Bortezomib, Free Base (Velcade, MG-341, PS-341, [(1S)-3-methyl-1-[[(2R)-3-phenyl-2-(pyrazine-2-carbo

Bortezomib is the active ingredient in the drug sold under the trade name Velcade(R). This drug has been approved in at least one country to treat multiple myeloma. It is a potent (Ki, 0.6nM), specific and reversible proteasome inhibitor. There is not any significant inhibitory activity against other enzymes or receptors. In a study with the National Cancer Institute's panel of 60 human cell lines, Bortezomib showed a mean IC50 of 7nM as tested by SRB analysis., Bortezomib is active in preclinical models of human prostate cancer, while its effects on apoptosis versus angiogenesis are cell type dependent. Bortezomib caused comparable growth suppression in LNCaP-Pro5 and PC3M-Pro4 cells with an IC90 of 10nM. Bortezomib inhibits cell proliferation of H460 cells (Human non-small cell lung cancer cell lines) with an IC50 of 0.1uM. Appearance: Supplied as a white to off-white powder, Purity: HPLC: ~99%, TLC: ~99%, Solubility: Soluble in DMSO at 200mg/ml. Soluble in ethanol at 200mg/ml. Very poorly soluble in water. Maximum solubility in plain water is estimated to be about 5-10uM. Melting Point: As Reported , Storage and Stability: May be stored at RT for short-term only. Long-term storage is recommended at -20°C. Stable for 12 months. For maximum recovery of product, centrifuge the original vial prior to removing the cap.