2416716-62-4
2416716-62-4 structure
- Name: Androgen receptor-IN-2
- Chemical Name: Androgen receptor-IN-2
- CAS Number: 2416716-62-4
- Molecular Formula: C24H24Cl2N4O4S
- Molecular Weight: 535.44
- Catalog: Research Areas Cancer
- Create Date: 2023-02-27 16:33:34
- Modify Date: 2024-04-05 17:40:10
-
Androgen receptor-IN-2 is a potent and orally active Androgen Receptor inhibitor. Androgen receptor-IN-2 has antitumor activity against prostate cancer[1].
| Name | Androgen receptor-IN-2 |
|---|
| Description | Androgen receptor-IN-2 is a potent and orally active Androgen Receptor inhibitor. Androgen receptor-IN-2 has antitumor activity against prostate cancer[1]. |
|---|---|
| Related Catalog | |
| Target |
Androgen receptor[1] |
| In Vitro | Androgen receptor-IN-2 (compound A109, androgen-induced PSA-Luciferase assay) inhibits androgen binding to androgen receptor with an IC50 of 535 nM[1]. Androgen receptor-IN-2 inhibits cell proliferation in LNCaP and LNCaP95 cells (IC50: 0.44 μM, 3.78 μM respectively)[1]. Androgen receptor-IN-2 shows a metabolic stability in liver microsome with a t1/2 of more than 120 min, and in hepatocytes with a t1/2 of more than 360 min[1]. |
| In Vivo | Androgen receptor-IN-2 (compound A109) (60 mg/kg, p.o.) induces partial regressions of tumor growth in NCG mice bearing LNCaP tumors[1]. Androgen receptor-IN-2 (5 mg/kg, p.o., single dose, in male CD-1 mice) shows a t1/2 of 8.1 h, Cmax of 2673.3 ng/mL, F (%) of 33.6[1]. Animal Model: LNCaP Xenografts Model[1] Dosage: 60 mg/kg Administration: Oral administration (p.o.) Result: Inhibited tumor growth no obvious drug related toxicity (bodyweight change). |
| References |
| Molecular Formula | C24H24Cl2N4O4S |
|---|---|
| Molecular Weight | 535.44 |