1489236-55-6
Chemical Structure
SARD279
- CAS No.: 1489236-55-6
- Formula:C33H41F3N4O5S
- Molecular Weight:662.76
InChIKey: NUYCVTGYOUGRSO-XNDQHBPLSA-N
SMILES: O=C(OCCOCCNC(CCCN(C1(C)C)C(N(C(C=C2)=CC(C(F)(F)F)=C2C#N)C1=O)=S)=O)CC3(C[C@H](C4)C5)C[C@H]5C[C@H]4C3
Biological Activity: SARD279 is a HyT degrader of androgen receptor (AR). SARD279 binds to AR, recruits HSP70, mediates ubiquitin-dependent proteasomal degradation, and competitively inhibits the transactivation of AR. SARD279 exhibits antiproliferative activity in AR-dependent prostate cancer cells and castration-resistant prostate cancer cells, including those harboring the ARF876L mutation. SARD279 can be used in studies related to prostate cancer and castration-resistant prostate cancer[1][2][3][4][5].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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SARD279 | 96.04% | SARD279 is a HyT degrader of androgen receptor (AR). SARD279 binds to AR, recruits HSP70, mediates ubiquitin-dependent proteasomal degradation, and competitively inhibits the transactivation of AR. SARD279 exhibits antiproliferative activity in AR-dependent prostate cancer cells and castration-resistant prostate cancer cells, including those harboring the ARF876L mutation. SARD279 can be used in studies related to prostate cancer and castration-resistant prostate cancer. | ||||||||||||||||||||
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References
- [1]. Salami J, et al. Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellular models of prostate cancer drug resistance. Communications biology. 2018;1:100. [Content Brief]
- [2]. Collins I, et al. Chemical approaches to targeted protein degradation through modulation of the ubiquitin-proteasome pathway. The Biochemical journal. 2017 Mar 15;474(7):1127-1147. [Content Brief]
- [3]. Xie S, et al. Small-Molecule Hydrophobic Tagging: A Promising Strategy of Druglike Technology for Targeted Protein Degradation. Journal of medicinal chemistry. 2023 Aug 24;66(16):10917-10933. [Content Brief]
- [4]. Chen J, et al. Enhanced protein degradation by intracellular delivery of pre-fused PROTACs using lipid-like nanoparticles. Journal of controlled release : official journal of the Controlled Release Society. 2021 Feb 10;330:1244-1249. [Content Brief]
- [5]. Gustafson JL, et al. Small-Molecule-Mediated Degradation of the Androgen Receptor through Hydrophobic Tagging. Angewandte Chemie (International ed. in English). 2015 Aug 10;54(33):9659-62. [Content Brief]
