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Tozasertib

Chemical Structure : Tozasertib

CAS No.: 639089-54-6

Tozasertib (MK-0457;VX-680;MK0457;VX680;VX 680;MK 0457)

Catalog No.: PC-42409Not For Human Use, Lab Use Only.

Tozasertib (MK-0457, VX-680) is a highly potent, selective and reversible Aurora kinase inhibitor with Ki of 0.6, 18 and 4.6 nM for Aurora A, B and C, respectively.

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Biological Activity

Tozasertib (MK-0457, VX-680) is a highly potent, selective and reversible Aurora kinase inhibitor with Ki of 0.6, 18 and 4.6 nM for Aurora A, B and C, respectively.
Tozasertib (MK-0457, VX-680) also inhibits the imatinib-resistant ABL(T315I) kinase with Kd of 5 nM, displays >100-fold selectivity for the Aurora-A kinase over 55 other kinases with the only exception FLT-3 (Ki=30 nM).
Tozasertib (MK-0457, VX-680) blocks cell-cycle progression and induces apoptosis in a diverse range of human tumor types.
Tozasertib (MK-0457, VX-680) causes profound inhibition of tumor growth in a variety of in vivo xenograft models.

Physicochemical Properties

M.Wt 464.5864
Formula C23H28N8OS
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Cyclopropanecarboxamide, N-[4-[[4-(4-methyl-1-piperazinyl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]thio]phenyl]-

References

1. Harrington EA, et al. Nat Med. 2004 Mar;10(3):262-7.

2. Young MA, et al. Cancer Res. 2006 Jan 15;66(2):1007-14.

3. Carter TA, et al. Proc Natl Acad Sci U S A. 2005 Aug 2;102(31):11011-6.

4. Giles FJ, et al. Blood. 2007 Jan 15;109(2):500-2.

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