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Lifirafenib (BGB-283)

Cat. No. M10475
Lifirafenib (BGB-283) Structure
Synonym:

Beigene-283

Size Price Availability
10mg USD 230  USD230 4-7 Days
25mg USD 500  USD500 4-7 Days
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
  • Current batch:
  • Purity >98.5%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 478.42
Formula C25H17F3N4O3
CAS Number 1446090-79-4
Purity >98.5%
Solubility DMSO 90 mg/mL
Storage at -20°C
References

[1] Xi Yuan, et al. Mol Oncol. RAF dimer inhibition enhances the antitumor activity of MEK inhibitors in K-RAS mutant tumors

[2] Xueting Yao, et al. J Pharm Biomed Anal. 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

[3] Hiroshi Kotani, et al. Oncogene. Distinct dependencies on receptor tyrosine kinases in the regulation of MAPK signaling between BRAF V600E and non-V600E mutant lung cancers

[4] Zhiyu Tang, et al. Mol Cancer Ther. BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers

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  Catalog
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