BGB-283
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MedKoo CAT#: 206465

CAS#: 1446090-77-2

Description: BGB-283, also known as Beigene-283 or Lifirafenib, 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.


Price and Availability

Size
Price

1g
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Size
Price

2g
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Size
Price

5g
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BGB-283 is not in stock, may be available through custom synthesis. For cost-effective reason, minimum 1 gram order is requested. The product will be characterized by NMR, HPLC and MS analysis. Purity (HPLC) is usually >98%. CoA, QC data, MSDS will be provided when product is successfully made. The estimated lead time is 2-3 months. Please send email to sales@medkoo.com to inquire quote.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 206465
Name: BGB-283
CAS#: 1446090-77-2
Chemical Formula: C25H17F3N4O3
Exact Mass: 478.12528
Molecular Weight: 478.43
Elemental Analysis: C, 62.76; H, 3.58; F, 11.91; N, 11.71; O, 10.03


Related CAS #: 1446090-77-2   1446090-79-4  

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

InChi Key: NGFFVZQXSRKHBM-FSSWDIPSSA-N

InChi Code: 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+/m1/s1

SMILES Code: [H][C@@]1(C2=CC(OC3=C(CCC4=O)C(N4)=NC=C3)=CC=C2O[C@]51[H])[C@@H]5C6=NC7=CC=C(C=C7N6)C(F)(F)F


Technical Data

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).

Harmonized System Code:
293490


References

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.