PF-04217903 Chemical Structure
Inhibitor of the c-Met kinase and the NPM-ALK. Crizotinib (PF02341066) inhibited cell proliferation in ALK-positive ALCL cells (IC50s=30 nM).
PHA-665752 is c-Met inhibitor with an IC50 of 9 nM and Ki of 4 nM.
SU11274 is a c-Met inhibitor (IC50 at 0.012μM).
Foretinib (GSK1363089, XL880) is a novel MET and VEGFR2/KDR kinases inhibitor with an IC50 of 0.4 and 0.8 nM for MET and KDR, respectively.
SGX-523 is an exquisitely selective MET receptor tyrosine kinase inhibitor with an IC50 of 4 nM.
JNJ-38877605 is a c-MET inhibitor with an IC50 of 4 nM.
XL-184 free base (Cabozantinib) is a potent multitargeted VEGFR2, Met, FLT3, Tie2, Kit and Ret inhibitor with IC50 of 0.035, 1.8, 14.4, 14.3 and 4.6 nM for VEGFR2, Met, FLT3, Tie2 and Kit, respectively.
MP-470 (Amuvatinib) is a multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Met, c-Kit, PDGFRalpha, Flt3, and c-Ret and with an IC50 of median 5 μM.
AMG-208 is a potent small molecular c-Met inhibitor with an IC50 of 9.3 nM.
MGCD-265 is a multi-targeted kinase inhibitor, which targets the c-MET, VEGFR1, VEGFR2, VEGFR3, Tie-2 and Ron receptor tyrosine kinases.
PF-04217903 is an orally bioavailabe, small-molecule MET tyrosine kinase inhibitor with potential antineoplastic activity. [1]
PF-04217903 demonstrates exquisite kinase selectivity. Inhibition studies of the c-Met mutants show that PF-04217903 is more susceptible to oncogenic mutations that attenuate potency than PF-02341066. [1]
PF-04217903 was evaluated against multiple kinase selectivity screening panels: Invitrogen Inc. (125 kinases), Millipore/Upstate Ltd. (105 kinases), University ofDundee (51 kinases), and Pfizer in-house (48 kinases) (Supporting Information). On the basis of the percent inhibition or IC50 values generated from each of these screens, PF-04217903 was estimated to be>1000-fold selective for c-Met compared with each of the other kinases included in these collective screening assays. [1]
| Molecular Weight (WM): | 372.38 |
|---|---|
| Formula: | C19H16N8O |
| CAS No.: | 956905-27-4 |
| Synonyms: |
N/A
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| Dissolve in (25°C): | DMSO ≥75mg/mL |
| Water <1mg/mL | |
| Ethanol <1mg/mL | |
| Storage: | 2 years-20°CPowder |
| 1 week-4°Cin DMSO | |
| 1 month-80°in DMSO |
A collection of 864 bioactive compounds
A collection of 481 inhibitors
A collection of 194 kinase inhibitors
A collection of 85 tyrosine kinase inhibitors.
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A unique collection of 17 small molecule modulators
A unique collection of 47 small molecule inhibitors
A unique collection of 63 GPCR small molecules

Western blot analysis of c-Met, MAPK and Akt. 0-100nM PF04217903 was added.
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Western blot analysis of c-Met, MAPK and Akt. 0-100nM PF04217903 was added.
Data independently produced by Dr. Zhang of Tianjin Medical University PF-04217903 purchased from Selleck
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