HG-7-85-01

• 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

• CAS Number:

  1258391-13-7