HG-7-85-01

HG-7-85-01

• CAS Number: 1258391-13-7
• UNSPSC 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].
• Target Antigen: Apoptosis; Bcr-Abl; c-Kit; JAK; PDGFR; Src
• Type: Reference compound
• Related Pathways: Apoptosis;Epigenetics;JAK/STAT Signaling;Protein Tyrosine Kinase/RTK;Stem Cell/Wnt
• Applications: Cancer-Kinase/protease
• Field of Research: Cancer
• Assay Protocol: https://www.medchemexpress.com/hg-7-85-01.html
• Solubility: DMSO : 125 mg/mL (ultrasonic)
• 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
• Molecular Weight: 608.68
• References & Citations: [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.
• Shipping Conditions: Room Temperature
• Clinical Information: No Development Reported