Tivantinib, 10 mg

From STEMCELL Technologies, this small molecule is a staurosporine derivative that binds to the inactive, dephosphorylated c-MET receptor tyrosine kinase in a manner not competitive with ATP, and is selective for c-MET (Ki ≅ 355 nM) in a screen of 230 kinases. The compound is also reported to display cytotoxic activity distinct from its inhibition of c-MET and to bind directly to the colchicine binding pocket of tubulin, reducing tubulin polymerization.

Synonyms for the compound include ARQ 197 and (3R,4R)-3-(5,6-dihydro-4H-pyrrolo[3,2,1-ij]quinolin-1-yl)-4-(1H-indol-3-yl)-2,5-pyrrolidinedione. It has a molecular formula of C₂₃H₁₉N₃O₂, a molecular weight of 369.4 g/mol, and a reported purity of ≥ 98%. It is supplied as a crystalline solid (CAS 905854-02-6) with reported solubility of ~0.1 mg/mL in a 1:5 solution of DMSO:PBS (pH 7.2), ~5 mg/mL in ethanol, and ~20 mg/mL in DMSO and DMF.

STEMCELL Technologies recommends storing the product at ≤20°C, protected from prolonged exposure to light, where it is stable as supplied for 12 months from the date of receipt. The compound has low solubility in aqueous media. Suitable solvents include DMSO (≤ 50 mM) and absolute ethanol (≤ 13 mM), and stock solutions should be freshly prepared and stored at ≤20°C. Aliquoting is advised to limit repeated freeze-thaw cycles, and final DMSO concentration in cell culture should remain below 0.1% to avoid potential cell toxicity. The safety data sheet states the substance is not classified as hazardous under GHS, though it may be harmful if inhaled, swallowed, or absorbed through skin, and may cause irritation of skin, eyes, and respiratory tract. The product is supplied for laboratory research use.