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EC 144

Cat. No. 4701 1 次引用 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： High affinity, potent and selective Hsp90 inhibitor
化学名： 5-[2-Amino-4-chloro-7-[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]-7H-pyrrolo[2,3-d]pyrimidin-5-yl]-2-methyl-4-pentyn-2-ol
纯度： ≥98% (HPLC)
说明书
引用文献 (1)
评论
文献 (2)
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 EC 144

EC 144 is a high affinity, potent and selective Hsp90 inhibitor (Ki = 0.2 nM and IC50 = 1.1 nM). Exhibits selectivity for Hsp90 over Grp94 and TRAP1 (Ki values are 61 and 255 nM respectively) and has no effect (IC50 >10 μM) against a panel of 285 kinases. Degrades Her-2 in MCF-7 breast cancer cells (EC50 = 14 nM). Blocks tumor growth and induces partial tumor regression in an N87 gastric tumor mouse model. Also inhibits LPS-induced TNFα release in an LPS shock mouse model and suppresses disease development in a rat model of collagen-induced arthritis. Exhibits <20-fold efficacy over BIIB 021 (Cat. No. 4608) in mice. Orally available and brain penetrant.

化合物库 for EC 144

EC 144 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for EC 144

分子量 413.9
公式 C21H24ClN5O2
储存 Store at -20°C
纯度 ≥98% (HPLC)
CAS Number 911397-80-3
PubChem ID 11517212
InChI Key VOASEWXFCTZRDF-UHFFFAOYSA-N
Smiles ClC1=C2C(N(CC3=C(C)C(OC)=C(C)C=N3)C=C2C#CCC(C)(C)O)=NC(N)=N1

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 EC 144

溶剂 最高浓度 mg/mL 最高浓度 mM
溶解性
DMSO 41.39 100
ethanol 2.07 5

制备储备液 for EC 144

以下数据基于产品分子量 413.9。 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
1 mM 2.42 mL 12.08 mL 24.16 mL
5 mM 0.48 mL 2.42 mL 4.83 mL
10 mM 0.24 mL 1.21 mL 2.42 mL
50 mM 0.05 mL 0.24 mL 0.48 mL

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产品说明书 for EC 144

分析证书/产品说明书
选择另一批次：
化学品安全技术说明书

参考文献 for EC 144

参考文献是支持产品生物活性的出版物。

Shi et al (2012) EC144 is a potent inhibitor of the heat shock protein 90. J.Med.Chem. 55 7786 PMID: 22938030

Yun et al (2011) EC144, a synthetic inhibitor of heat shock protein 90, blocks innate and adaptive immune responses in models of inflammation and autoimmunity. J.Immunol. 186 563 PMID: 21131419

If you know of a relevant reference for EC 144, please let us know.

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关键词: EC 144, EC 144 supplier, EC144, high, affinity, potent, selective, HSP90, heat, shock, proteins, inhibitors, inhibits, her-2, antitumor, orally, available, brain, penetrant, Hsp90, 4701, Tocris Bioscience

1 篇 EC 144 的引用文献

引用文献是使用了 Tocris 产品的出版物。 EC 144 的部分引用包括：

Catherine B et al (2021) Inhibition of the NLRP3 inflammasome by HSP90 inhibitors. Immunology 162 84-91 PMID: 32954500

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