Dabrafenib (GSK2118436)

Catalog No.S2807 Synonyms: GSK2118436A

For research use only.

Dabrafenib (GSK2118436, GSK2118436A) is a mutant BRAFV600 specific inhibitor with IC50 of 0.7 nM in cell-free assays, with 7- and 9-fold less potency against B-Raf(wt) and c-Raf, respectively.

Dabrafenib (GSK2118436) Chemical Structure

CAS No. 1195765-45-7

Selleck's Dabrafenib (GSK2118436) has been cited by 222 publications

Purity & Quality Control

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Biological Activity

Description Dabrafenib (GSK2118436, GSK2118436A) is a mutant BRAFV600 specific inhibitor with IC50 of 0.7 nM in cell-free assays, with 7- and 9-fold less potency against B-Raf(wt) and c-Raf, respectively.
Targets
B-Raf (V600E) [3]
(Cell-free assay)
B-Raf [3]
(Cell-free assay)
C-Raf [3]
(Cell-free assay)
0.7 nM 5.2 nM 6.3 nM
In vitro

Dabrafenib is selective for Raf kinase, with 400 fold selectivity towards B-Raf over 91% of the other kinases tested. Dabrafenib inhibits B-RafV600E kinase, leading to decreased ERK phosphorylation and inhibition of cell proliferationby an initial arrest in the G1 phase of the cell cycle in cancer cells that specifically encode the mutation for B-RafV600E. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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HepG2 MnXnT4lv[XOnIFHzd4F6 M2XkVGlvcGmkaYTpc44hd2ZiQj3SZYYhXjZyMFWgcZV1[W62IHnuJIh2dWGwIFjldGczKGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIFXST{BxcG:|cHjvdplt[XSrb36ge4l1cCCLQ{WwJI9nKDBwMEC0JO69VQ>? MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDlyME[3N{c,OjR7MEC2O|M9N2F-
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Assay
Methods Test Index PMID
Western blot β-catenin ; p-S6 / p-AKT308 / p-AKT473 ; pMEK / pERK / ERK 29167314 24735930 31158244
Growth inhibition assay IC50 24735930
In vivo Dabrafenib (orally administrated) inhibits the growth of B-RafV600E mutant melanoma (A375P) and colon cancer (Colo205) human tumor xenografts, growing subcutaneously in immuno-compromised mice. [1]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 30 mg/mL
(57.74 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+45% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.

5 mg/mL

Chemical Information

Molecular Weight 519.56
Formula

C23H20F3N5O2S2

CAS No. 1195765-45-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)(C)C1=NC(=C(S1)C2=NC(=NC=C2)N)C3=C(C(=CC=C3)NS(=O)(=O)C4=C(C=CC=C4F)F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04961619 Not yet recruiting Drug: dabrafenib|Drug: trametinib Melanoma Novartis Pharmaceuticals|Novartis February 1 2022 --
NCT04547946 Recruiting Drug: dabrafenib + trametinib Malignant Melanoma Novartis Pharmaceuticals|Novartis October 15 2021 --
NCT05171374 Recruiting Drug: Dabrafenib|Drug: Trametinib Melanoma Stage III|Melanoma Stage IV|Melanoma MelanomaPRO Russia|Novartis September 30 2021 --
NCT04775095 Recruiting -- Non Small Cell Lung Cancer|BRAF V600 Mutation Intergroupe Francophone de Cancerologie Thoracique|Novartis March 8 2021 --

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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