2883535-99-5
Chemical Structure
GT19630
- CAS No.: 2883535-99-5
- Formula:C35H30N6O5
- Molecular Weight:614.65
IUPAC Name: (R)-1-([1,1'-biphenyl]-4-yl)-3-chloropropan-2-ol
InChIKey: YGMJASQRQLEOKY-UHFFFAOYSA-N
SMILES: O=C(C1=CC=C2C(N(C3C(NC(CC3)=O)=O)CC2=C1)=O)NCC4=CC=C(CNC(CN5C6=C(C7=CC=CC=C75)C=CC=N6)=O)C=C4
Biological Activity: GT19630 is an orally active c-Myc PROTAC targeted degrader based on the cereblon E3 ubiquitin ligase, with an IC50 of 1.5 nM against human c-Myc. GT19630 mediates the degradation of MYC, GSPT1, GSPT2, CK1 alpha, N-Myc, B7-H3 and XIAP, and disrupts the MYC-GSPT1 synergistic regulatory feedback loop. GT19630 inhibits cell proliferation, blocks S-phase progression of the cell cycle, promotes cell apoptosis, reduces cell migration capacity, induces integrated stress response, and blocks oxidative phosphorylation by inhibiting the TCA cycle. GT19630 can be used in the research of Myc-driven hematological cancers, small cell lung cancer, breast cancer, TP53-mutant cancers, and venetoclax-resistant cancers[1][2][3][4][5].
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GT19630 | 98.85% | GT19630 is an orally active c-Myc PROTAC targeted degrader based on the cereblon E3 ubiquitin ligase, with an IC50 of 1.5 nM against human c-Myc. GT19630 mediates the degradation of MYC, GSPT1, GSPT2, CK1 alpha, N-Myc, B7-H3 and XIAP, and disrupts the MYC-GSPT1 synergistic regulatory feedback loop. GT19630 inhibits cell proliferation, blocks S-phase progression of the cell cycle, promotes cell apoptosis, reduces cell migration capacity, induces integrated stress response, and blocks oxidative phosphorylation by inhibiting the TCA cycle. GT19630 can be used in the research of Myc-driven hematological cancers, small cell lung cancer, breast cancer, TP53-mutant cancers, and venetoclax-resistant cancers. | ||||||||||||||||||||
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- [1]. Ma L, et al. Abstract 5479: Discovery and evaluation of GT19630, a c-Myc/GSPT1 cereblon E3 ligase modulator (CELMoD), for targeting Myc-driven blood cancers and small cell lung cancers (SCLC). Cancer Res. 2022;82(12_Supplement):5479.
- [2]. Tang M, et al. Targeting MYC for the treatment of breast cancer: use of the novel MYC-GSPT1 degrader, GT19630. Investigational new drugs. 2025 Feb;43(1):167-179. [Content Brief]
- [3]. Lin Q, et al. Cancer Biology of GSPT1: Mechanisms and Targeted Therapy Opportunities of Molecular Glue Degraders. Advanced science (Weinheim, Baden-Wurttemberg, Germany). 2025 Dec;12(47):e11789. [Content Brief]
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[4]. Nishida Y, et al. Dual MYC and GSPT1 Protein Degrader for MYC-Driven Cancers. bioRxiv. 2025 Apr 27.
- [5]. Nishida Y, et al. C-MYC Targeting by Degradation: Novel Dual c-Myc/GSPT1 Degrader GT19715 Exerts Profound Cell Kill In Vitro and In Vivo in Acute Myeloid Leukemia and Lymphomas. AACR Annual Meeting 2022 Poster Abstract AML-147. 2022.
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