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Formula | C23H20F3N5O2S2 |
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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) |
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* <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.) |
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. | ||||||
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Targets |
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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] |
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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] |
Cell Assay: |
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Animal Study: |
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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]
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.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.