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A 1331852

Cat. No. 7661 提交评论 说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）
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说明： Potent and selective Bcl-xL inhibitor; antitumor and inducer of apoptosis
化学名： 6-[8-[(2-Benzothiazolylamino)carbonyl]-3,4-dihydro-2(1H)-isoquinolinyl]-3-[5-methyl-1-(tricyclo[3.3.1.13,7]dec-1-ylmethyl)-1H-pyrazol-4-yl]-2-pyridinecarboxylic 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 溶解性 计算器 说明书 参考文献

生物活性 for A 1331852

A 1331852 is a high affinity and selective Bcl-xL inhibitor (Ki <0.01 nM), also inhibits Bcl-W, Bcl-2, and Mcl-1 (Ki values are 4, 6 and 142 nM, respectively). A 1331852 inhibits Bcl-xL-dependent Molt 4 acute lymphoblastic leukemia cell growth in vitro (EC50 = 6 nM). It enhances antitumor effects of Docetaxel (Cat. No. 4056) and Venetoclax (Cat. No. 6960) in xenograft models of breast and lung cancer. A 1331852 also induces apoptosis in and clears senescent biliary epithelial cells (BECs), and induces apoptosis in xenograft models of EBV-associated T- and natural killer cell lymphoma.

技术数据 for A 1331852

分子量 658.81
公式 C38H38N6O3S
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 1430844-80-6
PubChem ID 71565985
InChI Key QCQQONWEDCOTBV-UHFFFAOYSA-N
Smiles O=C(C1=C(CN(C2=CC=C(C3=C(C)N(CC4(C5)CC(C[C@@H]5C6)CC6C4)N=C3)C(C(O)=O)=N2)CC7)C7=CC=C1)NC8=NC9=C(S8)C=CC=C9

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.

溶解性数据 for A 1331852

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 13.18 20

制备储备液 for A 1331852

以下数据基于产品分子量 658.81。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

选择批次从而根据批次分子量重新计算:
浓度/溶剂体积/质量 1 mg 5 mg 10 mg
0.2 mM 7.59 mL 37.95 mL 75.89 mL
1 mM 1.52 mL 7.59 mL 15.18 mL
2 mM 0.76 mL 3.79 mL 7.59 mL
10 mM 0.15 mL 0.76 mL 1.52 mL

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参考文献 for A 1331852

参考文献是支持产品生物活性的出版物。

Bierbrauer et al (2020) A direct comparison of selective BH3-mimetics reveals BCL-XL, BCL-2 and MCL-1 as promising therapeutic targets in neuroblastoma. Br.J.Cancer 122 1544 PMID: 32203216

Moujalled et al (2020) Cotargeting BCL-2 and MCL-1 in high-risk B-ALL. Blood Adv. 4 2762 PMID: 32569380

Sasaki et al (2020) Increased p16INK4a-expressing senescent bile ductular cells are associated with inadequate response to ursodeoxycholic acid in primary biliary cholangitis. J.Autoimmun. 107 102377 PMID: 31812332

Sejic et al (2020) BCL-XL inhibition by BH3-mimetic drugs induces apoptosis in models of Epstein-Barr virus-associated T/NK-cell lymphoma. Blood Adv. 4 4775 PMID: 33017468

Leverson et al (2015) Exploiting selective BCL-2 family inhibitors to dissect cell survival dependencies and define improved strategies for cancer therapy. Sci.Transl.Med. 7 279ra40 PMID: 25787766

If you know of a relevant reference for A 1331852, please let us know.

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关键词: A 1331852, A 1331852 supplier, A1331852, potent, selective, bclxl, bcl-xl, inhibitors, antitumor, apoptosis, apoptotic, xenograft, lymphoma, SCLC, breast, leukemia, senescent, biliary, epithelial, cells, EBV, epstein, barr, virus, Bcl-2, Family, Other, Apoptosis, 7661, Tocris Bioscience

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