您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 品牌 > Sigma-Aldrich > A-1210477

A-1210477

品牌
Sigma-Aldrich
CAS
1668553-26-1
货号
SML1932
规格纯度
≥98% (HPLC)
参考价格
1088.31 *本价格含增值税费
促销
服务
  • 原厂保证
  • 包邮
  • 增值税票
数量
-+
产品名称:
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
产品介绍:

产品说明

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.

基本信息

经验(实验)分子式C46H55N7O7S
分子量850.04

产品性质

质量水平100
测定≥98% (HPLC)
形式powder
颜色 white to beige
溶解性DMSO: 2 mg/mL, clear
储存温度−20℃
SMILES stringO=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

储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

Sigma-Aldrich

推荐产品