Dabrafenib (GSK2118436)

Catalog No.S2807 1 Product Citations

Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM, with 4- and 6-fold less potency against B-Raf(wt) and c-Raf, respectively.

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Dabrafenib (GSK2118436) Chemical Structure

Dabrafenib (GSK2118436) Chemical Structure
Molecular Weight: 519.56

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Dabrafenib (GSK2118436) is available in the following compound libraries:

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Product Information

  • Compare Raf Inhibitors
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  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description Dabrafenib (GSK2118436) is a mutant BRAFV600 specific inhibitor with IC50 of 0.8 nM, with 4- and 6-fold less potency against B-Raf(wt) and c-Raf, respectively.
Targets B-Raf (V600E) [1] B-Raf [1] C-Raf [1]
IC50 0.8 nM 3.2 nM 5.0 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]
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(Only for Reference)

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.
Body Surface Area (m2)
Km factor202012128653
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Sylvie Laquerre, et al. 2009, EORTC International Conference. Abst B88.

[2] Greger JG, et al. Mol Cancer Ther, 2012, 11(4), 909-920.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-09-01)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02224781 Not yet recruiting Recurrent Melanoma|Stage IIIA Melanoma|Stage IIIB Melanoma|Stage IIIC Melanoma|Stage IV Melanoma National Cancer Institute (NCI) November 2014 Phase 3
NCT02082665 Not yet recruiting Cancer GlaxoSmithKline October 2014 Phase 1
NCT02110355 Not yet recruiting Advanced Malignancy|Advanced Solid Tumors|Cancer|Oncology|Oncology Patients|Tumors|Melanoma Amgen|GlaxoSmithKline September 2014 Phase 1|Phase 2
NCT02124772 Not yet recruiting Cancer GlaxoSmithKline September 2014 Phase 1
NCT02200562 Not yet recruiting Stage III or IV Melanoma University of Utah August 2014 Phase 1|Phase 2

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Chemical Information

Download Dabrafenib (GSK2118436) SDF
Molecular Weight (MW) 519.56


CAS No. 1195765-45-7
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Solubility (25°C) * In vitro DMSO 30 mg/mL (57 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol, 8 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name N-(3-(5-(2-aminopyrimidin-4-yl)-2-tert-butylthiazol-4-yl)-2-fluorophenyl)-2,6-difluorobenzenesulfonamide

Research Area

Product Citations (1)

Tech Support & FAQs

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