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)
Clear solution
2%DMSO Corn oil
3.0mg/ml 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
3.0mg/ml 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

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 307 publications

Tumour-selective activity of RAS-GTP inhibition in pancreatic cancer [ Nature, 2024, 629(8013):927-936] PubMed: 38588697
Identification of hypoxic macrophages in glioblastoma with therapeutic potential for vasculature normalization [ Cancer Cell, 2024, S1535-6108(24)00119-3] PubMed: 38640932
Base editing screens define the genetic landscape of cancer drug resistance mechanisms [ Nat Genet, 2024, 10.1038/s41588-024-01948-8] PubMed: 39424923
MET receptor serves as a promising target in melanoma brain metastases [ Acta Neuropathol, 2024, 147(1):44] PubMed: 38386085
Anaplastic thyroid cancer spheroids as preclinical models to test therapeutics [ J Exp Clin Cancer Res, 2024, 43(1):85] PubMed: 38500204
Single-cell RNA sequencing reveals melanoma cell state-dependent heterogeneity of response to MAPK inhibitors [ EBioMedicine, 2024, 107:105308] PubMed: 39216232
Ubiquitin-specific protease 22 controls melanoma metastasis and vulnerability to ferroptosis through targeting SIRT1/PTEN/PI3K signaling [ MedComm (2020), 2024, 5(8):e684] PubMed: 39135915
Combined therapy of dabrafenib and an anti-HER2 antibody-drug conjugate for advanced BRAF-mutant melanoma [ Cell Mol Biol Lett, 2024, 29(1):50] PubMed: 38594618
GLI1 confers resistance to PARP inhibitors by activating the DNA damage repair pathway [ Oncogene, 2024, 10.1038/s41388-024-03105-1] PubMed: 39095584
Dual targeting of MAPK and PI3K pathways unlocks redifferentiation of Braf-mutated thyroid cancer organoids [ Oncogene, 2024, 43(3):155-170] PubMed: 37985676

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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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