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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

MK 0457

Cayman Chemical Item Number 13600

Tozasertib; VX 680 (CAS 639089-54-6)

MK 0457 (CAS 639089-54-6)

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Description

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 is linked to tumorigenesis.1 MK 0457 is a potent pan-Aurora kinase inhibitor but favors Aurora A (Ki = 0.6 nM) over Aurora B (Ki = 18 nM) or Aurora C (Ki = 4.6 nM).2 It shows selectivity against a panel of more than 190 different protein kinases.2 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.1 By depleting Aurora activity, MK 0457 disrupts bipolar spindle formation during mitosis, arresting cell cycle progression at the G2/M phase.1

1 Li, Y., Zhang, Z., Chen, J., et al. VX680/MK-0457, a potent and selective Aurora kinase inhibitor, targets both tumor and endothelial cells in clear cell renal cell carcinoma. Am J Transl Res 2(3) 296-308 (2010).

2 Pollard, J.R., and Mortimore, M. Discovery and development of Aurora kinase inhibitors as anticancer agents. J Med Chem 52(9) 2629-2651 (2009).

Synonyms
  • Tozasertib
  • VX 680
Formal Name N-​[4-​[[4-​(4-​methyl-​1-​piperazinyl)-​6-​[(5-​methyl-​1H-​pyrazol-​3-​yl)amino]-​2-​pyrimidinyl]thio]phenyl]-​cyclopropanecarboxamide
CAS Number 639089-54-6
Molecular Formula C23H28N8OS
Formula Weight 464.6
Formulation A crystalline solid
Purity ≥98%
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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CN1CCN(C2=CC(NC3=NNC(C)​=C3)​=NC(SC4=CC=C(NC(C5CC5)​=O)​C=C4)​=N2)​CC1
Size Price Quantity Subtotal
25 mg $54.00 $0.00
50 mg $103.00 $0.00
100 mg $194.00 $0.00
250 mg $432.00 $0.00
Bulk Contact
Cart Total $0.00

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Pricing updated 2012-02-11. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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