| Bioactivity | 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]. |
| Invitro | 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. 0 --> IAG933 相关抗体: Cell Proliferation Assay[1] Cell Line: |
| 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: |
| Formula | C27H26ClF2N3O4 |
| Molar Mass | 529.96 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Chapeau EA, et al. Direct and selective pharmacological disruption of the YAP-TEAD interface by IAG933 inhibits Hippo-dependent and RAS-MAPK-altered cancers. Nat Cancer. 2024 Apr 2. |