ARV110
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-cyanophenox y)cyclohexyl)-6-(4-((4-(2-(2,6-dioxopip eridin-3-yl)-6-fluoro-1,3-dioxoisoindoli n-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
- 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
ARV110 Usage And Synthesis
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
ARV110Supplier
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