ARD-2128 free base · Synonyms: ARD 2128 · ARD2128
ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader.
For research use only. Not for human or veterinary use.
ARD-2128 structure
CAS No.: 2222111-87-5
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 5 mg | USD 400.00 | BP-01987-5mg | In stock | Get quote |
| 10 mg | USD 580.00 | BP-01987-10mg | In stock | Get quote |
| 25 mg | USD 898.00 | BP-01987-25mg | In stock | Get quote |
| 50 mg | USD 1,212.00 | BP-01987-50mg | In stock | Get quote |
| 100 mg | USD 1,636.00 | BP-01987-100mg | In stock | Get quote |
| 250 mg | USD 2,436.00 | BP-01987-250mg | In stock | Get quote |
| 500 mg | Inquire | BP-01987-500mg | In stock | Inquire |
| 1 g | Inquire | BP-01987-1g | In stock | Inquire |
Need another size or custom synthesis? Request a quote.
Description
ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 has the potential for the research of the prostate cance.
Biological activity
In Vitro ARD-2128 is highly potent and effective in the inhibition of cell growth in the VCaP cell line and LNCaP cell line with the IC50 values of 4 nM and 5 nM, respectively. ARD-2128 (1, 10, 100, and 1000 nM; 24 hours) effectively reduces the AR protein level by >50% at 1 nM and achieves the AR degradation of >90% at 10, 100, and 1000 nM, respectively, in VCaP cell. In Vivo ARD-2128 (20 mg/kg; p.o.; once) is effective in reducing the level of AR protein in mice after 24 hours. ARD-2128 (10-40 mg/kg; p.o.; daily for 21 days) shows antitumor activity in the VCaP xenograft model in mice. ARD-2128 (5mg/kg; p.o.) treatment shows the Cmax, AUC0-t and t1/2 values of 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively.
Identifiers
- SMILES
-
O=C(C1=CC=C(C=C1)N2CCN(CC2)CC3CCN(CC3)C4=CC5=C(C=C4)C(N(C5=O)C(C(N6)=O)CCC6=O)=O)N[C@H]7C(C)([C@@H](C7(C)C)OC8=CC=C(C(Cl)=C8)C#N)C - InChIKey
-
BWDWHHAZFQBJQL-JABICJEXSA-N
Specifications
- MW (average)
- 820.3750
- Formula
- C45H50ClN7O6
- CAS No.
- 2222111-87-5
- Physical state
- Solid
- Color
- Light yellow to green 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
- -20℃, sealed storage, away from moisture and light In solvent :-20℃, 1 month (sealed storage, away from moisture and light)
Solubility
Soluble in DMSO 100 mg/mL