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Lifirafenib (BGB-283) is a novel potent and selective RAF Kinase and EGFR inhibitor with IC50 values of 23, 29 and 495 nM for the recombinant BRAFV600E kinase domain, EGFR and EGFR T790M/L858R mutant. In BRAFV600E colorectal cancer cell lines, BGB-283 effectively inhibits the reactivation of EGFR and EGFR-mediated cell proliferation. BGB-283 inhibits the EGF-induced EGFR autophosphorylation on Tyr1068 in A431 cells in a dose-dependent manner.
In vivo, BGB-283 treatment leads to dose-dependent tumor growth inhibition accompanied by partial and complete tumor regressions in both cell-line derived and primary human colorectal tumor xenografts bearing B-RAFV600E mutation.
| Molecular Weight | 478.42 |
| Formula | C25H17F3N4O3 |
| CAS Number | 1446090-79-4 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Raf Products |
|---|
| Sorafenib-d3
Sorafenib-d3 (Donafenib) is a deuterium-labeled Sorafenib, it is the first deuterium-generation tumor suppressor small molecule. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively. |
| XL-281
XL-281 (BMS-908662) is an orally active inhibitor for RAF kinase, with IC50s of 2.6, 4.5 and 6 nM, for CRAF, B-RAF, and B-RAFV600E, respectively. |
| B-Raf IN 2
B-Raf IN 2 is a potent and selective BRAF inhibitor. |
| Brimarafenibum
Brimarafenibum (Brimarafenib) is a rapidly accelerated fibrosarcoma (Raf) kinase inhibitor, wtih antineoplastic effect. |
| Belvarafenib TFA
Belvarafenib TFA (HM95573 TFA) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively. |
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