Free shipping on all orders over $ 500

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

Price and Availability

For this product's availability, delivery time and price, please email [email protected] directly or click the "Inquiry Now" button below.


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] Federico Rossari, et al. J Hematol Oncol. Past, present, and future of Bcr-Abl inhibitors: from chemical development to clinical efficacy

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

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

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

[5] 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

Related Src-bcr-Abl Products
KX2-361

KX2-361 (KX-02) is a Src-kinase and tubulin polymerization inhibitor. KX2-361 shows anti-tumor activity and induces apoptosis of Glioblastoma (GBM) cell. KX2-361 shows good oral bioavailability and readily crosses the BBB in mice.

Risvodetinib

Risvodetinib (IkT-148009) is an orally active, selective and brain-penetrant protein tyrosine kinase inhibitor, displaying excellent target efficacy against c-Abl1, c-Abl2/Arg with IC50 values of 33 nM, 14 nM, respectively.

SI-2 hydrochloride

SI-2 hydrochloride is a highly promising SRC-3 inhibitor (PPI) with acceptable oral availability, with IC50 values of 3-20 nM for breast cancer cell death.

KB SRC 4 

KB SRC 4 is a potent, and highly selective c-Src inhibitor, with a Ki of 44 nM and a Kd of 86 nM, and shows no inhibition on c-Abl up to 125 μM; KB SRC 4 has antitumor activity.

Hydroxymethyl dasatinib 

Hydroxymethyl dasatinib (M24), a benzylhydroxy metabolite of Dasatinib, exhibits an IC50 of 46.7nM in K562 CML cells.

  Catalog
Abmole Inhibitor Catalog




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

All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.



Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.