
ARV-110
CAS No. 2222112-77-6
ARV-110( —— )
Catalog No. M24006 CAS No. 2222112-77-6
ARV-110 is an oral degrader of androgen receptor PROTAC for prostate cancer treatment.
Purity : >98% (HPLC)






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Biological Information
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Product NameARV-110
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NoteResearch use only, not for human use.
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Brief DescriptionARV-110 is an oral degrader of androgen receptor PROTAC for prostate cancer treatment.
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DescriptionARV-110 is an oral degrader of androgen receptor PROTAC for prostate cancer treatment.
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In VitroBavdegalutamide completely degrades AR in all cell lines tested, with an observed 50% degradation concentration (DC50) < 1 nM.Bavdegalutamide (0.01 nM-300 nM) leads to AR degradation in LNCaP cells in a dose-dependent manner.Bavdegalutamide (10 nM; 0.5-24 hours) leads to AR degradation in VCaP cells in a time-dependent manner.Bavdegalutamide (10-1000 nM) suppresses the expression of the AR-target gene PSA, inhibits AR-dependent cell proliferation, and induces apoptosis at low nanomolar concentrations.Bavdegalutamide (0.01 nM-100 nM) degrades clinically relevant mutant AR proteins (WT AR, F876L, T877A, M896V and H874V), and retains activity in a high androgen environment (R1881, 100 nM) in VCaP cells.
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In VivoBavdegalutamide (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.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.
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Synonyms——
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PathwayEndocrinology/Hormones
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TargetAndrogen Receptor (AR)
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RecptorAndrogen Receptor
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Research Area——
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Indication——
Chemical Information
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CAS Number2222112-77-6
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Formula Weight812.29
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Molecular FormulaC41H43ClFN9O6
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Purity>98% (HPLC)
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SolubilityDMSO:46 mg/mL (56.63 mM; Need ultrasonic)
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SMILESClC1=CC(O[C@H]2CC[C@@H](CC2)NC(C3=CC=C(N=N3)N4CCC(CC4)CN5CCN(CC5)C6=CC(C(N7C8CCC(NC8=O)=O)=O)=C(C=C6F)C7=O)=O)=CC=C1C#N
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Taavi K Neklesa,et al. ARV-110: an oral androgen receptor PROTAC degrader for prostate cancer. GU ASCO 2019
molnova catalog



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