3026007-23-5
Chemical Structure
ERD-12310A
- CAS No.: 3026007-23-5
- Formula:C51H56N4O6
- Molecular Weight:821.01
InChIKey: YPHNRJJXIRMLCD-KYKDEUJJSA-N
SMILES: O=C(N1)[C@H](CCC1=O)N(C2=O)CC3=C2C=CC4=C3OCC45CCN(CC5)C[C@H]6COC7(CC6)CCN(CC7)C8=CC=C(C=C8)[C@H]9[C@H](CCC%10=C9C=CC(O)=C%10)C%11=CC=CC=C%11
Biological Activity: ERD-12310A is an orally active ERα PROTAC degrader, with a Ki value of 0.95 nM against human ERα and a DC50 of 47 pM for ERα in MCF-7 cells. ERD-12310A forms a ternary complex with ERα and the CRBN E3 ubiquitin ligase, thereby inducing ubiquitination and proteasomal degradation of wild-type and ESR1Y537S mutant ERα. ERD-12310A induces tumor regression in ER+ breast cancer xenografts and inhibits tumor growth in ESR1Y537S mutant breast cancer xenografts. ERD-12310A can be used in studies related to ER-positive breast cancer and ESR1-mutant breast cancer[1][2].
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ERD-12310A | ERD-12310A is an orally active ERα PROTAC degrader, with a Ki value of 0.95 nM against human ERα and a DC50 of 47 pM for ERα in MCF-7 cells. ERD-12310A forms a ternary complex with ERα and the CRBN E3 ubiquitin ligase, thereby inducing ubiquitination and proteasomal degradation of wild-type and ESR1Y537S mutant ERα. ERD-12310A induces tumor regression in ER+ breast cancer xenografts and inhibits tumor growth in ESR1Y537S mutant breast cancer xenografts. ERD-12310A can be used in studies related to ER-positive breast cancer and ESR1-mutant breast cancer. | |||||||||||||||||||||
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- [1]. Peng R, et al. Development of PROTACs targeting estrogen receptor: an emerging technique for combating endocrine resistance. RSC medicinal chemistry. 2025 Mar 19;16(3):1023-1036. [Content Brief]
- [2]. Rej RK, et al. Discovery of ERD-12310A as an Exceptionally Potent and Orally Efficacious PROTAC Degrader of Estrogen Receptor α (ERα). Journal of medicinal chemistry. 2024 Dec 12;67(23):20933-20965. [Content Brief]
Keywords
