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
[H][C@]12OC3=CC=C(OC4=CC=NC5=C4CCC(=O)N5)C=C3[C@@]1([H])[C@@H]2C6=NC7=C(N6)C=C(C=C7)C(F)(F)F
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 |
|---|---|---|
| BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers. | 2015 Oct |
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| Targeting oncogenic Raf protein-serine/threonine kinases in human cancers. | 2018 Sep |
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| 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 Mar 20 |
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:57:20 UTC 2023
by
admin
on
Sat Dec 16 11:57:20 UTC 2023
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| Record UNII |
8762XZS5ZF
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| Record Status |
Validated (UNII)
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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 Sat Dec 16 11:57:20 UTC 2023 , Edited by admin on Sat Dec 16 11:57:20 UTC 2023
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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
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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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