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Products Details
Product Description
– 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[1].
Web ID
– HY-15814
Shipping
– Room temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C31H31F3N6O2S
References
– [1]Ellen Weisberg, et al. 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. Blood. 2010 May 27;115(21):4206-16.
CAS Number
– 1258391-13-7
Molecular Weight
– 608.68
SMILES
– O=C(NC1=CC=C(CN2CCN(CC)CC2)C(C(F)(F)F)=C1)C3=CC=CC(C4=CC=C5C(SC(NC(C6CC6)=O)=N5)=N4)=C3
Clinical Information
– No Development Reported
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– Apoptosis;Bcr-Abl;c-Kit;JAK;PDGFR;Src
Isoform
– Bcr-Abl;JAK1;PDGFRα
Pathway
– Apoptosis;Epigenetics;JAK/STAT Signaling;Protein Tyrosine Kinase/RTK;Stem Cell/Wnt
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
