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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 77 In Stock
5MG 125 In Stock
10MG 194 In Stock
25MG 382 In Stock
50MG 491 In Stock
100MG 707 In Stock
200MG 981 In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

Biological Information

  • Product Name
    ARV-110
  • Note
    Research use only, not for human use.
  • Brief Description
    ARV-110 is an oral degrader of androgen receptor PROTAC for prostate cancer treatment.
  • Description
    ARV-110 is an oral degrader of androgen receptor PROTAC for prostate cancer treatment.
  • In Vitro
    Bavdegalutamide 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.
  • 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.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.
  • Synonyms
    ——
  • Pathway
    Endocrinology/Hormones
  • Target
    Androgen Receptor (AR)
  • Recptor
    Androgen Receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2222112-77-6
  • Formula Weight
    812.29
  • Molecular Formula
    C41H43ClFN9O6
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO:46 mg/mL (56.63 mM; Need ultrasonic)
  • SMILES
    ClC1=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
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • 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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