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

Lifirafenib  (Synonyms: BGB-283)

Cat. No.: HY-18957 Purity: 98.73%
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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. : 1446090-79-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 189 In-stock
Solution
10 mM * 1 mL in DMSO USD 189 In-stock
Solid
5 mg USD 130 In-stock
10 mg USD 210 In-stock
50 mg USD 713 In-stock
100 mg USD 1109 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Lifirafenib:

Lifirafenib Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Lifirafenib

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

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BRaf c-Raf Raf

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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].

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

Lifirafenib Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

478.42

Formula

C25H17F3N4O3
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (209.02 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0902 mL 10.4511 mL 20.9021 mL 52.2553 mL
5 mM 0.4180 mL 2.0902 mL 4.1804 mL 10.4511 mL
10 mM 0.2090 mL 1.0451 mL 2.0902 mL 5.2255 mL
15 mM 0.1393 mL 0.6967 mL 1.3935 mL 3.4837 mL
20 mM 0.1045 mL 0.5226 mL 1.0451 mL 2.6128 mL
25 mM 0.0836 mL 0.4180 mL 0.8361 mL 2.0902 mL
30 mM 0.0697 mL 0.3484 mL 0.6967 mL 1.7418 mL
40 mM 0.0523 mL 0.2613 mL 0.5226 mL 1.3064 mL
50 mM 0.0418 mL 0.2090 mL 0.4180 mL 1.0451 mL
60 mM 0.0348 mL 0.1742 mL 0.3484 mL 0.8709 mL
80 mM 0.0261 mL 0.1306 mL 0.2613 mL 0.6532 mL
100 mM 0.0209 mL 0.1045 mL 0.2090 mL 0.5226 mL
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Lifirafenib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lifirafenib1446090-79-4BGB-283BGB283BGB 283EGFRRafEpidermal growth factor receptorErbB-1HER1Raf kinasesInhibitorinhibitorinhibit

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