1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
    MAPK/ERK Pathway
  2. EGFR
    Raf
  3. Lifirafenib

Lifirafenib (Synonyms: BGB-283)

Cat. No.: HY-18957 Purity: 98.02%
Handling Instructions

Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively.

For research use only. We do not sell to patients.

Lifirafenib Chemical Structure

Lifirafenib Chemical Structure

CAS No. : 1446090-77-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 172 In-stock
Estimated Time of Arrival: December 31
5 mg USD 156 In-stock
Estimated Time of Arrival: December 31
10 mg USD 216 In-stock
Estimated Time of Arrival: December 31
50 mg USD 648 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1008 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

Lifirafenib (BGB-283) is a novel and potent Raf Kinase and EGFR inhibitor with IC50 values of 23 and 29 nM for recombinant BRafV600E and EGFR, respectively.

IC50 & Target[1]

EGFR

29 nM (IC50)

BRafV600E

23 nM (IC50)

EGFRL858R/T790M

495 nM (IC50)

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[1].

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[1].

Clinical Trial
Molecular Weight

478.42

Formula

C₂₅H₁₇F₃N₄O₃

CAS No.

1446090-77-2

SMILES

FC(F)(F)C(C=C1)=CC2=C1N=C(N2)[[email protected]@H]3[[email protected]]([[email protected]@H]43)OC(C4=C5)=CC=C5OC6=CC=NC(N7)=C6CCC7=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (209.02 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0902 mL 10.4511 mL 20.9021 mL
5 mM 0.4180 mL 2.0902 mL 4.1804 mL
10 mM 0.2090 mL 1.0451 mL 2.0902 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.23 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.23 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

Melanoma, colon, breast, and lung cancer cells are left to attach for 16 hours and then treated with a 10-point dilution series in duplicate. CellTiter-Glo reagent is added in each well. Mixture is mixed on an orbital shaker for 2 minutes to allow cell lysing, followed by 10 minutes incubation at room temperature to allow development and stabilization of luminescent signal. Luminescent signal is measured using PHERAstar FS reader. EC50 values for cell viability are determined[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: When the average tumor size reaches 110 to 200 mm3, mice are randomized to treatment groups and treated twice per day or once daily by oral gavage (p.o.) with vehicle alone or 2.5 to 30 mg/kg of BGB-283. As control, mice are treated with erlotinib (100 mg/kg qd) or cetuximab (40 mg/kg twice weekly). Lifirafenib (BGB-283) and erlotinib are formulated at the desired concentration as a homogenous suspension in 0.5% (w/v) methylcellulose in purified water. Cetuximab is formulated by diluting the injection solution with saline before dosing[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Keywords:

LifirafenibBGB-283BGB283BGB 283EGFRRafEpidermal growth factor receptorErbB-1HER1Raf kinasesInhibitorinhibitorinhibit

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Product name:
Lifirafenib
Cat. No.:
HY-18957
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