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
Patent. CN113684276A 2021 Nov 23.
Patent. CN113684276A
Dabrafenib Mesylate purchased from AbMole
Patent. CN113249468A 2021 Aug 13.
Patent. CN113249468A
Dabrafenib Mesylate purchased from AbMole
Patent. CN113249482B 2021 Nov 12.
Patent. CN113249482B
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 |
|---|
| GDC-0879
GDC-0879 is a potent and selective B-Raf kinase inhibitor with an EC50 of 0.75 µM. |
| Vemurafenib (PLX4032)
Vemurafenib (PLX4032) is a first-in-class, potent, selective inhibitor of B-Raf that inhibits RAFV600E and C-RAF-1 activity with IC50s of 31 nM and 48 nM, respectively.In addition, Vemurafenib induces autophagy. |
| PLX-4720
PLX-4720 is a selective BRAFV600E inhibitor with the IC50 values of 160 nM and 130 nM for B-Raf and BRK respectively. |
| SB590885
SB590885 is a selective small-molecule inhibitor of the B-Raf kinase and Ki values are 0.16 and 1.72 nM for B-Raf and c-Raf respectively. |
| ZM 336372
ZM 336372 is a potent, selective ATP-competitive inhibitor of c-Raf in vitro (IC50 = 70 nM for inhibition of human c-Raf). |
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