IAG933
Based on 3 publication(s) in Google Scholar
IAG933 (YAP-TEAD-IN-3) is an orally available YAP/TAZ-TEAD inhibitor that has anti-tumor effects and promotes apoptosis. IAG933 YAP-TEAD-IN-3 inhibits Avi-human TEAD4217-434, with an IC50 value of 9 nM.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.47%
- CAS 番号: 2714434-21-4
- 分子式: C27H26ClF2N3O4
- 分子量:529.96
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 IAG933
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生物活性
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YAP/TAZ-TEAD |
IAG933 also has an inhibitory effect on NCI-H2052, with GI50 (inhibition of cell proliferation) and IC50 (inhibition of YAP reporter gene expression) values of 0.041 μM and 0.048 μM, respectively[1].
IAG933 (0-1 μM, 4 h) directly inhibits the interaction between YAP/TAZ and all four TEAD isoforms, selectively suppressing TEAD-driven transcriptional activity[2].
IAG933 (0.0001-10 μM, 24 h) shows a dose-dependent inhibition of TEAD target gene expression in MSTO211H and NCI-H226 cells, with IC50 values ranging from 11-26 nM[2].
IAG933 (0.001-10 μM, 72 h) demonstrates effective anti-proliferative activity in Hippo-dependent cell lines, with a GI50 of 13-91 nM in mesothelioma cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H2052, MSTO-211H
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Concentration:0, 0.3, 1 μM
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Incubation Time:4 h
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Result:Inhibited the binding of YAP and TAZ with TEAD subtypes.
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Cell Line:NCI-H2052, MSTO-211H
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Concentration:0.0001, 0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:24 h
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Result:Decreased the expression of CYR61, ANKRD1, and CTGF.
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Cell Line:MSTO-211H,NCI-H2052,NCI-H226,IST-MES2,NCI-H28，SF-268,NUGC-3,LMSU,NCI-H292,NCI-H522, Ludlu1, MKN-45, NCI-H460, CCK81, LU-99, NCI-H1792, NCI-H1944, HCC-44, SW837, HCC-1171, MDST8, NCI-H1755, CAL-12T, Hs746T, KATO-Ⅲ, CALU-3, RERF-GC-1B
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Concentration:0.001, 0.01, 0.1, 1, 10 μM
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Incubation Time:72 h
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Result:Suppressed the proliferation of mesothelioma and Hippo mutation cell lines showed moderate sensitivity against non-mesothelioma cell lines with Hippo mutations (SF-268, LMSU, and NUGC-3).
IAG933 (3-30 mg/kg, i.g., once a day, 2 weeks) causes tumor regression in the MSTO-211H rat xenograft model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse MSTO-211H cell-derived xenograft (CDX) model; mouse NCI-H226 cell-derived xenograft (CDX) model[2]
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Dosage:30, 60, 120, 240 mg/kg, single dose; 70, 210 mg/kg, once daily, 28 days
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Administration:i.g.
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Result:Had a short half-life in mice, inhibiting the transcription of TEAD in the body, promoting apoptosis, and lowering the expression of BCL2L1 and MCL1.
Led to tumor regression and a decrease in Ki67 expression.
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Animal Model:A rat MSTO-211H xenograft model[2]
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Dosage:3, 10, 30 mg/kg, once daily, 2 weeks
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Administration:i.g.
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Result:Showed the tumor stagnant at 10 mg/kg, and shrank at 30 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2714434-21-4
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性状 Solid
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分子量 529.96
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分子式 C27H26ClF2N3O4
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Color White to off-white
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SMILES
ClC(C(F)=CC1=C2C[C@](C3=CC=CC=C3)([C@@H]4CCCN4)O1)=[C@]2[C@@]5=C(C(NC)=O)C=NC(OCCO)=C5F
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別名
YAP-TEAD-IN-3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Biochim Biophys Acta Mol Cell Res
Development of a TEAD-independent reporter system for specific and sensitive measurement of YAP/TAZ activity. [Abstract]2026 Mar;1873(3):120111. PMID: 41534572 -
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溶剤 & 溶解度
DMSO : 116.67 mg/mL (220.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (284 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8869 mL | 9.4347 mL | 18.8693 mL | 47.1734 mL |
| 5 mM | 0.3774 mL | 1.8869 mL | 3.7739 mL | 9.4347 mL | |
| 10 mM | 0.1887 mL | 0.9435 mL | 1.8869 mL | 4.7173 mL | |
| 15 mM | 0.1258 mL | 0.6290 mL | 1.2580 mL | 3.1449 mL | |
| 20 mM | 0.0943 mL | 0.4717 mL | 0.9435 mL | 2.3587 mL | |
| 25 mM | 0.0755 mL | 0.3774 mL | 0.7548 mL | 1.8869 mL | |
| 30 mM | 0.0629 mL | 0.3145 mL | 0.6290 mL | 1.5724 mL | |
| 40 mM | 0.0472 mL | 0.2359 mL | 0.4717 mL | 1.1793 mL | |
| 50 mM | 0.0377 mL | 0.1887 mL | 0.3774 mL | 0.9435 mL | |
| 60 mM | 0.0314 mL | 0.1572 mL | 0.3145 mL | 0.7862 mL | |
| 80 mM | 0.0236 mL | 0.1179 mL | 0.2359 mL | 0.5897 mL | |
| 100 mM | 0.0189 mL | 0.0943 mL | 0.1887 mL | 0.4717 mL |
IAG933 関連分類
HY-153811 関連分類
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