Vemurafenib (PLX4032, RG7204) , ≥98% , 918504-65-1

CAS NO.：918504-65-1

Empirical Formula: C23H18ClF2N3O3S

Molecular Weight: 489.92

MDL number: MFCD18074504

PRODUCT Properties

• Density: 1.46
• storage temp.: -20°C
• solubility: Soluble in DMSO (up to 100 mg/ml)
• form: White powder.
• pka: 6.26±0.10(Predicted)
• color: White or off-white
• Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Description and Uses

In August 2011, the United States FDA approved vemurafenib (PLX- 4032, RO-5185426) for the treatment of patients with metastatic melanoma with the BRAFV600E mutation. Vemurafenib has been developed as a targeted therapy for patients with the BRAF gene mutation since oncogenic B-raf signaling is implicated in approximately 50% of melanomas. Vemurafenib was identified based on an initial high-throughput screen followed by the extensive use of structure-based drug design. Vemurafenib is a potent inhibitor of B-RafV600E kinase (IC₅₀=13 nM) compared to its potency against wildtype B-raf (IC₅₀=160 nM) and is fairly selective versus a panel of 200 kinases. It does inhibit other kinases (RAF1, SRMS, ACK1, MAP4K5, and FGR) and mutant B-raf kinases (BRAFV600K, BRAFV600D, and BRAFV600R) with enzyme IC_50's of <100 nM.

PLX4032 is an orally bioavailable, ATP-competitive inhibitor of mutant V600E and wild type B-Raf kinases (IC50s = 31 and 100 nM, respectively). It inhibits cell proliferation in a variety of cell lines expressing B-Raf V600E and synergizes strongly with taxol, vinblastine, and oxaliplatin in inhibiting the proliferation of B-RafV600E transformed cancer cells. PLX4032 is effective against the growth of tumors bearing the B-Raf V600E mutation.[Cayman Chemical]

Safety

• Symbol(GHS): GHS09
• Signal word: Warning
• Hazard statements: H410
• Precautionary statements: P273-P391-P501
• HS Code: 29339900