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Chemical Structure| 1297538-32-9 同义名 : ODM-201;BAY-1841788;Nubeqa.
CAS号 : 1297538-32-9
货号 : A147162
分子式 : C19H19ClN6O2
纯度 : 98%
分子量 : 398.846
MDL号 : MFCD29472270
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(263.26 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Androgen Receptor

    Androgen receptor, Ki:11 nM
描述 The androgen receptor (AR) belongs to the steroid hormone group of nuclear receptors with the estrogen receptor (ER), glucocorticoid receptor (GR), progesterone receptor (PR), and mineralocorticoid receptor (MR). Activation of androgen receptor (AR) is crucial for prostate cancer growth[3]. ODM-201 is a potent androgen receptor inhibitor with IC50 value of 26nM. In vitro, ODM-201 inhibited the androgen-induced nuclear translocation of overexpressed AR in HS-HEK293 cells. ODM-201 inhibited VCap cell proliferation with IC50 value of 230nM. However, ODM-201 had no effect on the viability of AR-negative tested, DU-145 prostate cancer cells and H1581 lung cancer cells[1].In vivo, oral administration of ODM-201 at 50mg/kg once or twice daily for 37 days significantly inhibited tumor growth in castrated (ORX) nude mice with subcutaneous VCap tumor [1]. After 7 days of oral administration with ODM-201 at 25~100mg/kg twice daily, blood: plasma levels for ODM-201 were 1.9–3.9% in mice, suggesting that the penetrance of ODM-201 through the blood brain barrier was negligible. Phase I/II clinical trial in men with mCRPC show that ODM-201 has promising anti-tumor activity in chemotherapy-pretreated patients[4].
作用机制 ODM-201 inhibits potently androgen binding to AR and androgen-induced nuclear translocation of AR[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.51mL

0.50mL

0.25mL

12.54mL

2.51mL

1.25mL

25.07mL

5.01mL

2.51mL
参考文献

[1] Moilanen AM, Riikonen R, Oksala R, et al. Discovery of ODM-201, a new-generation androgen receptor inhibitor targeting resistance mechanisms to androgen signaling-directed prostate cancer therapies. Sci Rep. 2015;5:12007

[2]Fizazi K, Massard C, et al. Activity and safety of ODM-201 in patients with progressive metastatic castration-resistant prostate cancer (ARADES): an open-label phase 1 dose-escalation and randomised phase 2 dose expansion trial. Lancet Oncol. 2014 Aug;15(9):975-85.

[3]Tan MH, Li J, Xu HE, Melcher K, Yong EL. Androgen receptor: structure, role in prostate cancer and drug discovery. Acta Pharmacol Sin. 2015; 36(1): 3‐23

[4] Fizazi K, Albiges L, Loriot Y, et al. ODM-201: a new-generation androgen receptor inhibitor in castration-resistant prostate cancer. Expert Review of Anticancer Therapy, 2015, 15(9): 1007-1017