MAPK Raf Dabrafenib


Catalog No. T1903   CAS 1195765-45-7
Synonyms: GSK2118436, GSK2118436A

Dabrafenib is a selective inhibitor of mutated forms of BRAF kinase (IC50s: 0.7/5 nM for B-Raf (V600E)/C-Raf).

Dabrafenib, CAS 1195765-45-7
Pack Size Availability Price/USD Quantity
5 mg In stock 50.00
10 mg In stock 68.00
25 mg In stock 80.00
50 mg In stock 95.00
100 mg In stock 131.00
200 mg In stock 176.00
1 mL * 10 mM (in DMSO) In stock 56.00
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Purity 100.00%
Purity 98.00%
Purity 98.00%
Biological Description
Chemical Properties
Storage & Solubility Information
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Description Dabrafenib is a selective inhibitor of mutated forms of BRAF kinase (IC50s: 0.7/5 nM for B-Raf (V600E)/C-Raf).
Targets&IC50 B-Raf ,   B-Raf (V600E) ,   C-Raf
In vivo GSK2118436 dramatically reduced tumor growth in mice bearing B-RafV600E human melanoma tumors. In this model, CD1 nu/nu mice bearing A375P F11 (B-RafV600E) tumors were dosed orally with GSK2118436 at doses of 0.1, 1, 10, and 100 mg/kg once daily for 14 days. Dose-proportional reductions in tumor growth were observed. In the 100 mg/kg group, complete tumor regression was observed in 50% of treated animals [1]. The vaginal opening (VO) occurred earlier in Dabrafenib (DAB) females than in controls; however, the timing of the first estrus was unaffected. DAB-treated females evaluated just before VO had mostly immature reproductive tracts with no evidence of ovulation, similar to age-matched controls; however, DAB-treated females had keratinized and histologically open vaginas [4].
Cell Research
For longer term proliferation assays, cells are plated and treated with compound or combination of compounds in RMPI-1640 containing 10% FBS for 12 days. Compound treatments are replaced at least once during the assay. After 12 days, cells are stained with 0.5% methylene blue in 50% ethanol. Images are captured using flatbed scanner.
Synonyms GSK2118436 , GSK2118436A
Purity 100.00%
Molecular Weight 519.56
Formula C23H20F3N5O2S2
CAS No. 1195765-45-7


0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

DMSO: 28 mg/mL (53.9 mM)

Ethanol: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

30% PEG400+0.5% Tween80+5% propylene glycol: 8 mg/mL


References and Literature
1. Rheault TR, et al. Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors. ACS Med Chem Lett. 2013 Feb 7;4(3):358-62. 2. Jung B, et al. Anti-septic effects of dabrafenib on HMGB1-mediated inflammatory responses. BMB Rep. 2016 Apr;49(4):214-9. 3. Greger JG, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther, 2012, 11(4), 909-920. 4. Posobiec LM, et al. Early Vaginal Opening in Juvenile Female Rats Given BRAF-Inhibitor Dabrafenib Is Not Associated with Early Physiologic Sexual Maturation. Birth Defects Res B Dev Reprod Toxicol. 2015 Dec;104(6):244-52.

Related compound libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Clinical Compound Library Stem cell Differentiation Compound Library Apoptosis Compound Library Autophagy Compound Library MAPK Inhibitor Library Tyrosine kinase inhibitor library FDA-approved Drug Library Kinase Inhibitor Library Anti-cancer Approved drug Library Anti-cancer Clinical Compound Library Fluorochemical Library Anti-cancer Metabolism Compound Library Anti-obesity Compound Library Anti-cancer Active Compound library Anti-cancer Drug library Drug Repurposing Library Target-Focused Phenotypic Screening Library Small Molecule Immuno-Oncology Compound Library HIF-1 Signaling Pathway Compound Library Anti-COVID-19 Compound Library Anti-Lung Cancer Compound Library Drug-induced Liver Injury (DILI) Compound Library FDA Approved & Pharmacopeial Drug Library Anti-Pancreatic Cancer Compound Library Glutamine Metabolism Compound Library

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