Lifirafenib HCl

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 206465

CAS#: 2025320-97-0 (HCl)

Description: Lifirafenib, also known as Beigene-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.

Chemical Structure

Lifirafenib HCl
CAS# 2025320-97-0 (HCl)

Theoretical Analysis

MedKoo Cat#: 206465
Name: Lifirafenib HCl
CAS#: 2025320-97-0 (HCl)
Chemical Formula: C26H19ClF3N3O3
Exact Mass: 478.12528
Molecular Weight: 513.9012
Elemental Analysis: C, 60.77; H, 3.73; Cl, 6.90; F, 11.09; N, 8.18; O, 9.34

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Related CAS #: 1446090-77-2 (free base)   1446090-79-4 (free base)   2025320-97-0 (HCl)   2025321-07-5 (mesylate)   2025321-56-4 (tosylate)    

Synonym: BGB-283; BGB 283; BGB283; Beigene-283; Beigene283; Beigene 283; Lifirafenib

IUPAC/Chemical Name: 5-(((1R,1aS,6bR)-1-(6-(trifluoromethyl)-1H-benzo[d]imidazol-2-yl)-1a,6b-dihydro-1H-cyclopropa[b]benzofuran-5-yl)oxy)-3,4-dihydro-1,8-naphthyridin-2(1H)-one hydrochloride


InChi Code: InChI=1S/C26H18F3N3O3.ClH/c27-26(28,29)13-2-1-12-9-18(31-17(12)10-13)23-22-16-11-14(3-5-19(16)35-24(22)23)34-20-7-8-30-25-15(20)4-6-21(33)32-25;/h1-3,5,7-11,22-24,31H,4,6H2,(H,30,32,33);1H/t22-,23-,24-;/m0./s1

SMILES Code: O=C1NC2=NC=CC(OC3=CC=C(O[C@@]4([H])[C@]5([H])[C@@H]4C6=CC7=CC=C(C(F)(F)F)C=C7N6)C5=C3)=C2CC1.[H]Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 513.9012 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Tang Z, Yuan X, Du R, Cheung SH, Zhang G, Wei J, Zhao Y, Feng Y, Peng H, Zhang
Y, Du Y, Hu X, Gong W, Liu Y, Gao Y, Liu Y, Hao R, Li S, Wang S, Ji JF, Zhang LH,
Li S, Sutton D, Wei M, Zhou C, Wang L, Luo L. BGB-283, a Novel RAF Kinase and
EGFR inhibitor, Displays Potent Antitumor Activity in B-RAF Mutated Colorectal
Cancers. Mol Cancer Ther. 2015 Jul 24. pii: molcanther.0262.2015. [Epub ahead of
print] PubMed PMID: 26208524.