All AbMole products are for research use only, cannot be used for human consumption.
Dabrafenib (GSK2118436A) is a potent ATP-competitive inhibitor of B-Raf, B-Raf V600E and c-Raf with IC50 of 3.2 nM, 0.8 nM and 5.0 nM, respectively. Dabrafenib is selective for Raf kinase, with 400 fold selectivity towards B-Raf over 91% of the other kinases tested. 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. GSK2118436 treatment results in no detectable negative impact on existing systemic immunity or the de novo generation of tumor-specific T cells. Dabrafenib (GSK2118436A) is currently in phase III clinical trial in patients with melanoma.
Arch Pathol Lab Med. 2024 May 16.
Genetic Landscape and Its Prognostic Impact in Children With Langerhans Cell Histiocytosis
Dabrafenib purchased from AbMole
Int J Mol Sci. 2021 Nov 4;22(21):11951.
BRAF and MEK Inhibitors Affect Dendritic-Cell Maturation and T-Cell Stimulation
Dabrafenib purchased from AbMole
Int J Mol Sci. 2018 Jan 18;19(1) pii: E289.
BRAF and MEK Inhibitors Influence the Function of Reprogrammed T Cells: Consequences for Adoptive T-Cell Therapy
Dabrafenib purchased from AbMole
Cell Rep. 2016 Jun 28;16(1):263-77.
BRAF(V600E) Kinase Domain Duplication Identified in Therapy-Refractory Melanoma Patient-Derived Xenografts.
Dabrafenib purchased from AbMole
Journal of Cell Science. 2016 Jun 1;129(11):2261-72.
PAX5 interacts with RIP2 to promote NF-κB activation and drug-resistance in B-lymphoproliferative disorders.
Dabrafenib purchased from AbMole
EMBO Mol Med. 2015 Jun 23;1104-18.
Intra- and inter-tumor heterogeneity in a vemurafenib-resistant melanoma patient and derived xenografts.
Dabrafenib purchased from AbMole
Cell Rep. 2014 Nov 20;1375-86.
Parallel in vivo and in vitro melanoma RNAi dropout screens reveal synthetic lethality between hypoxia and DNA damage response inhibition.
Dabrafenib purchased from AbMole
Cell Experiment | |
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Cell lines | A375-GFP, 888Mel-MEK1T55delinsRT,SK-MEL-28 |
Preparation method | Dose–response curves were performed as follows: 3,000–6,000 cells were plated per well in a 96-well plate. For each condition, triplicates were plated. The next day, drug was added to the wells. At day 5 of the assay, medium-containing drug was removed and survival was measured by CellTiter-Blue Cell Viability Assay (G8081, Promega). |
Concentrations | 0, 0.25, 0.5, 1, 2.5, 5 µ M |
Incubation time | 5 Days |
Animal Experiment | |
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Animal models | A375 cells infected with pQXCIPGFP, MEK1WT, and MEK1T55delinsRT Mice--Derived Xenografts |
Formulation | Dabrafenib powder was first dissolved in DMSO and consequently, before injection, dissolved in 0.5% hydroxypropylmethylcellulose (Sigma-Aldrich), 0.2% Tween-80 in pH 8.0 distilled H2O. |
Dosages | 30 mg/kg daily (6 days per week) |
Administration | oral gavage |
Molecular Weight | 519.56 |
Formula | C23H20F3N5O2S2 |
CAS Number | 1195765-45-7 |
Solubility (25°C) | DMSO 30 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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NST-628
NST-628 is a brain-permeable MAPK pathway molecule glue that inhibits RAF phosphorylation and MEK activation. NST-628 also binds RAF and prevents the formation of BRAF-CRAF and BRAF-ARAF heterodimers, effectively inhibiting the RAS-MAPK pathway. |
Cyclorasin 9A5
Cyclorasin 9A5 is an 11-residue cell-permeable cyclic peptide that orthosterically inhibits the Ras-Raf protein interaction with an IC50 of 120 nM. |
R18
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PROTAC RAF degrader 1
PROTAC RAF degrader 1 is a PROTAC RAF degrader. |
B-Raf IN 15
B-Raf IN 15 is a BRAF inhibitor. |
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Products are for research use only. Not for human use. We do not sell to patients.
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