HG-7-85-01

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].

Product Specifications

CAS Number

[1258391-13-7]

UNSPSC

12352005

Target

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

Purity

99.94

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 Formula

C31H31F3N6O2S

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.