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PLX 4032
- RG 7204 - Vemurafenib - RO 5185426
- Soluble in DMSO
- MF: C23H18ClF2N3O3S
- MW: 489.92
Description
PLX 4032 (Vemurafenib) is a selective BRAF inhibitor targeting the oncogenic BRAF V600E mutant, with reported IC50 value of 44 nM.
BRAF V600E drives constitutive MAPK signaling in melanoma and other cancers. PLX 4032 is a benchmark tool for studying mutant-selective RAF inhibition, melanoma cell death, ERK pathway suppression and resistance mechanisms.
Key Features
- Selective inhibitor of BRAF V600E
- Reported IC50: 44 nM
- Suppresses mutant BRAF-driven MAPK signaling
- Benchmark compound for melanoma pharmacology research
Applications
- BRAF V600E kinase assays
- Melanoma cell model studies
- RAF/MEK/ERK pathway research
- Targeted therapy resistance models
More Information
| Parent CAS No. | 918504-65-1 |
|---|---|
| Chemical Name | N-(3-(5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl)propane-1-sulfonamide |
| SMILES | C(C1C(=CC=C(NS(=O)(=O)CCC)C=1F)F)(C1=CNC2=NC=C(C3C=CC(Cl)=CC=3)C=C12)=O |
| MFCD | N.A. |
| InChi | InChI=1S/C23H18ClF2N3O3S/c1-2-9-33(31,32)29-19-8-7-18(25)20(21(19)26)22(30)17-12-28-23-16(17)10-14(11-27-23)13-3-5-15(24)6-4-13/h3-8,10-12,29H,2,9H2,1H3,(H,27,28) |
| InChiKey | GPXBXXGIAQBQNI-UHFFFAOYSA-N |
| CID | 42611257 |
| Short Description | B-Raf inhibitor |
References
- G Bollag et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature 2010, 467, 596–599.
- PI Poulikakos et al. RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF. Nature 2010, 464, 427-430.
- E Sala et al. BRAF Silencing by Short Hairpin RNA or Chemical Blockade by PLX4032 Leads to Different Responses in Melanoma and Thyroid Carcinoma Cells. Mol. Cancer Res. 2008, 6(5), 751-759.
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