481704-21-6

• 常用中文名：反式-4-羟基-L-脯氨酸甲酯盐酸盐
• 常用英文名：tans-4-Hydroxy-D-proline methyl ester hydrochloride
• CAS号：481704-21-6
• 分子式：C₆H₁₂ClNO₃
• 分子量：181.617
• 相关类别： 生物化工 氨基酸及其衍生物 脯氨酸类衍生物
• 发布时间：2018-12-24 16:59:11
• 更新时间：2026-08-24 11:07:47
• tans-4-羟基-D-脯氨酸甲酯盐酸盐是一种不可切割的ADC连接物,用于合成抗体药物结合物(ADC)。tans-4-羟基-D-脯氨酸甲酯盐酸盐也是一种基于烷基链的PROTAC连接剂,可用于合成PROTAC[1][2]。

名称

• 中文名: 反式-4-羟基-L-脯氨酸甲酯盐酸盐
• 英文名: (2R,4S)-Methyl 4-hydroxypyrrolidine-2-carboxylatehydrochloride
• 中文别名: 反式-4-羟基-D-脯氨酸甲酯盐酸盐; 反式4羟基D脯胺酸甲酯盐酸盐; (2S,4R)-4-甲基环戊-2-烯甲酸甲酯盐酸盐; (S)-4-羟基-D-脯氨酸甲酯盐酸盐; 反式-4-羟基-D-脯胺酸甲酯盐酸盐; (2R,4S)-4-羟基吡咯烷-2-羧酸甲酯盐酸盐; (2R,4S)-4-羟基吡咯烷-2-甲酸甲酯盐酸盐; (2S,4R)-甲基-4-羟基吡咯烷-2-羧酸盐盐酸盐; (2S,4R)-甲基 4-羟基吡咯烷-2-羧酸盐酸盐; (4S)-4-羟基-D-脯氨酸甲酯盐酸盐
• 英文别名: (2R,4S)-methyl 4-hydroxypyrrolidine-2-cboxylate hydrochloride H-Hyp-OMe.HCl; Methyl (4R)-4-hydroxy-L-prolinate hydrochloride (1:1); Trans-4-HYDROXY-D-PROLINE METHYL ESTER; (2R,4S)-trans-4-hydroxy-D-proline methyl ester hydrochloride; (2S,4R)-Methyl 4-hydro×ypyrrolidine-2-cbo×ylate hydrochloride; L-Proline, 4-hydroxy-, methyl ester, (4R)-, hydrochloride (1:1); TRANS-4-HYDROXY-D-PROLINE METHYL ESTER HYDROCHLORIDE; 4-hydroxy-1-Methylpyrrolidine-2-cboxylate hydrochloride; (2S,4R)-methyl 4-hydroxypyrrolidine-2-cboxylate hydrochlorid; l-hydroxy-2-oxopentane; (4S)-D-Proline-4-hydroxyMethylester hydrochloride; (2S,4R)-methyl 4-hydroxypyrrolidine-2-cboxylate hydrochloride //BP; (2R,4S)-methyl 4-hydroxypyrrolidine-2-cboxylate Hydrochloride/Trans-4-HYDROXY-D-PROLINE METHYL ESTER Hydrochloride; D-Proline, 4-hydroxy-, Methyl ester, hydrochloride (1:1), (4S); Methyl (2R,4S)-4-hydroxypyrrolidine-2-cboxylate hydrochloride; (S)-4-HYDROXY-D-PROLINE METHYL ESTER HCL; trans-4-Hydroxy-D-proline methyl ester hydrochloride, (2R,4S)-4-Hydroxy-2-(methoxycbonyl)pyrrolidine hydrochloride; D-Proline-4-hydroxyMethylester hydrochloride (4S); Trans-4-hydroxy-L-proline methyl ester hydrochloride; 1-Hydroxy-pentan-2-on; 1-hydroxy-pentan-2-one; Hydroxymethyl-propyl-keton; 1-Hydroxy-2-pentanone; (2R,4S); tans-4-Hydroxy-D-proline methyl ester (hydrochloride); 2-Pentanone,1-hydroxy; 4S-hydroxy-1-pyrrolidine-2R-carboxylic acid methyl ester hydrochloride salt; 1-hydroxy-2-oxopentane; (S)-4-Hydroxy-D-proline Methyl Ester Hydrochloride; (4S)-4-Hydroxy-D-proline Methyl ester hydrochloride; H-D-Hyp-OMe.HCl; (4S)-4-hydroxy-D-Proline methyl ester hydrochloride (1:1); L-hydroxyproline methyl ester hydrochloride; rans-4-Hydroxy-D-proline methyl ester hydrochloride; (2S,4R)-4-Hydroxy-2-(methoxycbonyl)pyrrolidinium chloride; H-D-trans-Hyp-OMe.HCl

物化性质

• 分子式: C₆H₁₂ClNO₃
• 分子量: 181.617
• 精确质量: 181.050568
• PSA: 58.56000
• LogP: 0.01300
• 储存条件: 室温

生物活性

• 描述: tans-4-羟基-D-脯氨酸甲酯盐酸盐是一种不可切割的ADC连接物,用于合成抗体药物结合物(ADC)。tans-4-羟基-D-脯氨酸甲酯盐酸盐也是一种基于烷基链的PROTAC连接剂,可用于合成PROTAC[1][2]。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> 抗体- 药物偶联物 >> ADC连接器
  信号通路 >> 蛋白裂解靶向嵌合体 >> PROTAC Linker
• 靶点:

  Non-cleavable

• 体外研究: ADC由抗体组成,抗体通过ADC连接体连接ADC细胞毒素[1]。PROTAC包含两个不同的配体,通过连接体连接；一个是E3泛素连接酶的配体,另一个是靶蛋白的配体。PROTAC利用细胞内泛素-蛋白酶体系统选择性降解目标蛋白质[2]。
• 参考文献:

  [1]. Beck A, et al. Strategies and challenges for the next generation of antibody-drug conjugates. Nat Rev Drug Discov. 2017;16(5):315-337.

  [2]. Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-985.

合成路线

3398-22-9 ~85% 481704-21-6

文献：WO2003/104249 A1, ; Page 14 ;

647857-51-0 ~% 481704-21-6

文献：WO2004/7444 A2, ; Page 141 ;

67-56-1 142347-81-7 ~% 481704-21-6

文献：WO2013/49164 A1, ; Paragraph 838-839 ;

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