Dabrafenib (GSK2118436A)

Catalog No. A11381

Dabrafenib (GSK2118436A)是一种有效且选择性的B-RAF蛋白激酶抑制剂，具有V600E突变，目前正在临床试验中。

Product Citations

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

Technical details

Catalog Num	A11381
M. Wt	519.6
Formula	C23H20F3N5O2S2
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	1195765-45-7
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

Biological Activity

Dabrafenib (GSK2118436A)是一种有效且选择性的B-RAF蛋白激酶抑制剂，具有V600E突变，目前正在临床试验中。

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.