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基本描述
| 规格或纯度 | ≥98% |
|---|---|
| 英文名称 | Tozasertib |
| 别名 | VX-680;MK-0457;陶扎色替 |
| 英文别名 | VX680; MK-0457;VX-680;Tozasertib;N-[4-[[4-(4-Methyl-1-piperazinyl)-6-[(5-methyl-1H-pyrazol-3-yl)amino]-2-pyrimidinyl]thio]phenyl]cyclopropanecarboxamide; MK 0457; VX 680;VX-680;MK-0457 |
| 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 inhibitor VX-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 kinases |
名称和标识符
| 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 |
| 分子式 |
C23H28N8OS |
| PubChem CID | 5494449 |
| 分子量 | 464.6 |
数据库链接
| CAS Registry No. | 639089-54-6 |
|---|---|
| Wikipedia | VX-680 |
| DiscoveRx TREEspot | VX-680/MK-0457| |
| PubChem CID | 5494449 |
| ChEMBL Ligand | CHEMBL572878 |
| RCSB PDB Ligand | VX6 |
化学和物理性质
| 溶解性 | Soluble in plain water (10-30 μM), DMSO (100 mg/ml), ethanol (<1 mg/ml) at 25 °C, and methanol. |
|---|
靶标
| Target ID | 1936 | ||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 名称 | aurora kinase A | ||||||||||||||||||||||||
| 缩写名 | AurA | ||||||||||||||||||||||||
| 家族 | Aurora kinase (Aur) family | ||||||||||||||||||||||||
| 别名 | KIAA0786 | ||||||||||||||||||||||||
| 基因和蛋白信息 |
|
||||||||||||||||||||||||
| Ensembl Gene | ENSG00000087586 (Hs) , ENSMUSG00000027496 (Mm) , ENSRNOG00000004479 (Rn) | ||||||||||||||||||||||||
| Entrez Gene | 6790 (Hs) , 20878 (Mm) , 261730 (Rn) | ||||||||||||||||||||||||
| OMIM | 603072 (Hs) | ||||||||||||||||||||||||
| UniProtKB | O14965 (Hs) , P97477 (Mm) , P59241 (Rn) | ||||||||||||||||||||||||
| RefSeq Nucleotide | NM_003600 (Hs) , NM_011497 (Mm) , NM_153296 (Rn) | ||||||||||||||||||||||||
| RefSeq Protein | NP_003591 (Hs) , NP_035627 (Mm) , NP_695208 (Rn) | ||||||||||||||||||||||||
| Protein GI | 38327562 (Hs) , 46358064 (Mm) , 76253851 (Rn) | ||||||||||||||||||||||||
| ChEMBL Target | CHEMBL4722 (Hs) , CHEMBL2211 (Mm) |
| Target ID | 1937 | ||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 名称 | aurora kinase B | ||||||||||||||||||||||||
| 缩写名 | AurB | ||||||||||||||||||||||||
| 家族 | Aurora kinase (Aur) family | ||||||||||||||||||||||||
| 别名 | KIAA0786 | ||||||||||||||||||||||||
| 基因和蛋白信息 |
|
||||||||||||||||||||||||
| Ensembl Gene | ENSG00000178999 (Hs) , ENSMUSG00000020897 (Mm) , ENSRNOG00000005659 (Rn) | ||||||||||||||||||||||||
| Entrez Gene | 9212 (Hs) , 20877 (Mm) , 114592 (Rn) | ||||||||||||||||||||||||
| OMIM | 604970 (Hs) | ||||||||||||||||||||||||
| UniProtKB | O55099 (Rn) , O70126 (Mm) , Q96GD4 (Hs) | ||||||||||||||||||||||||
| RefSeq Nucleotide | NM_001256834 (Hs) , NM_011496 (Mm) , NM_053749 (Rn) | ||||||||||||||||||||||||
| RefSeq Protein | NP_004208 (Hs) , NP_035626 (Mm) , NP_446201 (Rn) | ||||||||||||||||||||||||
| Protein GI | 83776600 (Hs) , 51317394 (Mm) , 16758580 (Rn) | ||||||||||||||||||||||||
| ChEMBL Target | CHEMBL1075275 (Mm) , CHEMBL2185 (Hs) |
| Target ID | 1938 | ||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 名称 | aurora kinase C | ||||||||||||||||||||||||
| 缩写名 | AurC | ||||||||||||||||||||||||
| 家族 | Aurora kinase (Aur) family | ||||||||||||||||||||||||
| 别名 | KIAA0786 | ||||||||||||||||||||||||
| 基因和蛋白信息 |
|
||||||||||||||||||||||||
| Ensembl Gene | ENSG00000105146 (Hs) , ENSMUSG00000070837 (Mm) , ENSRNOG00000015825 (Rn) | ||||||||||||||||||||||||
| Entrez Gene | 6795 (Hs) , 20871 (Mm) , 292554 (Rn) | ||||||||||||||||||||||||
| OMIM | 603495 (Hs) | ||||||||||||||||||||||||
| UniProtKB | O88445 (Mm) , Q9UQB9 (Hs) | ||||||||||||||||||||||||
| RefSeq Nucleotide | NM_001015878 (Hs) , NM_001080965 (Mm) , NM_001106221 (Rn) | ||||||||||||||||||||||||
| RefSeq Protein | NP_001015878 (Hs) , NP_001074434 (Mm) , NP_001099691 (Rn) | ||||||||||||||||||||||||
| Orphanet | 160048 (Hs) | ||||||||||||||||||||||||
| Protein GI | 62865639 (Hs) , 124378046 (Mm) , 157820399 (Rn) | ||||||||||||||||||||||||
| ChEMBL Target | CHEMBL3935 (Hs) |
关联配体
| Ligand ID | 5718 |
|---|---|
| 名称 | tozasertib |
| 别名 | MK 0457 |
| 类别 | Synthetic organic |
| 学名 | N-[4-({4-[(3-methyl-1H-pyrazol-5-yl)amino]-6-(4-methylpiperazin-1-yl)pyrimidin-2-yl}sulfanyl)phenyl]cyclopropanecarboxamide |
| 生物活性评价 |
The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in |
| 评价 |
Tozasertib is a potent inhibitor of all three members of the Aurora kinase family |
参考文献
| 1. Harrington EA, Bebbington D, Moore J, Rasmussen RK, Ajose-Adeogun AO, Nakayama T, Graham JA, Demur C, Hercend T, Diu-Hercend A et al.. (2004) VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo.. Nat Med, 10 (3): (262-7). [PMID:14981513] |
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