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  3. ARV-110

ARV-110 

Cat. No.: HY-138641
Handling Instructions

ARV-110 is an orally active, specific androgen receptor (AR) PROTAC degrader. ARV-110 promotes ubiquitination and degradation of AR. ARV-110 can be used for the research of prostate cancer.

For research use only. We do not sell to patients.

ARV-110 Chemical Structure

ARV-110 Chemical Structure

CAS No. : 2222112-77-6

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Description

ARV-110 is an orally active, specific androgen receptor (AR) PROTAC degrader. ARV-110 promotes ubiquitination and degradation of AR. ARV-110 can be used for the research of prostate cancer[1].

In Vitro

ARV-110 completely degrades AR in all cell lines tested, with an observed 50% degradation concentration (DC50) < 1 nM[1].
ARV-110 (0.01 nM-300 nM) leads to AR degradation in LNCaP cells in a dose-dependent manner[1].
ARV-110 (10 nM; 0.5-24 hours) leads to AR degradation in VCaP cells in a time-dependent manner[2].
ARV-110 (10-1000 nM) suppresses the expression of the AR-target gene PSA, inhibits AR-dependent cell proliferation, and induces apoptosis at low nanomolar concentrations[2].
ARV-110 (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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

ARV-110 (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, ARV-110 also exhibits significant inhibition of tumor growth and AR signaling[2].
ARV-110 (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

812.29

Formula

C₄₁H₄₃ClFN₉O₆

CAS No.
SMILES

O=C(C1=NN=C(N2CCC(CN3CCN(C4=CC5=C(C(N(C(CC6)C(NC6=O)=O)C5=O)=O)C=C4F)CC3)CC2)C=C1)N[[email protected]]7CC[[email protected]](OC8=CC=C(C#N)C(Cl)=C8)CC7

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

References

Purity: 99.64%

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Keywords:

ARV-110ARV110ARV 110Androgen Receptorandrogenreceptorprostatecancermetastaticcastration-resistant prostate cancerInhibitorinhibitorinhibit

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ARV-110
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