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PF-04217903 methanesulfonate

Chemical Structure : PF-04217903 methanesulfonate

CAS No.: 956906-93-7

PF-04217903 methanesulfonate (PF04217903 methanesulfonate;PF 04217903 methanesulfonate)

Catalog No.: PC-42833Not For Human Use, Lab Use Only.

PF-04217903 is a potent, selective, ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM, inhibits HGF-stimulated tyrosine phosphorylation of wild type c-Met with IC50 of 7.3 nM in cell-based assays.

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

Biological Activity

PF-04217903 is a potent, selective, ATP-competitive c-Met kinase inhibitor with Ki of 4.8 nM, inhibits HGF-stimulated tyrosine phosphorylation of wild type c-Met with IC50 of 7.3 nM in cell-based assays; shows similar potency for inhibition of c-Met phosphorylation in mIMCD3 mouse epithelial cells (IC50=6.9 nM) and MDCK cell (IC50=9.5 nM); also exhibits inhibitory activities against c-Met mutations including V1092I, H1094R, M1250T, R988C, and T11010I (IC50=530 nM), but has little to no activity against mutants Y1230C and Y1235D; inhibits tumor cell proliferation, survival, migration/invasion both in vitro and in vivo.

Solid Tumors

Phase 1 Discontinued

Physicochemical Properties

M.Wt 468.489
Formula C20H20N8O4S
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

10 mM in DMSO

Chemical Name/SMILES

1H-Pyrazole-1-ethanol, 4-[1-(6-quinolinylmethyl)-1H-1,2,3-triazolo[4,5-b]pyrazin-6-yl]-, methanesulfonate (1:1)

References

1. Zou HY, et al. Mol Cancer Ther. 2012 Apr;11(4):1036-47.

2. Sennino B, et al. Cancer Res. 2013 Jun 15;73(12):3692-703.

3. Cui JJ, et al. J Med Chem. 2012 Sep 27;55(18):8091-109.

4. Yeh I, et al. Nat Commun. 2015 May 27;6:7174.

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