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A 1210477

Cat. No. 6409 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

Discontinued Product

6409 has been discontinued.

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说明： Selective, high affinity Mcl-1 inhibitor; proapoptotic
化学名： 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
纯度： ≥98% (HPLC)
说明书
引用文献
评论
文献 (2)
通路 (1)
生物活性 技术数据 说明书 参考文献

生物活性 for A 1210477

A 1210477 is a selective, high affinity Mcl-1 inhibitor (Ki = 454 pM). Disrupts Mcl-BIM complexes (IC50 in low μM range). Also inhibits Mcl-1NOXA interactions. Exhibits no effect on Bcl-XL-Bim or Bcl-X-BCL-Xs interactions. Induces apoptosis in multiple myeloma and non-small cell lung cancer cell lines and exhibits a synergistic effect with NavitoclaxTM to induce apoptosis in vitro. Cell permeable.

技术数据 for A 1210477

分子量 850.04
公式 C46H55N7O7S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1668553-26-1
PubChem ID 66575373
InChI Key XMVAWGSQPHFXKU-UHFFFAOYSA-N
Smiles CN(C)S(=O)(=O)N1CCN(CC1)C1=CC=C(OCC2=C(C(C)=NN2C)C2=C3N(CCN4CCOCC4)C(C(O)=O)=C(CCCOC4=CC=CC5=C4C=CC=C5)C3=CC=C2)C=C1

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

参考文献 for A 1210477

参考文献是支持产品生物活性的出版物。

Bruncko et al (2015) Structure-guided design of a series of MCL-1 inhibitors with high affinity and selectivity. J.Med.Chem. 58 2180 PMID: 25679114

Leverson et al (2015) 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 PMID: 25590800

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关键词: A 1210477, A 1210477 supplier, A1210477, Mcl-1, inhibitors, inhibits, apoptosis, proapoptotic, selective, high, affinity, multiple, myeloma, non-small, cell, lung, cancer, Bcl-2, Family, 6409, Tocris Bioscience

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