Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C25H17F3N4O3 |
| Molecular Weight | 478.4227 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
FC(F)(F)C1=CC2=C(C=C1)N=C(N2)[C@@H]3[C@H]4OC5=C(C=C(OC6=C7CCC(=O)NC7=NC=C6)C=C5)[C@@H]34
InChI
InChIKey=NGFFVZQXSRKHBM-FKBYEOEOSA-N
InChI=1S/C25H17F3N4O3/c26-25(27,28)11-1-4-15-16(9-11)31-24(30-15)21-20-14-10-12(2-5-17(14)35-22(20)21)34-18-7-8-29-23-13(18)3-6-19(33)32-23/h1-2,4-5,7-10,20-22H,3,6H2,(H,30,31)(H,29,32,33)/t20-,21-,22-/m0/s1
| Molecular Formula | C25H17F3N4O3 |
| Molecular Weight | 478.4227 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 3 / 3 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Lifirafenib (BGB-283 or BEIGENE-283), a dual inhibitor targeting BRAF kinase and EGFR, was studied for the treatment of different cancer types harboring mutations in BRAF, KRAS, and NRAS. Lifirafenib participates in Phase II clinical trial in combination with PD-0325901 to treat the patients with solid tumor.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| A high-performance liquid chromatography-tandem mass spectrometry method for the determination of lifrafenib, a novel RAF kinase and EGFR inhibitor, in human plasma and urine and its application in clinical pharmacokinetic study. | 2019-03-20 |
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| Targeting oncogenic Raf protein-serine/threonine kinases in human cancers. | 2018-09 |
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| BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers. | 2015-10 |
| Substance Class |
Chemical
Created
by
admin
on
Edited
Tue Apr 01 17:38:06 GMT 2025
by
admin
on
Tue Apr 01 17:38:06 GMT 2025
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| Record UNII |
8762XZS5ZF
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| Record Status |
Validated (UNII)
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| Code System | Code | Type | Description | ||
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C124995
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89670174
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DB14773
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8762XZS5ZF
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10554
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FG-149
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1446090-79-4
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300000034330
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BEIGENE-283
Created by
admin on Tue Apr 01 17:38:06 GMT 2025 , Edited by admin on Tue Apr 01 17:38:06 GMT 2025
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PRIMARY | MedKoo CAT NO.: 206465, CAS NO.: 1446090-77-2Description: BGB-283 is a Novel potent and selective RAF Kinase and EGFR inhibitor. BGB-283-displays Potent Antitumor Activity in B-RAF Mutated Colorectal Cancers. In vitro, BGB-283 potently inhibits B-RAFV600E-activated ERK phosphorylation and cell proliferation. It demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harbouring B-RAFV600E and EGFR mutation/amplification. In B-RAFV600E CRC cell lines, BGB-283 effectively inhibits the reactivation of EGFR and EGFR-mediated cell proliferation. 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. BGB-283 as a potent antitumor drug candidate with clinical potential for treating CRC harbouring B-RAFV600E mutation. (last updated: 5/17/2016). | ||
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CHEMBL3545246
Created by
admin on Tue Apr 01 17:38:06 GMT 2025 , Edited by admin on Tue Apr 01 17:38:06 GMT 2025
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TARGET -> INHIBITOR |
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SALT/SOLVATE -> PARENT |
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ACTIVE MOIETY |
Here, we report characterization of a dual RAF kinase/EGFR inhibitor, BGB-283, which is currently under clinical investigation. In vitro, BGB-283 potently inhibits BRAF(V600E)-activated ERK phosphorylation and cell proliferation. It demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harboring BRAF(V600E) and EGFR mutation/amplification. In BRAF(V600E) colorectal cancer cell lines, BGB-283 effectively inhibits the reactivation of EGFR and EGFR-mediated cell proliferation. 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 BRAF(V600E) mutation. These findings support BGB-283 as a potent antitumor drug candidate with clinical potential for treating colorectal cancer harboring BRAF(V600E) mutation.
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