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HG-7-85-01 

Cat. No. M28074

All AbMole products are for research use only, cannot be used for human consumption.

HG-7-85-01  Structure

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Quality Control & Documentation
Biological Activity

HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC50s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC50>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression.

Chemical Information
Molecular Weight 608.68
Formula C31H31F3N6O2S
CAS Number 1258391-13-7
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
References

[1] Hwan Geun Choi, et al. Bioorg Med Chem Lett. Development of 'DFG-out' inhibitors of gatekeeper mutant kinases

[2] Ellen Weisberg, et al. PLoS One. Reversible resistance induced by FLT3 inhibition: a novel resistance mechanism in mutant FLT3-expressing cells

[3] Ellen Weisberg, et al. Mol Cancer Ther. Discovery and characterization of novel mutant FLT3 kinase inhibitors

[4] Ellen Weisberg, et al. Blood. Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRalpha, Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants

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  Catalog
Abmole Inhibitor Catalog




Keywords: HG-7-85-01  supplier, Src-bcr-Abl, inhibitors, activators

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