达洛鲁胺, 雄激素受体拮抗剂

Androgen Receptor Antagonists
有货

库存信息

关闭
货号 (SKU) 包装规格 是否现货 价格 数量
D408674-1ml
1ml 现货 Stock Image
查看相关系列
Compound libraries (12332)

基本描述

英文别名 BAY-1841788 | N-((S)-1-(3-(3-chloro-4-cyanophenyl)-1H-pyrazol-1-yl)propan-2-yl)-5-(1-hydroxyethyl)-1H-pyrazole-3-carboxamide
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Darolutamide (ODM-201)
生化机理 Darolutamide(ODM-201,BAY-1841788)是一种新型雄激素受体(AR)拮抗剂,可阻断 AR 核转位,Ki值为 11 nM。第 3 阶段
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 拮抗剂
作用机制 雄激素受体拮抗剂
产品介绍


Information

Darolutamide (ODM-201) Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with K i of 11 nM. Phase 3.
In vitro

In AR-HEK293 cells stably expressing full-length hAR, ODM-201 inhibits human AR (hAR) with IC50 of 26 nM. ODM-201 inhibits VCaP cell proliferation with IC50 of 230 nM, while has no effect on the viability of AR-negative cell lines tested, DU-145 prostate cancer cells and H1581 lung cancer cells.

In vivo

In mice bearing VCaP xenografts, ODM-201 (50\u2009mg/kg, p.o.) significantly inhibits castration-resistant prostate tumor growth.
Cell Data

cell lines:

Concentrations:~10 μM

Incubation Time:4 days

Powder Purity:≥99%

产品属性

ALogP 3.034
hba_count 3
HBD Count 3
Rotatable Bond 6

关联靶点(人)

AR Tclin 雄激素受体(Androgen receptor) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Canonical SMILES CC(O)C1=CC(=N[NH]1)C(=O)NC(C)C[N]2C=CC(=N2)C3=CC(=C(C=C3)C#N)Cl
分子量 398.85
Reaxy-Rn 23068895
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=23068895&ln=

化学和物理性质

DMSO(mg / mL) Max Solubility 80
DMSO(mM) Max Solubility 200.58
Water(mg / mL) Max Solubility <1

安全和危险性(GHS)

Reaxy-Rn 23068895
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=23068895&ln=

技术规格说明书

Concentration 9-11(mmol/L)
Proton NMR spectrum Conforms to Structure

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器

Shall we send you a message when we have discounts available?

Remind me later

Thank you! Please check your email inbox to confirm.

Oops! Notifications are disabled.