产品名称

英文名称：Tozasertib

同义词

VX-680、MK-0457、Cyclopropane carboxylic acid{4-[4-(4-methyl-piperazin-1-yl)-6-(5-methyl-2H-pyrazol-3-ylamino)-pyrimidin-2-ylsulphanyl]-phenyl}-amide、Cyclopropanecarboxamide, N-[4-[[4-(4-methyl-1-piperazinyl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidiny、陶扎色替

产品性质

CAS编号：639089-54-6

分子式：C23H28N8OS

分子量：464.6

PubChem编号：5494449

别名：陶扎色替

英文别名：VX-680|MK-0457|Cyclopropane carboxylic acid{4-[4-(4-methyl-piperazin-1-yl)-6-(5-methyl-2H-pyrazol-3-ylamino)-pyrimidin-2-ylsulphanyl]-phenyl}-amide|Cyclopropanecarboxamide, N-[4-[[4-(4-methyl-1-piperazinyl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidiny

规格或纯度：≥98%

英文名称：Tozasertib

生化机理：Tozasertib is a potent pan-ARK inhibitor but favors ARK-1 (Ki = 0.6 nM) over ARK-2 (Ki = 18 nM) or ARK-3 (Ki = 4.6 nM). It shows selectivity against a panel of more than 190 different protein kinases. Tozasertib effectively inhibits proliferation of several different cell lines of clear cell renal carcinoma (IC50 < 10 μM), inhibiting H3 histone phosphorylation and increasing apoptosis. By depleting ARK activity, tozasertib disrupts bipolar spindle formation during mitosis, arresting cell cycle progression at the G2/M phase.Aurora kinase inhibitor (K i values are 0.6, 18 and 4.6 nM for Aurora kinase A, B and C, respectively). Exhibits selectivity for Aurora kinase over 190 other protein kinases.

储存温度：-20°C储存

运输条件：超低温冰袋运输

备注：如果有可能，您尽量在使用的当天配置溶液，并在当天使用完它。但是，如果您需要预先配制储备溶液，我们建议您将溶液等份保存在-20°C的密封小瓶中。通常，它们最多可以使用一个月。在使用前和打开样品瓶之前，我们建议您让您的产品在室温下平衡至少1小时。需要更多关于溶解度，用法和处理的建议吗？请访问我们的常见问题（FAQ）页面以获取更多详细信息。

产品介绍：VX-680 (Tozasertib, MK-0457)是一种pan-Aurora抑制剂，对Aurora A作用最强，Kiapp为0.6 nM，而对Aurora B/Aurora C的作用稍弱，对Aurora A选择性比其他55种激酶强高100倍。A potent and selective pan-ARK inhibitorVX-680 (Tozasertib, MK-0457) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinasesA potent and selective pan-ARK inhibitor;Aurora Kinase抑制剂

ALogP：3.4

IUPAC Name：N-[4-[4-(4-methylpiperazin-1-yl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]pyrimidin-2-yl]sulfanylphenyl]cyclopropanecarboxamide

INCHI：InChI=1S/C23H28N8OS/c1-15-13-20(29-28-15)25-19-14-21(31-11-9-30(2)10-12-31)27-23(26-19)33-18-7-5-17(6-8-18)24-22(32)16-3-4-16/h5-8,13-14,16H,3-4,9-12H2,1-2H3,(H,24,32)(H2,25,26,27,28,29)

InChi Key：GCIKSSRWRFVXBI-UHFFFAOYSA-N

Canonical SMILES：CC1=CC(=NN1)NC2=CC(=NC(=N2)SC3=CC=C(C=C3)NC(=O)C4CC4)N5CCN(CC5)C

Isomeric SMILES：CC1=CC(=NN1)NC2=CC(=NC(=N2)SC3=CC=C(C=C3)NC(=O)C4CC4)N5CCN(CC5)C

PubChem CID：5494449

CAS Registry No.：639089-54-6

Wikipedia：VX-680

DiscoveRx TREEspot：VX-680/MK-0457|

ChEMBL Ligand：CHEMBL572878

RCSB PDB Ligand：VX6

溶解性：Soluble in plain water (10-30 μM), DMSO (100 mg/ml), ethanol (<1 mg/ml) at 25 °C, and methanol.

产品包装