1. Stem Cell/Wnt
  2. YAP
  3. IAG933

IAG933 是一种新型的小分子化合物。IAG933 是一种针对 YAP-TEAD 蛋白-蛋白相互作用 (PPI) 的直接且选择性强的干扰剂。IAG933 通过与 TEAD 蛋白的 Ω-loop 口袋结合,直接阻止 YAP/TAZTEADs 形成复合体,从而干扰 YAP 的致癌功能。IAG933 可以用于对 Hippo 信号通路和特定类型癌症的研究。

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IAG933 Chemical Structure

IAG933 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IAG933 is a small molecule compound. IAG933 is a direct and selective disruptor of YAP-TEAD protein-protein interaction (PPI). By binding to the Ω-loop pocket of TEAD protein, IAG933 directly prevents YAP/TAZ from forming complexes with TEADs, thereby interfering with YAP's carcinogenic function. IAG933 can be used to study the Hippo signaling pathway and specific types of cancer[1].

体外研究
(In Vitro)

IAG933 (0.0001-10 μM,24 h) 几乎完全抑制了 msto211h 细胞和另一种 hippo 改变的间皮瘤系 NCI-H226 中 TEAD 靶基因 CCN1,ANKRD1 和 CCN2 的表达,IC50 在 11 -26 nM 之间。特别是在间皮瘤中,无论通路改变如何,其生长抑制 (GI50) 值在 13 至 91 nM 之间[1]
IAG933 (0.0001-10 μM,72 h) 在多种 Hippo 信号通路改变的肿瘤细胞系中显示出显著的抗增殖活性,尤其是在胸膜间皮瘤细胞系中[1]

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

Cell Proliferation Assay[1]

Cell Line: TEAD-dependent mesothelioma lines
Concentration: 0.37 μM
Incubation Time: 72 h
Result: Showed significant anti-proliferative activity in mesothelioma, hippo altered, and non-hippo mutant cell lines, and the cell line activity decreased to less than 10% after 72 hours of administration
体内研究
(In Vivo)

IAG933 (30-240 mg/kg,op.;24 时) 在小鼠 msto211h 细胞来源的异种移植物模型中进行单剂量评估实验表现出对 TEAD 转录快速且高效的抑制作用[1]
IAG933 (70 和 210 mg/kg,op.;28天) 可预防胸膜肿瘤负荷增加引起的小鼠发病,抗肿瘤反应持续4周以上,且 IAG933 不会造成体重减轻和耐受性问题在小鼠模型中[1]
IAG933 (10 and 30 mg/kg,op.;14 天) 对肿瘤的暴露量与剂量成正比,没有观察到体重减轻,治疗耐受性良好在大鼠模型中[1]
IAG933 (200 mg/kg,op.;70 天) 表现出良好的抗肿瘤反应在 nf2 改变的三阴性乳腺癌 PDX 模型中[1]

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

Animal Model: NF2-altered PDX model of triple-negative breast cancer[1]
Dosage: 200 mg/kg
Administration: Oral gavage (p.o.)
Result: Demonstrated a favorable tumor response, including deep tumor shrinkage and persistent tumor arrest.
Animal Model: mouse MSTO-211H cell-derived xenograft (CDX) models[1]
Dosage: 30-240 mg/kg
Administration: Oral gavage (p.o.)
Result: Demonstrated dose-dependent antitumor effects, including tumor arrest and significant tumor shrinkage. At a dose of 240 mg/kg, nearly complete regression of the tumor was observed. No weight loss was observed during treatment.
分子量

529.96

Formula

C27H26ClF2N3O4

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

IAG933 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    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.

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IAG933
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HY-158384
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