Dabrafenib

Catalog No.S2807 Batch:S280707

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Technical Data

Formula

C23H20F3N5O2S2
Molecular Weight 519.56 CAS No. 1195765-45-7
Solubility (25°C)* In vitro DMSO 100 mg/mL (192.47 mM)
Water Insoluble
Ethanol Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Dabrafenib is a mutant BRAFV600E 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]
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)

Cell Assay:

[2]
  • Cell lines

    A375PF11 cells

  • Concentrations

    > 10 uM

  • Incubation Time

    24 h

  • Method

    Cells were treated with different concentrations of drug for 24 h.
Animal Study:

[4]
  • Animal Models

    Male C57Bl/6J mice

  • Dosages

    3 mg/kg

  • Administration

    Osmotic pumps

Customer Product Validation

Data from [Data independently produced by J Clin Invest, 2014, 124(11), 5074-84]

Data from [Data independently produced by J Clin Invest, 2014, 24(3), 1406-17]

Data from [Cell Death Dis, 2014, 5, e1278]

Data from [Transl Res, 2014, 10.1016/j.trsl.2014.06.005]

Selleck's Dabrafenib has been cited by 322 publications

Pan-inhibition of super-enhancer-driven oncogenic transcription by next-generation synthetic ecteinascidins yields potent anti-cancer activity [ Nat Commun, 2025, 16(1):512] PubMed: 39779693
HDAC and MEK inhibition synergistically suppresses HOXC6 and enhances PD-1 blockade efficacy in BRAFV600E-mutant microsatellite stable colorectal cancer [ J Immunother Cancer, 2025, 13(1)e010460] PubMed: 39800382
Novel selective strategies targeting the BCL-2 family to enhance clinical efficacy in ALK-rearranged non-small cell lung cancer [ Cell Death Dis, 2025, 16(1):194] PubMed: 40113795
Dihydrotanshinone I enhanced BRAF mutant melanoma treatment efficacy by inhibiting the STAT3/SOX2 signaling pathway [ Front Oncol, 2025, 15:1429018] PubMed: 39944829
Assessing cancer therapeutic efficacy in vivo using [2H7]glucose deuterium metabolic imaging [ Sci Adv, 2025, 11(13):eadr0568] PubMed: 40138413
Let-7a microRNA modulates caspase-3-dependent apoptosis in melanoma cells treated with dabrafenib and trametinib combination [ Ir J Med Sci, 2025, none] PubMed: 40063190
Loss of tumor cell MHC Class II drives insensitivity of BRAF-mutant anaplastic thyroid cancers to MAPK inhibitors [ bioRxiv, 2025, 2025.01.27.635086] PubMed: 40093098
Antigenic cancer persister cells survive direct T cell attack [ bioRxiv, 2025, 2025.03.14.643359] PubMed: 40166148
Cancer cells impair monocyte-mediated T cell stimulation to evade immunity [ Nature, 2024, 10.1038/s41586-024-08257-4] PubMed: 39604727
Tumour-selective activity of RAS-GTP inhibition in pancreatic cancer [ Nature, 2024, 629(8013):927-936] PubMed: 38588697

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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