Takinib|1111556-37-6|-陌孚医药/Medlife

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Takinib

目录号: PL06938 纯度: ≥99%

CAS No. :1111556-37-6

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中文名称	Takinib
英文名称	Takinib
英文别名	N1-(1-Propyl-1H-benzimidazol-2-yl)-1,3-benzenedicarboxamide;Takinib;3-N-(1-propylbenzimidazol-2-yl)benzene-1,3-dicarboxamide;GTPL9655;N1-(1-Propyl-1H-benzo[d]imidazol-2-yl)isophthalamide;s8663;SY251736;A16960;Z332866662;1-N-(1-propyl-1H-1,3-benzodiazol-2-yl)benzene-1,3-dicarboxamide;N1-(1-propyl-1H-1,3-benzodiazol-2-yl)benzene-1,3-dicarboxamide
Cas No.	1111556-37-6
分子式	C₁₈H₁₈N₄O₂
分子量	322.36
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	Takinib (EDHS-206) 是一种有效且选择性的 TAK1 抑制剂 (IC₅₀=9.5 nM)，比 IRAK4 (IC₅₀=120 nM) 和 IRAK1 (IC₅₀=390 nM) 作用强 1.5 log 倍。Takinib 是一种TAK1自磷酸化的抑制剂，在 ATP 结合口袋内非竞争性结合。在类风湿关节炎和转移性乳腺癌细胞模型中，Takinib 诱导 TNF-α 刺激的细胞凋亡 (apoptosis)。Takinib 也是恶性疟原虫蛋白激酶 9 (PfPK9) 的抑制剂 (K_D(app) of 0.46 nM)。
生物活性	Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC 50 =9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (K D(app) of 0.46 μM).
性状	Solid
IC50 & Target[1][2]	TAK1 9.5 nM (IC50) IRAK4 120 nM (IC50
体外研究(In Vitro)	Takinib (10-10000 nM; 24 hours) induces apoptosis following TNF-α stimulation in MDA-MB-231 cells. Takinib (10 μM; 0-1 hours) reduces phosphorylation of IKK and p65. Takinib serves as a chemical starting point for the development of Pf PK9 (KD(app) of 0.46 μM) inhibitors for malaria. Takinib (2 hours; 0.1-20 μM; human RASFs) induces phosphorylation of TAK1, STAT3 and STAT3 in IL-1β-treated (10 ng/mL; 30 min) RASFs. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Takinib (50 mg/kg; intraperitoneally; daily from days 18-36) reduces the clinical score in type II collagen-induced arthritis (CIA) mouse model of rheumatoid arthritis. Takinib (50 mg/kg; oral gavage; daily until 17 days) slows tumor growth in the Hodgkin lymphoma xenograft NSG mice. 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
参考文献	[1]. Totzke J, et al. Takinib, a Selective TAK1 Inhibitor, Broadens the Therapeutic Efficacy of TNF-α Inhibition for Cancer and Autoimmune Disease. Cell Chem Biol. 2017 Aug 17;24(8):1029-1039. [2]. Scarneo SA, et.al. Pharmacological inhibition of TAK1, with the selective inhibitor takinib, alleviates clinical manifestation of arthritis in CIA mice. Arthritis Res Ther. 2019 Dec 17;21(1):292.

溶解度数据	In Vitro: DMSO : 50 mg/mL (155.11 mM; Need ultrasonic)配制储备液

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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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