IAG933

IAG933
Identifiers
	IUPAC name 4-[(2S)-5-chloro-6-fluoro-2-phenyl-2-[(2S)-pyrrolidin-2-yl]-3H-1-benzofuran-4-yl]-5-fluoro-6-(2-hydroxyethoxy)-N-methylpyridine-3-carboxamide;
CAS Number	2714434-21-4;
PubChem CID	156855755;
IUPHAR/BPS	13367;
ChemSpider	129424100;
PDB ligand	WCF (PDBe, RCSB PDB);
Chemical and physical data
Formula	C27H26ClF2N3O4
Molar mass	529.97 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CNC(=O)C1=CN=C(C(=C1C2=C3C[C@@](OC3=CC(=C2Cl)F)([C@@H]4CCCN4)C5=CC=CC=C5)F)OCCO;
	InChI InChI=InChI=1S/C27H26ClF2N3O4/c1-31-25(35)17-14-33-26(36-11-10-34)24(30)22(17)21-16-13-27(20-8-5-9-32-20,15-6-3-2-4-7-15)37-19(16)12-18(29)23(21)28/h2-4,6-7,12,14,20,32,34H,5,8-11,13H2,1H3,(H,31,35)/t20-,27-/m0/s1; Key:HUVOYQMXUNTUAI-DCFHFQCYSA-N;

IAG933 is an investigational new drug that is being evaluated for the treatment of cancer.^[1]

IAG933 is a small molecule inhibitor developed by Novartis Pharmaceuticals to directly disrupt the YAP/TAZ-TEAD protein-protein interaction, a critical mediator of oncogenic signaling in the Hippo pathway. This drug has demonstrated potent and selective inhibition of all four TEAD paralogs, resulting in YAP eviction from chromatin and reduced Hippo-mediated transcription.^[2] As of 2024, IAG933 is undergoing Phase I clinical trials to evaluate its safety, tolerability, and preliminary anti-tumor activity in patients with advanced mesothelioma and other solid tumors harboring specific molecular alterations in the Hippo pathway.^[3]

References

^ "IAG933". AdisInsight. Springer Nature Switzerland AG.
^ Chapeau EA, Sansregret L, Galli GG, Chène P, Wartmann M, Mourikis TP, et al. (July 2024). "Direct and selective pharmacological disruption of the YAP-TEAD interface by IAG933 inhibits Hippo-dependent and RAS-MAPK-altered cancers". Nature Cancer. 5 (7): 1102–1120. doi:10.1038/s43018-024-00754-9. PMC 11286534. PMID 38565920.
^ Clinical trial number NCT04857372 for "A Phase I Study of IAG933 in Patients With Advanced Mesothelioma and Other Solid Tumors" at ClinicalTrials.gov

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[1] "IAG933". AdisInsight. Springer Nature Switzerland AG.

[Chapeau_2024-2] Chapeau EA, Sansregret L, Galli GG, Chène P, Wartmann M, Mourikis TP, et al. (July 2024). "Direct and selective pharmacological disruption of the YAP-TEAD interface by IAG933 inhibits Hippo-dependent and RAS-MAPK-altered cancers". Nature Cancer. 5 (7): 1102–1120. doi:10.1038/s43018-024-00754-9. PMC 11286534. PMID 38565920.

[3] Clinical trial number NCT04857372 for "A Phase I Study of IAG933 in Patients With Advanced Mesothelioma and Other Solid Tumors" at ClinicalTrials.gov

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Identifiers

IUPAC name 4-[(2S)-5-chloro-6-fluoro-2-phenyl-2-[(2S)-pyrrolidin-2-yl]-3H-1-benzofuran-4-yl]-5-fluoro-6-(2-hydroxyethoxy)-N-methylpyridine-3-carboxamide
CAS Number	2714434-21-4
PubChem CID	156855755
IUPHAR/BPS	13367
ChemSpider	129424100
PDB ligand	WCF (PDBe, RCSB PDB)
Chemical and physical data
Formula	C₂₇H₂₆ClF₂N₃O₄
Molar mass	529.97 g·mol⁻¹
3D model (JSmol)	Interactive image
SMILES CNC(=O)C1=CN=C(C(=C1C2=C3C[C@@](OC3=CC(=C2Cl)F)([C@@H]4CCCN4)C5=CC=CC=C5)F)OCCO
InChI InChI=InChI=1S/C27H26ClF2N3O4/c1-31-25(35)17-14-33-26(36-11-10-34)24(30)22(17)21-16-13-27(20-8-5-9-32-20,15-6-3-2-4-7-15)37-19(16)12-18(29)23(21)28/h2-4,6-7,12,14,20,32,34H,5,8-11,13H2,1H3,(H,31,35)/t20-,27-/m0/s1 Key:HUVOYQMXUNTUAI-DCFHFQCYSA-N