ChemicalBook >?? ???? >ARV-771
ARV-771
|
|
ARV-771 ??
- ??
- 1.39±0.1 g/cm3(Predicted)
- ?? ??
- Sealed in dry,Store in freezer, under -20°C
- ???
- DMSO:65.92(Max Conc. mg/mL);68.22(Max Conc. mM)
DMF:20.0(Max Conc. mg/mL);20.7(Max Conc. mM)
DMF:PBS (pH 7.2) (1:6):0.14(Max Conc. mg/mL);0.14(Max Conc. mM)
Ethanol:55.0(Max Conc. mg/mL);56.92(Max Conc. mM)
- ??? ??
- ??? ??
- ?? ?? (pKa)
- 13.61±0.46(Predicted)
- ??
- White to light yellow
- InChIKey
- PQOGZKGXGLHDGS-BZTQNJCZNA-N
??
- ?? ? ?? ??
- ?? ? ???? ?? (GHS)
| ????(GHS): |
|
|||||||||||||||||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| ?? ?: | Warning | |||||||||||||||||||||||||||||||||||
| ??·?? ??: |
|
|||||||||||||||||||||||||||||||||||
| ??????: |
|
ARV-771 C??? ??, ??, ??
Biological Functions
ARV-771, a von Hippel–Landau (VHL) E3 ligase-based BET PROTAC, is highly active against cellular models of CRPC. ARV-771 in these cells results in rapid BET protein degradation with DC50 (the drug concentration that results in 50% protein degradation) values <1 nM. Interestingly, ARV–771–mediated BET degradation leads to decreased both FL-AR and AR-V7 at the transcript level. In contrast, treating CRPC cells with BET inhibitors leads to the suppression of AR-V7 but not of FL-AR levels. Moreover, ARV-771 causes significantly greater apoptotic cell death than a BET inhibitor. ARV-771 dramatically suppresses the proliferation of castration-resistant prostate cancer models via inducing Von Hippel Lindau (VHL) E3 ligase-mediated degradation of BRDs and inhibiting AR signaling. A subsequent study has demonstrated that ARV-771 can also suppress the proliferation of mantle cell lymphoma cells via increasing the levels of tumour suppressors, including CDKN1A/p21, HEXIM1, and NOXA[1].?? ??
[1] Yuanfei Deng. “ARV-771 Acts as an Inducer of Cell Cycle Arrest and Apoptosis to Suppress Hepatocellular Carcinoma Progression.” Frontiers in Pharmacology (2022).ARV-771 ?? ?? ? ???
???
?? ??
ARV-771 ?? ??
???( 97)?? ??
| ??? | ?? | ??? | ?? | ?? ? | ?? |
|---|---|---|---|---|---|
| Hubei Chuchang Biotech Co., Ltd. | +undefined15623860702 |
info@chuchangbiotech.com | China | 202 | 58 |
| Shanghai finete Pharmaceutical Co., Ltd. | +86-18221039705 |
CHINA | 139 | 55 | |
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 |
ivan@atkchemical.com | China | 32965 | 60 |
| BOC Sciences | +1-631-485-4226 |
inquiry@bocsci.com | United States | 19553 | 58 |
| Zhengzhou Alfa Chemical Co.,Ltd | +8618530059196 |
sale04@alfachem.cn | China | 11915 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 |
marketing@targetmol.com | United States | 32161 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 +8613203830695 |
laboratory@coreychem.com | China | 30233 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 |
sales@hzclap.com | CHINA | 6312 | 58 |
| Wuhan Fortuna Chemical Co., Ltd | +86-027-59207850 |
info@fortunachem.com | China | 5972 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 |
sales@sarms4muscle.com | China | 10473 | 58 |