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BMS 777607

Chemical Structure : BMS 777607

CAS No.: 1025720-94-8

BMS 777607 (BMS777607, ASLAN002, BMS 817378)

Catalog No.: PC-42888Not For Human Use, Lab Use Only.

BMS 777607 (ASLAN002) is a potent, selective, orally efficacious inhibitor of Met kinase with IC50 of 3.9 nM, also potently inhibits Ron, Axl, Tyro-3 and Mer (IC50<15 nM), 40-fold selectivity over Lck, VEGFR-2 and TrkA/B.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

BMS 777607 (ASLAN002) is a potent, selective, orally efficacious inhibitor of Met kinase with IC50 of 3.9 nM, also potently inhibits Ron, Axl, Tyro-3 and Mer (IC50<15 nM), 40-fold selectivity over Lck, VEGFR-2 and TrkA/B.
BMS 777607 inhibits cell scattering activated by exogenous HGF in c-Met-expressing PC-3 and DU145 prostate cancer cells, suppresses HGF-stimulated cell migration and invasion with IC50 of <0.1 uM.
BMS 777607 potently blocks HGF-stimulated c-Met autophosphorylation and downstream activation of Akt and ERK at nanomolar level.
BMS 777607 demonstrates complete tumor stasis in Met-dependent GTL-16 human gastric carcinoma xenograft models.

Physicochemical Properties

M.Wt 512.8926
Formula C25H19ClF2N4O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 39 mg/mL

Chemical Name/SMILES

3-Pyridinecarboxamide, N-[4-[(2-amino-3-chloro-4-pyridinyl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-1,2-dihydro-2-oxo-

References

1. Schroeder GM, et al. J Med Chem. 2009 Mar 12;52(5):1251-4.

2. Dai Y, et al. Mol Cancer Ther. 2010 Jun;9(6):1554-61.

3. Dai Y, et al. Clin Exp Metastasis. 2012 Mar;29(3):253-61.

4. Onken J, et al. Oncotarget. 2016 Mar 1;7(9):9876-89.

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