Dabrafenib

Catalog No.S2807 Batch:S280709

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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, 24(3), 1406-17]

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

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 285 publications

MET receptor serves as a promising target in melanoma brain metastases [ Acta Neuropathol, 2024, 147(1):44] PubMed: 38386085
Dual targeting of MAPK and PI3K pathways unlocks redifferentiation of Braf-mutated thyroid cancer organoids [ Oncogene, 2024, 43(3):155-170] PubMed: 37985676
Antagonism of regulatory ISGs enhances the anti-melanoma efficacy of STING agonists [ Front Immunol, 2024, 15:1334769] PubMed: 38312842
H3K4me3 remodeling induced acquired resistance through O-GlcNAc transferase [ Drug Resist Updat, 2023, 71:100993] PubMed: 37639774
A reversible SRC-relayed COX2 inflammatory program drives resistance to BRAF and EGFR inhibition in BRAFV600E colorectal tumors [ Nat Cancer, 2023, 4(2):240-256] PubMed: 36759733
Interleukin 17 signaling supports clinical benefit of dual CTLA-4 and PD-1 checkpoint inhibition in melanoma [ Nat Cancer, 2023, 4(9):1292-1308] PubMed: 37525015
Signaling-induced systematic repression of miRNAs uncovers cancer vulnerabilities and targeted therapy sensitivity [ Cell Rep Med, 2023, S2666-3791(23)00367-1] PubMed: 37734378
Signaling-induced systematic repression of miRNAs uncovers cancer vulnerabilities and targeted therapy sensitivity [ Cell Rep Med, 2023, 4(10):101200] PubMed: 37734378
MiR126-targeted-nanoparticles combined with PI3K/AKT inhibitor as a new strategy to overcome melanoma resistance [ Mol Ther, 2023, 10.1016/j.ymthe.2023.11.021] PubMed: 37990493
An in vivo avian model of human melanoma to perform rapid and robust preclinical studies [ EMBO Mol Med, 2023, 15(3):e16629] PubMed: 36692026

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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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