[CAS NO. 2222111-87-5] ARD-2128
PRODUCTS SPECIFICATIONS [2222111-87-5]
DESCRIPTION [2222111-87-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 820.37 |
| Molecular Formula | C45H50ClN7O6 |
| SMILES | O=C(N[C@H]1C(C)(C)[C@H](OC2=CC=C(C#N)C(Cl)=C2)C1(C)C)C3=CC=C(N4CCN(CC5CCN(C6=CC7=C(C(N(C(CC8)C(NC8=O)=O)C7=O)=O)C=C6)CC5)CC4)C=C3 |
Summary
ARD-2128 is a highly potent, orally bioavailable PROTAC androgen receptor (AR) degrader. ARD-2128 effectively reduces AR protein, suppresses AR-regulated genes in tumor tissues, and inhibits growth of tumor without signs of toxicity. ARD-2128 has the potential for the research of the prostate cancer [1] .
IC50 & Target
IC50: 4 nM (VCaP), 5 μM (LNCaP) [1]
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 IC
50
values of 4 nM and 5 nM, respectively
[1]
.
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
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | VCaP cell |
| Concentration: | 1, 10, 100, and 1000 nM |
| Incubation Time: | 24 hours |
| Result: | Reduces the AR protein level and achieves the AR degradation. |
In Vivo
ARD-2128 (20 mg/kg; p.o.; once) is effective in reducing the level of AR protein in mice after 24 hours
[1]
.
ARD-2128 (10-40 mg/kg; p.o.; daily for 21 days) shows antitumor activity in the VCaP xenograft model in mice
[1]
.
ARD-2128 (5mg/kg; p.o.) treatment shows the C
max
, AUC
0-t
and t
1/2
values of 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | SCID mice [1] |
| Dosage: | 20 mg/kg |
| Administration: | Oral |
| Result: | Reducing the level of AR protein in mice after 24 hours. |
| Animal Model: | SCID mice [1] |
| Dosage: | 10, 20, and 40 mg/kg |
| Administration: | P.o.; daily for 21 days |
| Result: | Inhibits tumor growth by 46, 69, and 63%, respectively. |
| Animal Model: | Male ICR Mice [1] |
| Dosage: | 5 mg/kg |
| Administration: | P.o. (Pharmacokinetic Analysis) |
| Result: | The C max , AUC 0-t and t 1/2 were 1304 ng/mL, 22361 ng h/mL and 18.8 hours, respectively. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
-20°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 100 mg/mL ( 121.90 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.2190 mL | 6.0948 mL | 12.1896 mL |
| 5 mM | 0.2438 mL | 1.2190 mL | 2.4379 mL |
| 10 mM | 0.1219 mL | 0.6095 mL | 1.2190 mL |