TAK-243|1450833-55-2|(MLN7243)-陌孚医药/Medlife

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TAK-243 (Synonyms: MLN7243)

目录号: PL07801 纯度: ≥98%

CAS No. :1450833-55-2

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中文名称	TAK-243
英文名称	TAK-243
英文别名	TAK-243
Cas No.	1450833-55-2
分子式	C₁₉H₂₀F₃N₅O₅S₂
分子量	519.52
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

TAK-243 (MLN7243) 是一种首创的，选择性的泛素激活酶，UAE (UBA1) 抑制剂 (IC₅₀=1 nM)，其阻断了泛素结合，破坏了单泛素信号传导和全蛋白泛素化。TAK-243 (MLN7243) 诱导内质网应激 (ERS) 反应，消除 NF-κB 通路活化，促进细胞凋亡。

生物活性

TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC 50 =1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.

性状

Solid

IC50 & Target[1][2]

IC50: 1 nM (UBA1)

体外研究(In Vitro)

TAK-243 shows anti-proliferative effect on a panel of cell lines derived from hematologic and solid tumors with variable EC50 values that ranged from 0.006 μM to 1.31 μM.
TAK-243 reduces growth and viability of human AML cell lines (OCI-AML2, TEX, U937 and NB4) in a concentration- and time-dependent manner with IC50s ranging from 15-40 nM after treatment for 48 hours. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

TAK-243 significantly delays tumor growth in mice (T/C=0.02) with no toxicity as evidenced by no changes in mouse body weight, serum chemistry, or organ histology. TAK-243 reduces primary AML tumor burden in both tested samples without toxicity. 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]. Hyer ML, et al. A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment. Nat Med. 2018 Feb;24(2):186-193.
[2]. Best SR, et al. TAK-243, a small molecule inhibitor of ubiquitin-activating enzyme (UAE), induces ER stress and apoptosis in diffuse large B-cell lymphoma (DLBCL) cells. Blood 2017 130:1533.
[3]. Samir H. Barghout, et

溶解度数据	In Vitro: DMSO : 50 mg/mL (96.24 mM; Need ultrasonic)H₂O : 1 mg/mL (1.92 mM; Need ultrasonic)配制储备液

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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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