2416716-62-4

2416716-62-4 structure
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: 2025-08-28 17:57:15
  • 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

[1]. Han-Jie Zhou, et al. Androgen receptor modulators and methods for their use. Patent. US20200123117A1.

Molecular Formula C24H24Cl2N4O4S
Molecular Weight 535.44
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