SGX-523 C Met Inhibitors Cas 1022150-57-7 Atp Competitive Kinase Inhibitors
SGX-523 C Met Inhibitors Cas 1022150-57-7 Atp Competitive Kinase Inhibitors
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Chemical Information
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Product name:SGX-523 |
Purity:98% min |
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CAS NO:1022150-57-7 |
Solubility:DMSO3.6 mg/mL (10.02 mM) |
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Molecular Formula:C18H13N7S |
Package:Package according to customer requirements |
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Molecular Weight:359.408 |
Storage:Store at -20℃ |
Quality control
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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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.
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