Dabrafenib

Catalog No.S2807 Batch:S280708

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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
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
2%DMSO Corn oil

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 3.000mg/ml (5.77mM) Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clear DMSO stock solution to 980 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
Clear solution
2% DMSO 45% PEG300 2%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 3.000mg/ml (5.77mM) Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clarified DMSO stock solution to 450 μL PEG300, mix evenly to clarify it; add 20 μL Tween-80 to the above system, mix evenly to clarify it; Then continue to add 510 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <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

References

  • https://www.researchgate.net/publication/269940032_Abstract_B88_A_selective_Raf_kinase_inhibitor_induces_cell_death_and_tumor_regression_of_human_cancer_cell_lines_encoding_B-RafV600E_mutation
  • https://pubmed.ncbi.nlm.nih.gov/22389471/
  • https://pubmed.ncbi.nlm.nih.gov/24900673/
  • https://pubmed.ncbi.nlm.nih.gov/34296750/

Customer Product Validation

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

Data from [ 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 332 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
EGFR TKIs suppress MUC1 glycosylation through the PI3K/AKT/SP1/C1GALT1 pathway to enhance TnMUC1 CAR-T efficacy in EGFR-mutant NSCLC [ Cell Rep Med, 2025, S2666-3791(25)00272-1] PubMed: 40562040
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
Axl inhibitor-mediated reprogramming of the myeloid compartment of the in vitro tumor microenvironment is influenced by prior targeted therapy treatment [ Front Immunol, 2025, 16:1601420] PubMed: 40539073
Novel TEAD1 Inhibitor VT103 Enhances Dabrafenib Efficacy in BRAF V600E Mutated Lung Adenocarcinoma via Survivin Downregulation [ Cancer Sci, 2025, 10.1111/cas.70075] PubMed: 40202586
Bioluminescence-based assays for quantifying endogenous protein interactions in live cells [ J Biol Chem, 2025, 301(8):110454] PubMed: 40617353
A novel patient-derived cutaneous melanoma cell line reveals key features of metastatic melanoma [ Front Oncol, 2025, 15:1531013] PubMed: 40756116
Dihydrotanshinone I enhanced BRAF mutant melanoma treatment efficacy by inhibiting the STAT3/SOX2 signaling pathway [ Front Oncol, 2025, 15:1429018] PubMed: 39944829
Src/FN1 pathway activation drives tumor cell cluster formation and metastasis in lung cancer: A promising therapeutic target [ Sci Adv, 2025, 11(28):eadv7377] PubMed: 40632865

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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.