Tozasertib , ≥98% , 639089-54-6

Synonym(s):
;N-[4-[[4-(4-Methyl-1-piperazinyl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]thio]phenyl]cyclopropanecarboxamide;Tozasertib

CAS NO.：639089-54-6

Empirical Formula: C23H28N8OS

Molecular Weight: 464.59

MDL number: MFCD13185152

PRODUCT Properties

• Melting point: 248-253°C (dec.)
• Density: 1.40±0.1 g/cm3(Predicted)
• storage temp.: 2-8°C
• solubility: Soluble in DMSO (up to 100 mg/ml).
• pka: 14.09±0.70(Predicted)
• form: powder
• color: white to beige
• Stability: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

Description and Uses

The Aurora kinases (A, B, and C) are a family of serine-threonine kinases that regulate various stages of mitotic function. With significant roles in cell cycle and cell division, Aurora kinase gene amplification and overexpression are linked to tumorigenesis. MK-0457 is a potent pan-Aurora kinase inhibitor but favors Aurora A (K_i = 0.6 nM) over Aurora B (K_i = 18 nM) or Aurora C (K_i = 4.6 nM). It shows selectivity against a panel of more than 190 different protein kinases. MK-0457 effectively inhibits proliferation of several different cell lines of clear cell renal carcinoma (IC₅₀s = <10 μM) and blocks the growth of tumors in a rodent model of cancer (80 mg/kg), inhibiting histone H3 phosphorylation and increasing apoptosis. By depleting Aurora activity, MK-0457 disrupts bipolar spindle formation during mitosis, arresting cell cycle progression at the G₂/M phase.

Tozasertib is used as a multikinase inhibitor once used for cancer treatment.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302
• Precautionary statements: P280-P305+P351+P338