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A-1210477
产品价格查看更多规格...
| 产品编号 | 包装单位 | 单价(元) | 国内现货 | 国外库存 | 询价单 |
| 4086509 | 5 MG | 1190 | |||
| 4086509 | 25 MG | 4390 |
产品别名
1668553-26-1
A-1210477
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-pyrazol-4-yl]-1-[2-(4-morpholinyl)ethyl]-3-[3-(1-naphthalenyloxy)propyl]-1H-indole-2-carboxylic acid
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C46H55N7O7S |
| Molecular weight | 850.04 |
| Biochem/physiol Actions【生化/生理作用】 | A-1210477 is a BH3 mimetic that targets MCL-1 with high affinity (Ki = 0.43 nM) and selectivity (Ki >0.66 μM for BCL-2, BCL-XL, BCL-W, and A1), exhibiting little to no activity toward panels of 80 kinases (IC50 >8.5 μM) and 21 GPCRs (IC50 & EC50 >10 μM). A-1210477 selectively inhibits the survival of MCL-1-dependent (IC50 ~4 μM/multiple myeloma H929, 5.3 μM/NSCLC H2110, 7.2 μM/NSCLC H23), but not BCL-2-dependent RS4;11, cultures via apoptosis induction and potentiates BCL-2/BCL-XL inhibitor ABT-263 (Navitoclax) killing in a variety of cancer cell cultures where ABT-263 alone is ineffective. A-1210477 is also shown to cause cellular MCL-1 upregulation, most likely due to blocking MCL-1 interaction with BH3-only proteins such as NOXA and MULE known to mediate MCL-1 ubiquitylation for proteasomal degradation. |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥98% (HPLC) |
| form【形式】 | powder |
| color【颜色】 | white to beige |
| solubility【溶解性】 | DMSO: 2 mg/mL, clear |
| storage temp.【储存温度】 | −20℃ |
| SMILES string | O=C(O)C(N1CCN2CCOCC2)=C(C3=C1C(C4=C(N(N=C4C)C)COC5=CC=C(C=C5)N6CCN(CC6)S(=O)(N(C)C)=O)=CC=C3)CCCOC7=C8C=CC=CC8=CC=C7.[H]Cl |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
