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Chemical Structure : PF-04217903 methanesulfonate
CAS No.: 956906-93-7
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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $88 | In stock | |
| 50 mg | $258 | In stock | |
| 100 mg | $478 | In stock | |
| 500 mg | Get quote |
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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
| M.Wt | 468.489 | |
| Formula | C20H20N8O4S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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) |
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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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