| Chemical Properties | Back Directory | [Boiling point ]
626.125±55.00 °C(Press: 760.00 Torr)(predicted) | [density ]
1.367±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | [form ]
Solid | [pka]
13.275±0.46(predicted) | [color ]
White to off-white | [InChIKey]
HUVOYQMXUNTUAI-UHFFFAOYSA-N | [SMILES]
ClC1=C(C=C2C(=C1C1=C(C(=NC=C1C(=O)NC)OCCO)F)CC(C1C=CC=CC=1)(C1NCCC1)O2)F |
| Hazard Information | Back Directory | [Uses]
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[1][2]. | [in vivo]
IAG933 (30-240 mg/kg, i.g., once a day, 28 days) shows a dose-dependent anti-tumor effect in mouse xenograft models, promoting cell apoptosis[2].
IAG933 (3-30 mg/kg, i.g., once a day, 2 weeks) causes tumor regression in the MSTO-211H rat xenograft model[2]. | Animal Model: | Mouse MSTO-211H cell-derived xenograft (CDX) model; mouse NCI-H226 cell-derived xenograft (CDX) model[2] | | Dosage: | 30, 60, 120, 240 mg/kg, single dose; 70, 210 mg/kg, once daily, 28 days | | Administration: | i.g. | | 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] | | Dosage: | 3, 10, 30 mg/kg, once daily, 2 weeks | | Administration: | i.g. | | Result: | Showed the tumor stagnant at 10 mg/kg, and shrank at 30 mg/kg. |
| [IC 50]
YAP/TAZ-TEAD | [References]
[1] Bordas V, et al. Preparation of biaryl derivatives as YAP/TAZ-TEAD protein-protein interaction inhibitors. World Intellectual Property Organization, WO2021186324 A1. 2021-09-23.
[2] Emilie A Chapeau， 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 Jul;5(7):1102-1120. DOI:10.1038/s43018-024-00754-9 |
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| Company Name: |
DC Chemicals
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| Tel: |
021-58447131 13564518121 |
| Website: |
www.chemicalbook.com/showsupplierproductslist927327/0_en.htm |
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