Dabrafenib (GSK2118436A)

Name: Dabrafenib (GSK2118436A)
Brand: Adooq Bioscience
SKU: A11381
Rating: 100 (6 reviews)

Catalog No.: A11381

Raf inhibitor

Product Citations (6)

Dabrafenib (GSK2118436A) Chemical Structure

CAS NO. 1195765-45-7

Dabrafenib is a potent and selective inhibitor of B-RAF protein kinase carrying V600E mutation, currently in clinical trial.

Availability: In stock

Package	Price	Qty
5 mg	$50.00
25 mg	$70.00
50 mg	$90.00
100 mg	$125.00
10mM * 1mL in DMSO	$50.00
Custom Size	Get quote

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Products are for laboratory research use only. Not for human use. We do not sell to patients.

Adooq Products cited in reputable paper

Publications Citing Use of Adooq Dabrafenib (GSK2118436A)

Yuki Shimizu, .et al. Acquired resistance to BRAF inhibitors is mediated by BRAF splicing variants in BRAF V600E mutation-positive colorectal neuroendocrine carcinoma, Cancer Lett, 2022, Sep 1;543 PMID: 35724767
Aya Hasan Alshammari, .et al. Discrimination of hand-foot skin reaction caused by tyrosine kinase inhibitors based on direct keratinocyte toxicity and vascular endothelial growth factor receptor-2 inhibition, Biochem Pharmacol, 2022, Mar;197:114914 PMID: 35041812
Chenyang He, .et al. Detection of Dabrafenib using Optical Fibre Long Period Grating Sensor Modified with Surface Imprinted Polymers for Dose Detection and Prevention of Cancer Resistance, Clinical and Translational Biophotonics, 2020, TTh3B.2
Hirosumi Tamura, .et al. Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues, Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
Brittany M. Duggan, .et al. Tyrosine kinase inhibitors of Ripk2 attenuate bacterial cell wall-mediated lipolysis, inflammation and dysglycemia, Sci Rep, 2017, 7: 1578 PMID: 28484277
Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358

Biological Activity

Dabrafenib is a potent and selective inhibitor of B-RAF protein kinase carrying V600E mutation, currently in clinical trial.

Targets

B-Raf (V600E) (Cell-free assay)	B-Raf (Cell-free assay)	C-Raf (Cell-free assay)
0.8 nM	3.2 nM	5.0 nM

Solubility *

In vitro (25°C)	DMSO	28 mg/mL (53.89 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	2% DMSO+45% PEG 300+2% Tween 80+ddH2O	4 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq 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.

Preparing Stock Solutions

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
0.1 mM	19.25 mL	96.23 mL	192.46 mL
0.5 mM	3.85 mL	19.25 mL	38.49 mL
1 mM	1.92 mL	9.62 mL	19.25 mL
5 mM	0.38 mL	1.92 mL	3.85 mL

*The above data is based on the productmolecular weight 519.6 . Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Chemical Properties

Catalog Num	A11381
Actions	Inhibitor
CAS No.	1195765-45-7
Formula	C23H20F3N5O2S2
M. Wt	519.6
Purity	>98%
Synonyms	GSK2118436A
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
Storage	Store lyophilized at -20ºC, keep desiccated. In lyophilized form, the chemical is stable for 36 months. In solution, store at -20ºC and use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.