MedKoo Cat#: 206465 | Name: Lifirafenib HCl

Description:

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

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
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: 478.1253

Molecular Weight: 513.90

Elemental Analysis: C, 60.77; H, 3.73; Cl, 6.90; F, 11.09; N, 8.18; O, 9.34

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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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) 1854985-74-2 (maleate)
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 Key
VIZZONBMKQWTRV-NYTZCTPBSA-N
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
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 513.90 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
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.