BGB-283 free base · Synonyms: BGB 283 · BGB283

Lifirafenib is a novel and potent Raf Kinase and EGFR inhibitor.

For research use only. Not for human or veterinary use.

Target EGFR Raf

Research area Cancer

Purity >98% Stock Inquire

Data Sheet SDS COA

BGB-283 structure

CAS No.: 1446090-79-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
50 mg	USD 490.00	BP-02435-50mg	In stock	Get quote
100 mg	USD 780.00	BP-02435-100mg	In stock	Get quote
250 mg	USD 1,570.00	BP-02435-250mg	In stock	Get quote
500 mg	USD 2,500.00	BP-02435-500mg	In stock	Get quote
1 g	USD 4,014.00	BP-02435-1g	In stock	Get quote
2 g	Inquire	BP-02435-2g	In stock	Inquire

Need another size or custom synthesis? Request a quote.

Description

Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRaf V600E and EGFR, respectively.

Biological activity

In Vitro Lifirafenib (BGB-283) potently inhibits BRafV600E-activated ERK phosphorylation and cell proliferation. It demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harboring BRafV600E and EGFR mutation/amplification. In BRafV600E colorectal cancer cell lines, Lifirafenib (BGB-283) effectively inhibits the reactivation of EGFR and EGFR-mediated cell proliferation. In Vivo Lifirafenib (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 BRafV600E mutation.

Identifiers

SMILES: O=C1NC2=NC=CC(OC3=CC=C(O[C@@]4([H])[C@]5([H])[C@@H]4C6=NC7=CC=C(C(F)(F)F)C=C7N6)C5=C3)=C2CC1
InChIKey: NGFFVZQXSRKHBM-FKBYEOEOSA-N

Specifications

MW (average): 478.4227
Formula: C₂₅H₁₇F₃N₄O₃
CAS No.: 1446090-79-4
Physical state: Solid
Color: White to off-white
Shipping: 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: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month

Solubility

Soluble in DMSO : ≥ 100 mg/mL

Documents

References

[1].Tang Z, et al. BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers. Mol Cancer Ther. 2015 Oct;14(10):2187-97.

Same target

Search EGFR

Same research area

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