Chemical Structure : Tozasertib
CAS No.: 639089-54-6
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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50 mg | $128 | In stock | |
100 mg | $198 | In stock | |
250 mg | $328 | In stock | |
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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.
M.Wt | 464.5864 | |
Formula | C23H28N8OS | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
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Chemical Name/SMILES |
Cyclopropanecarboxamide, N-[4-[[4-(4-methyl-1-piperazinyl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]thio]phenyl]- |
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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