Tanzisertib|899805-25-5|-陌孚医药/Medlife

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Tanzisertib

目录号: PL04444 纯度: ≥99%

CAS No. :899805-25-5

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中文名称	Tanzisertib
英文名称	Tanzisertib
英文别名	4-[[9-[(3S)-oxolan-3-yl]-8-(2,4,6-trifluoroanilino)purin-2-yl]amino]cyclohexan-1-ol;TANZISERTIB;UNII-M5O06306UO;CHEMBL1950289;CC-930;Tanzisertib (USAN);Tanzisertib [USAN];3tti;trans-4-((9-((3S)-Tetrahydrofuran-3-yl)-8-((2,4,6-trifluorophenyl)amino)-9H-purin-2-yl)amino)cyclohexanol;Trans-4-({9-[(3s)-Tetrahydrofuran-3-Yl]-8-[(2,4,6-Trifluorophenyl)amino]-9h-Purin-2-Yl}amino)cyclohexanol;Tanzisertib(CC-930);CC930;CC 930;M5O06306UO;Tanzisertib [USAN:INN];GTPL9836;JNK 930;EX-A3;trans-4-[[9-[(3S)-Tetrahydro-3-furanyl]-8-[(2,4,6-trifluorophenyl)amino]-9H-purin-2-yl]amino]cyclohexanol (ACI);Tanzisertib
Cas No.	899805-25-5
分子式	C₂₁H₂₃F₃N₆O₂
分子量	448.44
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

Tanzisertib (CC-930) 是有效的 JNK1/2/3 抑制剂，IC₅₀ 分别为61/7/6 nM。

生物活性

Tanzisertib (CC-930) is a potent JNK1/2/3 inhibitor with IC 50 s of 61/7/6 nM, respectively.

性状

Solid

IC50 & Target[1][2]

JNK3 6 nM (IC50) JNK2 7 nM (IC50

体外研究(In Vitro)

Tanzisertib (CC-930) inhibits the formation of phospho-cJun in human PBMC stimulated by phorbol-12-myristate-13-acetate and phytohemeagglutinin (IC50=1 μM). Tanzisertib (CC-930) (1-2 μM) substantially reduces hepatocyte apoptosis and necrosis, abrogates apoptosis and necrosis in FC-loaded WT hepatocytes. Tanzisertib (CC-930) blocks the JNK pathway that is activated by pro-fibrotic cytokines in systemic sclerosis. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Tanzisertib (CC-930) (10 and 30 mg/kg, p.o.) inhibits the production of TNFa by 23% and 77% in the acute rat LPS-induced TNFa production PK-PD model. Tanzisertib (CC-930) (150 mg/kg) prevents the development of fibrosis in different models, but can also induce the regression of pre-existing fibrosis. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Plantevin Krenitsky V, et al. Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1433-8.
[2]. Gan LT, et al. Hepatocyte free cholesterol lipotoxicity results from JNK1-mediated mitochondrial injury and is HMGB1 and TLR4-dependent. J Hepatol. 2014 Dec;61(6):1376-84.
[3]. Reich N, et al. Jun N-termina

溶解度数据	In Vitro: 1M HCl : 100 mg/mL (223.00 mM; ultrasonic and adjust pH to 1 with HCl)DMSO : ≥ 33 mg/mL (73.59 mM)

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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