A-1210477
Cat. No.：YN270175
CAS No. ：1668553-26-1
| 产品名称: | A-1210477 |
| CAS No.: | 1668553-26-1 |
| Chemical Name: | 7-[5-[[4-[4-[(dimethylamino)sulfonyl]-1-piperazinyl]phenoxy]methyl]-1,3-dimethyl-1H-pyrazol-4-yl]-1-[2-(4-morpholinyl)ethyl]-3-[3-(1-naphthalenyloxy)propyl]-1H-indole-2-carboxylic acid |
| Synonyms: | 7-(1,3-Dimethyl-5-((4-(4-(methylsulfonyl)piperazin-1-yl)phenoxy)methyl)-1H-pyrazol-4-yl)-1-(2-morpholinoethyl)-3-(3-(naphthalen-1-yloxy)propyl)-1H-indole-2-carboxylic acid;7-[5-[[4-[4-[(Dimethylamino)sulfonyl]-1-piperazinyl]phenoxy]methyl]-1,3-dimethyl-1H |
| 分子量: | 850.04 |
| 分子式: | C₄₆H₅₅N₇O₇S |
| SMILES: | O=C(C(N1CCN2CCOCC2)=C(CCCOC3=C4C=CC=CC4=CC=C3)C5=C1C(C6=C(COC7=CC=C(N8CCN(S(=O)(N(C)C)=O)CC8)C=C7)N(C)N=C6C)=CC=C5)O |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | A-1210477 是一种有效，选择性的MCL-1抑制剂，Ki值为 0.45 nM。A-1210477 特异性结合 MCL-1，并以 MCL-1 依赖性方式促进癌细胞凋亡 (apoptosis)。 |
| IC50和靶点: | [{name:"Mcl-1:0.45 nM (Ki)"},{name: "Bcl-2:132 nM (Ki)"},{name: "Bfl-1:660 nM (Ki)"},{name: "Bcl-W:2280 nM (Ki)'}, 'Apoptosis'] |
| In Vitro: | |
| In Vivo: | |
| Clinical Trial: | |
| Solvent & Solubility: |
Leverson, J.D., Zhang, H., Chen, J., et al.Potent and selective small-molecule MCL-1 inhibitors demonstrate on-target cancer cell killing activity as single agents and in combination with ABT-263 (navitoclax)Cell Death Dis.6,e1590(2015)
Bruncko, M., Wang, L., Sheppard, G.S., et al.Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity.J. Med. Chem.58(5),2180-2194(2015)
Opfeman, J.T.Attacking cancer's Achilles heel: Antagonism of anti-apoptotic BCL-2 family membersFEBS J.283(14),2661-2675(2016)
