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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Aurora Kinase-Tozasertib
Tozasertib

Chemical Structure : Tozasertib

CAS No.: 639089-54-6

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

货号: 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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100 mg ¥1980 In stock
250 mg ¥3280 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 464.5864
分子式 C23H28N8OS
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
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]-

参考文献

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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