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Vemurafenib

Chemical Structure : Vemurafenib

CAS No.: 918504-65-1

Vemurafenib (PLX-4032;RG7204;RO5185426)

Catalog No.: PC-42871Not For Human Use, Lab Use Only.

Vemurafenib (PLX-4032, RG7204, RO5185426) is a potent, selective B-RAF V600E inhibitor with IC50 of 30 nM, displays similar potency for c-RAF-1 (IC50=48 nM), and has selectivity against many other kinases, including wild type B-RAF (IC50=100nM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Vemurafenib (PLX-4032, RG7204, RO5185426) is a potent, selective B-RAF V600E inhibitor with IC50 of 30 nM, displays similar potency for c-RAF-1 (IC50=48 nM), and has selectivity against many other kinases, including wild type B-RAF (IC50=100nM).
Vemurafenib (PLX-4032) potently inhibits proliferation of a panel of tumor cell lines, selectively blocks the RAF/MEK/ERK pathway in BRAF mutant cells.
Vemurafenib (PLX-4032) causes tumor regressions and improves animal survival in tumor xenograft models of BRAF(V600E)-expressing melanoma.

Physicochemical Properties

M.Wt 489.9221
Formula C23H18ClF2N3O3S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: 6.2 mg/mL

Chemical Name/SMILES

1-Propanesulfonamide, N-[3-[[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-

References

1. Bollag G, et al. Nature. 2010 Sep 30;467(7315):596-9.

2. Joseph EW, et al. Proc Natl Acad Sci U S A. 2010 Aug 17;107(33):14903-8.

3. Yang H, et al. Cancer Res. 2010 Jul 1;70(13):5518-27.

4. Søndergaard JN, et al. J Transl Med. 2010 Apr 20;8:39.

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