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(S,R,S)-AHPC-Me HCl

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Chemical Structure| 1948273-03-7 同义名 : E3 Ligase Ligand 1;VHL ligand 2 hydrochloride;(S,R,S)-AHPC-Me hydrochloride
CAS号 : 1948273-03-7
货号 : A725161
分子式 : C23H33ClN4O3S
纯度 : 99%+
分子量 : 481.051
MDL号 : MFCD30729675
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(124.73 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(207.88 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 (S,R,S)-AHPC-Me hydrochloride (VHL ligand 2 hydrochloride) is a VHL ligand derived from (S,R,S)-AHPC used to engage the von Hippel-Lindau (VHL) protein[1]. (S,R,S)-AHPC-Me hydrochloride is useful for producing ARV-771, a BET PROTAC degrader based on the von Hippel-Lindau (VHL) E3 ligase that effectively degrades BET proteins in castration-resistant prostate cancer (CRPC) cells with a DC50 <1 nM[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.08mL

0.42mL

0.21mL

10.39mL

2.08mL

1.04mL

20.79mL

4.16mL

2.08mL
参考文献

[1]WO/2017/030814A1

[2]Raina K, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9.