ARV-771

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Chemical Structure| 1949837-12-0 同义名 : -
CAS号 : 1949837-12-0
货号 : A365449
分子式 : C49H60ClN9O7S2
纯度 : 97%
分子量 : 986.64
MDL号 : MFCD30738017
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(50.68 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
动物实验配方：
生物活性
描述 ARV-771 is a PROTAC targeting on pan-BET, containing a BRD4-binding moiety (JQ-1) and a VHL-binding moiety. Treatment with ARV-771 led to an efficient degradation of BRD2, 3 and 4 in CRPC cell lines (22Rv1, VCaP, and LnCaP95 cell lines) at concentration of 4, 11 and 34nM post 16h, and achieved a superior suppression of c-MYC on mRNA level at concentration of 10nM post 16h compared with BET small molecular inhibitor JQ-1 and OTX-015. Consistent with this effect on c-MYC by ARV-771, ARV-771 caused higher levels of CRPC cell growth inhibition and cell apoptosis compared with the treatment with JQ-1, OTX-015 and enzalutamide. Unlike BET inhibitors, the attenuation of AR signaling and AR levels could also be observed after ARV-771 treatment. Administration of ARV-771, s.c., once daily demonstrated efficiency in multiple tumor xenograft models of CRPC at various doses ranging in 3-30mg/kg. ARV-766 works as a negative control of ARV-771[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.01mL

0.20mL

0.10mL

5.07mL

1.01mL

0.51mL

10.14mL

2.03mL

1.01mL
参考文献

[1]Raina K, Lu J, 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.