PF-04217903
PF-04217903
CAS: 956905-27-4
Molecular Formula: C19H16N8O
PF-04217903 - Names and Identifiers
PF-04217903 - Physico-chemical Properties
| Molecular Formula | C19H16N8O |
| Molar Mass | 372.38 |
| Density | 1.53 |
| Boling Point | 718.1±60.0 °C(Predicted) |
| pKa | 14.31±0.10(Predicted) |
| Storage Condition | -20℃ |
| Use | PF-04217903 is a selective, ATP competitive c-Met inhibitor with an IC50 of 4.8 nM and is sensitive to oncogene mutations (no activity to Y1230C mutations). |
| In vitro study | PF-04217903 is more selective than Staurosporine or PF-02341066, PF-04217903 acts on c-Met more than 1000 times more selective than the other group of 208 kinases, and is more sensitive to c-Met oncogenic mutations. In addition to acting on WT c-Met,PF-04217903 also effectively inhibits c-Met-H1094R, c-Met-R988C, and c-Met-T1010I activities, with IC50 of 3.1 nM, 6.4 nM, and 6.7 nM, respectively, but has little inhibitory effect on c-Met-Y1230C, IC50 >10 μm. The combination of PF-04217903 and Sunitinib significantly inhibited endothelial cell proliferation, but not tumor cells B16F1, Tib6, EL4, and LLC. PF-04217903 significantly inhibited the growth of LXFA 526L and LXFA 1647L clones with IC50 of 16 nM and 13 nM, respectively, and the effect was enhanced when combined with Cetuximab. PF-04217903 effectively inhibits c-Met-driven biological processes such as growth, motility, invasion and morphological changes of a variety of tumor cells. 2 μm PF-04217903 treatment of GTL-16 cells, promoting cell death, involving down-regulation of phosphorylated 4E-BP1, ERK/MAPK-related proteins, and the PI3K/AKT pathway. |
| In vivo study | Although it acts on the B16F1 and Tib6 tumor models sensitive to Sunitinib and cannot inhibit tumor growth, the combination of PF-04217903 and Sunitinib acts on the EL4 and LLC tumor models resistant to Sunitinib, compared with the two being administered separately, the significant inhibition of tumor growth by significantly blocking vasodilation suggests that the key role in Sunitinib-resistant tumors is the HGF/c-Met axis. |
PF-04217903 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.685 ml | 13.427 ml | 26.854 ml |
| 5 mM | 0.537 ml | 2.685 ml | 5.371 ml |
| 10 mM | 0.269 ml | 1.343 ml | 2.685 ml |
| 5 mM | 0.054 ml | 0.269 ml | 0.537 ml |
Last Update：2024-01-02 23:10:35
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Tel: 609-228-6898
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Product Name: PF-04217903 Visit Supplier Webpage Request for quotation
CAS: 956905-27-4
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Email: 3008007409@qq.com
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QQ: 3008007409
CAS: 956905-27-4
Tel: 18301782025
Email: 3008007409@qq.com
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