ARV110 CAS 2222112-77-6
Introduction：Basic information about ARV110 CAS 2222112-77-6, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
ARV110 Basic information
| Product Name: | ARV110 |
| Synonyms: | 3-Pyridazinecarboxamide, N-[trans-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-[[4-[2-(2,6-dioxo-3-piperidinyl)-6-fluoro-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-1-piperazinyl]methyl]-1-piperidinyl]-;ARV-110;N-((1R,4R)-4-(3-chloro-4-cyanophenoxy)cyclohexyl)-6-(4-((4-(2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxoisoindolin-5-yl)piperazin-1-yl)methyl)piperidin-1 -yl)pyridazine-3-carboxamide;N-(trans-4-(3-Chloro-4-cyanophenoxy)cyclohexyl)-6-(4-((4-(2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxoisoindolin-5-yl)piperazin-1-yl)methyl)piperidin-1-yl)pyridazine-3-carboxamide;Bavdegalutamide;Bavdegalutamide (ARV-110);3-Pyridazinecarboxamide, N-[trans-4-(3-chloro-4-cyanophenoxy)cyclohexyl]...;prostate,castration-resistant prostate cancer,receptor,ARV 110,androgen,Bavdegalutamide,Androgen Receptor,inhibit,cancer,ARV110,Inhibitor,metastatic |
| CAS: | 2222112-77-6 |
| MF: | C41H43ClFN9O6 |
| MW: | 812.29 |
| EINECS: | |
| Product Categories: | |
| Mol File: | 2222112-77-6.mol |
ARV110 Chemical Properties
| Boiling point | 1074.1±65.0 °C(Predicted) |
| density | 1.49±0.1 g/cm3(Predicted) |
| storage temp. | Store at-20°C, away from moisture |
| solubility | DMSO : 26.67 mg/mL (32.83 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 80°C) |
| pka | 10.59±0.40(Predicted) |
| form | Solid |
| color | Light yellow to yellow |
| InChIKey | CLCTZVRHDOAUGJ-SYVGMNBRSA-N |
| SMILES | C1(C(N[C@@H]2CC[C@@H](OC3=CC=C(C#N)C(Cl)=C3)CC2)=O)=NN=C(N2CCC(CN3CCN(C4C(F)=CC5=C(C=4)C(=O)N(C4CCC(=O)NC4=O)C5=O)CC3)CC2)C=C1 |
Safety Information
| Description | ARV-110 is an androgen receptor PROTAC degrader. It promotes ubiquitination and degradation of the androgen receptor. |
| Characteristics | ARV-110 is a PROteolysis TArgeting Chimera (PROTAC) protein degrader that recruits the cereblon-containing E3 ubiquitin ligase to direct the polyubiquitination and subsequent proteasomal degradation of AR. It selectively degrades wild-type AR and most clinically relevant mutants with low nanomolar potency. |
| Uses | Bavdegalutamide (ARV-110) is an orally active, specific androgen receptor (AR) PROTAC degrader. Bavdegalutamide promotes ubiquitination and degradation of AR. Bavdegalutamide can be used for the research of prostate cancer (Pink: AR ligand (HY-168299); Blue: E3 ligase ligand (HY-W093272); Black: linker (HY-W091986))[1]. |
| in vivo | Bavdegalutamide (oral gavage; 1 mg/kg; QD) exhibits a greater than 90% AR degradation in vivo. In LNCaP, VCaP and prostate cancer patient derived xenograft (PDX) models, Bavdegalutamide also exhibits significant inhibition of tumor growth and AR signaling[2].Bavdegalutamide (oral gavage; 3 or 10 mpk; 30 days) demonstrates in vivo efficacy and reduction of AR-target gene expression in a long term, castrate, enzalutamide-resistant VCaP tumor model. The TGI are 70% and 60% for 3 mpk and 10 mpk dosage. Respectively[2]. |
| References | [1] Taavi Neklesa, et al. ARV-110: An androgen receptor PROTAC degrader for prostate cancer. American Association for Cancer Research. 2018. 78 (13): pp. 5236. [2] Taavi K Neklesa,et al. ARV-110: an oral androgen receptor PROTAC degrader for prostate cancer. GU ASCO 2019 |
ARV110 Preparation Products And Raw materials
