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BMS-599626 | Her1/Her2 inhibitor

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Catalog #:

Product Description

BMS-599626 is a pyrrolotriazine-based inhibitor of HER1, HER2, and HER4 kinases at IC50s of 20 nM, 30 nM, and 190 nM, respectively. Aside from micromolar potency for Lck and MEK (4 uM, and 2.5 uM, respectively), it is highly selective (>40 uM) over a wide panel of kinases. [1] Studies indicate that BMS-599626 inhibits HER1 and HER2 through distinct mechanisms. BMS-599626 is believed to be ATP competitive for HER1, while ATP-non-competitive for HER2. [1] Proliferation of cell lines dependent on HER1 and HER2 was measured in the range of 0.24 to 1 uM; cell lines not dependent on HER signaling were not affected by BMS-599626.

In Sal2 tumor cell lines, BMS-599626 was found to inhibit phosphorylation of CD8HER2 and MAPK in a dose-dependent manner. [1] In OV202 cells, BMS-599626 has been shown to work in synergy with IGF-1R inhibitors by the mechanism of enhanced apoptosis. [2]

Technical information:

Chemical Formula:   C27H27FN8O3.HCl
CAS #:   873837-23-1
Molecular Weight:   567.01
Purity:   >98%
Appearance:   White
Chemical Name:   N-(4-(2-amino-3-chloropyridin-4-yloxy)-3-fluorophenyl)-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide
Solubility:   Up to 100 mM in DMSO
Synonyms:   BMS-599626, BMS 599626, BMS599626, AC480

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


1. Wong et al., Preclinical antitumor activity of BMS-599626, a pan-HER kinase inhibitor that inhibits HER1/HER2 homodimer and heterodimer signaling. Clin Cancer Res. 2006, 12, 6186-6193. Pubmed ID: 17062696
2. Haluska et al., HER receptor signaling confers resistance to the insulin-like growth factor-I receptor inhibitor, BMS-536924. Mol. Cancer Ther. 2008, 7, 2589-2598. Pubmed ID: 18765823

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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