CAS: 2750830-09-0; 4-(4-((1-(4-((Trans-3-(4-Cyano-3-Methoxyphenoxy)-2,2,4,4-Tetramethylcyclobutyl)Carbamoyl)Phenyl)Piperidin-4-yl)Methyl)Piperazin-1-yl)-N-((S)-2,6-Dioxopiperidin-3-yl)-2-Fluorobenzamide
- 英文名称4-(4-((1-(4-((Trans-3-(4-Cyano-3-Methoxyphenoxy)-2,2,4,4-Tetramethylcyclobutyl)Carbamoyl)Phenyl)Piperidin-4-yl)Methyl)Piperazin-1-yl)-N-((S)-2,6-Dioxopiperidin-3-yl)-2-Fluorobenzamide
- 中文名称4-(4-((1-(4-(((1R,3R)-3-(4-氰基-3-甲氧基苯氧基)-2,2,4,4-四甲基环丁基)氨基甲酰基)苯基)哌啶-4-基)甲基)哌嗪-1-基)-N-((S)-2,6-二氧代哌啶-3-基)-2-氟苯甲酰胺
- IUPAC名称4-(4-((1-(4-(((1r,3r)-3-(4-cyano-3-methoxyphenoxy)-2,2,4,4-tetramethylcyclobutyl)carbamoyl)phenyl)piperidin-4-yl)methyl)piperazin-1-yl)-N-((S)-2,6-dioxopiperidin-3-yl)-2-fluorobenzamide
- CAS编号2750830-09-0
- FDA UNII编号:5BD7R933PV
- 分子式:C45H54FN7O6分子量:807.97
- 产品CID: 2202490
物理性质
- 沸点993.4±65.0 °C(预测)
- 密度1.32±0.1 g/cm3(温度: 20 °C; Press: 760 Torr)(预测)
- pKa:10.58±0.40(预测)
- LogP:5.9
- 储存条件Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
- 产品应用该化合物是新型的,强大的,口服生物可口服的PROTAC ARAR降解器.LUXDADALUTAMOIDE不仅降解野型ARA,而且降解临床相关的ARLBD变异,包括最普遍的AR L702H,H875Y和T878A变异.在体外,ARV-766降解了各种前列腺癌细胞的AR,包括隐藏抗抗性发作,临床相关点突变的细胞,野生VAP.I.A.ARTV-762还保持了抗抗抗AAR L.702H变异体的威力.在V.V.766体内,可口腔内,AR.V-7 66以观察到的抗性剂量最大降解度大于90%(DMAX).ARV/766,在野生LNCAP和VA-P.VAXA ENEST模型中,显著且剂量依赖剂量抑制性肿瘤生长,包括LNCPAXXANT模型.
MSDS等安全信息
合成工艺路线路线简述
供应商参考报价(招募中)
品牌试剂参考报价(招募中)
📌 第三方产品分析报告
主要参考文献
Zhang Y, Ming A, Wang J, Chen W, Fang Z. PROTACs targeting androgen receptor signaling: Potential therapeutic agents for castration-resistant prostate cancer. Pharmacol Res. 2024 Jul;205:107234. doi: 10.1016/j.phrs.2024.107234. Epub 2024 May 28.合成参考文献
参考文献:10.1021/acs.jmedchem.4c01017
摘要:Schade M, Scott JS, Hayhow TG, Pike A, Terstiege I, Ahlqvist M, Johansson JR, Diene CR, Fallan C, Balazs AYS, Chiarparin E, Wilson D. Structural and Physicochemical Features of Oral PROTACs. J Med Chem. 2024 Aug 08;67(15):13106–16. doi: 10.1021/acs.jmedchem.4c01017.
📝 需求与反馈
尽可能描述清楚需求与问题信息
