2378056-80-3
Chemical Structure
A947
- CAS No.: 2378056-80-3
- Formula:C61H76N12O7S
- Molecular Weight:1121.40
IUPAC Name: 2,4-dichloro-7-methoxyquinazolin-6-ol
InChIKey: QQVCUSPUMMUFTD-UACDVHTESA-N
SMILES: NC1=C(C=C(C(C=CC=C2)=C2O)N=N1)N3C[C@H](CC4)N(C5=CC=NC(O[C@H](C6)C[C@@H]6OC(CC7)CCN7CC8CCN(C9=NOC([C@@H](C(C)C)C(N(C[C@@H]%10O)[C@@H](C%10)C(N[C@H](C%11=CC=C(C(SC=N%12)=C%12C)C=C%11)C)=O)=O)=C9)CC8)=C5)[C@H]4C3
Biological Activity: A947 is a VHL-based SMARCA2 PROTAC degrader with a DC50 of 39 pM and a Kd of 93 nM for human SMARCA2. A947 recruits SMARCA2 to the VHL E3 ubiquitin ligase for ubiquitination modification, mediates its degradation via the proteasome, and exerts selective degradation effects on SMARCA4 and PBRM1. A947 induces G1 cell cycle arrest, inhibits transcription, and exerts growth inhibitory effects in SMARCA4G12C-mutant cancer cells. A947 acts synergistically with MCL1 inhibitors to induce apoptosis in SMARCA4G12C-mutant cancer cells. A947 can be used in studies related to SMARCA4G12C-mutant non-small cell lung cancer and non-small cell lung cancer[1][2].
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A947 | A947 is a VHL-based SMARCA2 PROTAC degrader with a DC50 of 39 pM and a Kd of 93 nM for human SMARCA2. A947 recruits SMARCA2 to the VHL E3 ubiquitin ligase for ubiquitination modification, mediates its degradation via the proteasome, and exerts selective degradation effects on SMARCA4 and PBRM1. A947 induces G1 cell cycle arrest, inhibits transcription, and exerts growth inhibitory effects in SMARCA4G12C-mutant cancer cells. A947 acts synergistically with MCL1 inhibitors to induce apoptosis in SMARCA4G12C-mutant cancer cells. A947 can be used in studies related to SMARCA4G12C-mutant non-small cell lung cancer and non-small cell lung cancer. | |||||||||||||||||||||
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- [1]. Cantley J, et al. Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers. Nature communications. 2022 Nov 10;13(1):6814. [Content Brief]
- [2]. Zhang D, et al. Tissue distribution and retention drives efficacy of rapidly clearing VHL-based PROTACs. Communications medicine. 2024 May 16;4(1):87. [Content Brief]
Keywords
