PLX-4032

5 mg

Cat. No.: 34-S51

$99.00

PLX-4032 (AKA Vemurafenib) is a highly selective inhibitor of BRAF kinase activity with an IC₅₀ of 44 nmol/L against V600E-mutant BRAF. BRAFV600E cancer-causing mutation occurs in most melanomas and about eight percent of all solid tumors. PLX-4032 has been shown to selectively inhibit the RAF/MEK/ERK pathway in BRAF mutant cells and induce regression of BRAF mutant xenographs. PLX4032 has also been shown to cause programmed cell death in melanoma cell lines and may be a potential anti-tumor agent.   

 

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TECHNICAL INFORMATION

Other Names: Vemurafenib, PLX4032, R7204, RG7204,  RO5185426

Chemical Formula:  C23H18ClF2N3O3S

CAS Number: 918504-65-1

Molecular Weight: 489.92

Purity:  >98%

Appearance:  a crystalline solid 

Solubility: DMSO

 

STORAGE AND HANDLING

Storage: Store at 4°C and protected from light. Following reconstitution, store aliquots at -20°C. 

Stability: Stock solutions stable at -20°C for up to 2 years.

Shipping Conditions: Shipped at room temperature.

 

PRODUCT USE

Soluble in DMSO at 100 mg/ml. If precipitate is observed,  vortex for 5 minutes. For most cells, the maximum tolerance to DMSO is less than 0.5%.

 

References

Bollag et al. (2010) Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature. 267(7315):596-9.

Smalley K. (2010) PLX-4032 | a small-molecule B-Raf inhibitor for the potential treatment of malignant melanoma. Curr Opin Investig Drugs. 11(6):699-706.

Flaherty et al. (2010) Inhibition of mutated | activated BRAF in metastatic melanoma. N Engl J Med. 363(9):809-19.

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