606

References

[1]. Buchanan SG, 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, 8(12), 3181-3190.

[2]. Shen A, 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.