Tozasertib, Free Base (N-[4-[[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanyl]phenyl]cyclopropanecarboxamide, VX-680, MK-0457, VX6)

Blue Ice

464, 59

Supplied as a white to off-white powder.

Tozasertib is a potent inhibitor of all aurora kinases, including the A, B and C isotypes (Ki=0.6nM, 18nM and 4.6nM, respectively). It also inhibits ABL kinase (Ki=30nM), an imatinib-resistant ABL mutant (T315I) kinase (Ki=42nM), and Flt-3 (Ki=30nM). Tozasertib binds to an inactive aurora conformation.

Solubility:
Soluble in DMSO at 100mg/ml; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-30uM; buffers, serum, or other additives may increase or decrease the aqueous solubility.

Storage and Stability:
May be stored at RT for short-term only. Long-term storage is recommended at -20°C. For maximum recovery of product, centrifuge the original vial prior to removing the cap.