2. Apoptosis
  3. MDM-2/p53 Apoptosis
  4. MI-773 TFA

MI-773 TFA 是一种具有口服活性的选择性 MDM2-p53 相互作用抑制剂，对 MDM2 的 Ki 值为 0.88 nM。 MI-773 TFA 可阻断 MDM2-TP53 的相互作用。 MI-773 TFA 可强效激活 p53。 MI-773 TFA 可诱导细胞凋亡 (Apoptosis)。 MI-773 TFA 可在腺样囊性癌异种移植模型中引起肿瘤消退。 MI-773 TFA 在神经母细胞瘤中表现出抗癌作用。 MI-773 TFA 可用于腺样囊性癌的相关研究。

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CAS No. : 1303609-37-1

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MI-773 TFA 相关抗体

Top Publications Citing Use of Products

    MI-773 TFA purchased from MCE. Usage Cited in: Nat Chem Biol. 2018 Feb;14(2):118-125.  [Abstract]

    HCT 116 cells are treated with 4, ent-4 and SAR405838 for 2 h and lysed for western blotting analysis probing for USP7, p53, p-Ser15-p53, p21, MDM2 and β-actin as indicated.

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    MI-773 TFA is an orally active, selective MDM2-p53 interaction inhibitor with a Ki of 0.88 nM for MDM2. MI-773 TFA blocks the MDM2-TP53 interaction. MI-773 TFA potently activates p53. MI-773 TFA induces Apoptosis. MI-773 TFA causes tumor regression in xenograft models of adenoid cystic carcinoma. MI-773 TFA exhibits anticancer effects in neuroblastoma. MI-773 TFA can be used for the research of adenoid cystic carcinoma[1][2].

    体内研究
    (In Vivo)

    MI-773 (10-100 mg/kg；口服；每日) 可在 UM-PDX-HACC-5 腺样囊性癌模型中诱导剂量依赖性的肿瘤生长抑制与消退，其中 100 mg/kg 剂量可通过 p53 依赖性细胞凋亡介导 127% TGI 指数和 86% 的肿瘤缩小[1]。
    MI-773 (100 mg/kg; p.o.; daily) 在 ACCx6 腺样囊性癌 PDX 模型中可介导显著的肿瘤消退[1]。
    MI-773 (100 mg/kg; p.o.; daily) 在 ACCx9 腺样囊性癌 PDX 模型中可介导显著的肿瘤消退[1]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: CB.17.SCID (male and female, severe combined immunodeficient)[1]
    Dosage: 10 mg/kg; 50 mg/kg; 100 mg/kg
    Administration: p.o.; daily
    Result: Modestly reduced tumor growth rate, resulting in a tumor growth inhibition (TGI) index of 34% and final average tumor volume of 600 mm3 at 20 days of treatment (10 mg/kg).
    Caused significant tumor regression, with a TGI index of 127%, 86% tumor shrinkage, and final average tumor volume of 30 mm3 at 20 days of treatment (100 mg/kg).
    Increased time to tumor failure (defined as 2x increase in pre-treatment volume; p=0.044) (100 mg/kg).
    Increased percentage of TUNEL-positive apoptotic cells (p=0.015) and p53-positive cells (p<0.001) in tumor tissue, with p53 localization shifted from nuclear to cytoplasmic (100 mg/kg).
    Increased p53 and phospho-p53 (Ser392) protein levels in tumor lysates (50 or 100 mg/kg).
    Showed no observable weight loss in all treatment groups.
    分子量

    676.53

    Formula

    C31H35Cl2F4N3O5
    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献

    MI-773 TFA 相关分类

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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    MI-7731303609-37-1MI773MI 773MDM-2/p53Apoptosisp21G2/M phase checkpoint genesG1 cell cycle arrestMDM2-p53 interactionp53apoptosisMDM2patient-derived xenograft modelsadenoid cystic carcinomaneuroblastoma cellsInhibitorinhibitorinhibit

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    目录号：
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