All AbMole products are for research use only, cannot be used for human consumption.
Dabrafenib (GSK2118436) is a selective, orally bioavailable inhibitor of Mutant B-raf (BRAF) protein kinase with potential antineoplastic activity. B-raf belongs to the the raf/mil family of serine/threonine protein kinases and plays a role in regulating the MAP kinase/ERKs signaling pathway, which may be constitutively activated due to BRAF gene mutations. Mutations in BRAF are associated with increased growth and proliferation of cancer cells. Dabrafenib (GSK2118436) selectively binds to and inhibits the activity of B-raf, which may inhibit the proliferation of tumor cells which contain a mutated BRAF gene. Administration of the mutant BRAFi dabrafenib is associated with induction of keratinocytic proliferation, which in some cases develops features of low-grade malignancy.
2024 Jan.
MAPK pathway modulation and its implications in KRAS mutant lung adenocarcinoma
Dabrafenib Mesylate purchased from AbMole
Immunobiology. 2023 Jan;228(1):152311.
Characterization of the impact of immune checkpoint inhibitors on platelet activation and aggregation
Dabrafenib Mesylate purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | A375P, SKMEL28 and Colo205 cell lines |
| Preparation method | A375P-F11 assay: A375P cells were plated in 96-well plates by limiting dilution and single cell-derived clones were harvested and tested for sensitivity to B-Raf inhibitors. The F11 clone was selected for future studies and was named A375P-F11. Cellular pSmad Assay to Measure Anti-TGF-β Activity: Activity of compounds was tested in a mechanistic assay in HepG2 cells. Cells were seeded in 12-well plates at a density of 500,000 cells/well and allowed to adhere overnight at 37℃/5% CO2. Media (BME+10% serum) was removed and compound in serum free media was added to the cells for 45 minutes at 37oC/5% CO2. Cells were stimulated with 1 ng/ml TGF-β (R&D systems) for 60 minutes. Cells were lysed in buffer (25 mM Tris-HCl ph: 7.5, 2 mM EDTA, 2 mM EGTA,1% Triton X-100, 0.1 % SDS, 50 mM sodium-β-glycerophosphate, 2 mM sodium orthovanadate, 12.5 mM sodium pyrophosphate, protease and phosphatase inhibitor cocktails) for 30 minutes, scraped, collected, clarified by centrifugation and prepared for western blots in LDS/reducing reagent (Invitogen). Samples were resolved on 4-12% Bis-Tris gels, transferred to PVDF, and probed for total and phospho-Smad2 using antibodies from Cell Signaling. Gels were imaged using the odyssey blot scanner (Licor) and quantified using Licor software. Phospho:total Smad2 ratios were determined and the IC50 was defined as the concentration of compound which decreased the phospho:total ratio by 50%. |
| Concentrations | 0~10 nM |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | A375P F11 Melanoma Xenograft in nude mice |
| Formulation | 0.5% hydroxypropylmethylcellulose (Sigma) and 0.2% Tween-80 in distilled water pH 8.0 |
| Dosages | 0.2 mL/20g daily |
| Administration | oral gavage |
| Molecular Weight | 615.67 |
| Formula | C23H20F3N5O2S2.CH4O3S |
| CAS Number | 1195768-06-9 |
| Solubility (25°C) | DMSO 22 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Raf Products |
|---|
| Sorafenib-d3
Sorafenib-d3 (Donafenib) is a deuterium-labeled Sorafenib, it is the first deuterium-generation tumor suppressor small molecule. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively. |
| XL-281
XL-281 (BMS-908662) is an orally active inhibitor for RAF kinase, with IC50s of 2.6, 4.5 and 6 nM, for CRAF, B-RAF, and B-RAFV600E, respectively. |
| B-Raf IN 2
B-Raf IN 2 is a potent and selective BRAF inhibitor. |
| Brimarafenibum
Brimarafenibum (Brimarafenib) is a rapidly accelerated fibrosarcoma (Raf) kinase inhibitor, wtih antineoplastic effect. |
| Belvarafenib TFA
Belvarafenib TFA (HM95573 TFA) is a potent and pan RAF (Rapidly Accelerated Fibrosarcoma) inhibitor, with IC50s of 56 nM, 7 nM and 5 nM for B-RAF, B-RAFv600E and C-RAF respectively. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
