ARV-110 free base · Synonyms: Bavdegalutamide
ARV-110 (Bavdegalutamide) is an orally bioavailable, specific androgen receptor (AR) PROTAC degrader that leads to ubiquitination and degradation of…
For research use only. Not for human or veterinary use.
ARV-110 structure
CAS No.: 2222112-77-6
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 1 g | USD 380.00 | BP-01988-1g | In stock | Get quote |
| 5 g | USD 1,180.00 | BP-01988-5g | In stock | Get quote |
| 10 g | Inquire | BP-01988-10g | In stock | Inquire |
Need another size or custom synthesis? Request a quote.
Description
ARV-110 (Bavdegalutamide) is an orally bioavailable, specific androgen receptor (AR) PROTAC degrader that leads to ubiquitination and degradation of AR.
Biological activity
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.
Identifiers
- 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[C@H]7CC[C@H](OC8=CC=C(C#N)C(Cl)=C8)CC7 - InChIKey
-
CLCTZVRHDOAUGJ-SYVGMNBRSA-N
Specifications
- MW (average)
- 812.2880
- Formula
- C41H43ClFN9O6
- CAS No.
- 2222112-77-6
- Physical state
- Solid
- Color
- Light yellow to yellow
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20°C, sealed storage, away from moisture; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO 26.67 mg/mL