1. Vitamin D Related/Nuclear Receptor
  2. Androgen Receptor
  3. RD162

RD162 是一种二芳基硫代乙内酰脲,一种口服有效的非甾体抗雄激素 (NSAA)。RD162 与雄激素受体 (AR) 特异性结合。RD162 在去势抵抗人前列腺癌小鼠模型中诱导肿瘤消退。

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RD162 Chemical Structure

RD162 Chemical Structure

CAS No. : 915087-27-3

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5 mg ¥1500
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50 mg ¥8000
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RD162, a diarylthiohydantoin, is an orally active non-steroidal antiandrogen (NSAA). RD162 specifically binds to androgen receptor (AR). RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer[1].

体外研究
(In Vitro)

RD162 (1-10 μM; 4 days) suppresses growth and induces apoptosis in the human prostate cancer cell line VCaP which has endogenous AR gene amplification[1].
RD162 has little to no binding to the progesterone, estrogen or glucocorticoid receptors in an in vitro fluorescence polarization assay[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: VCaP cells
Concentration: 1, 10 μM
Incubation Time: 4 days
Result: Suppressed cell growth.
体内研究
(In Vivo)

RD162 (10 mg/kg; oral gavage; daily; for 28 days) causes all tumors regressed[1].
RD162 (0.1, 1, 10 mg/kg; oral gavage; daily; for 5 days) consistently reduces luciferase activity with 10 mg/kg/day human LNCaP/AR xenografts grown in castrated male mice whereas lower doses of 0.1 and 1.0 mg/kg/day has minimal effect. RD162 substantially reduces cellular proliferation after 5 days[1].
RD162 (20 mg/kg; gavage) is ∼50 percent bioavailable after oral delivery with a serum half-life of about 30 hours[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Castrate male mice bearing LNCaP/AR xenografts[1]
Dosage: 10 mg/kg
Administration: Oral gavage; daily; for 28 days
Result: Caused all tumors regressed.
Animal Model: Male mice[1]
Dosage: 20 mg/kg (Pharmacokinetic Analysis)
Administration: Oral gavage (in 0.5% hydroxy-methyl-propyl-cellulose)
Result: Had ∼50 percent bioavailable after oral delivery with a serum half-life of about 30 hours.
分子量

476.45

Formula

C22H16F4N4O2S

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO 中的溶解度 : 125 mg/mL (262.36 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0989 mL 10.4943 mL 20.9886 mL
5 mM 0.4198 mL 2.0989 mL 4.1977 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0989 mL 10.4943 mL 20.9886 mL 52.4714 mL
5 mM 0.4198 mL 2.0989 mL 4.1977 mL 10.4943 mL
10 mM 0.2099 mL 1.0494 mL 2.0989 mL 5.2471 mL
15 mM 0.1399 mL 0.6996 mL 1.3992 mL 3.4981 mL
20 mM 0.1049 mL 0.5247 mL 1.0494 mL 2.6236 mL
25 mM 0.0840 mL 0.4198 mL 0.8395 mL 2.0989 mL
30 mM 0.0700 mL 0.3498 mL 0.6996 mL 1.7490 mL
40 mM 0.0525 mL 0.2624 mL 0.5247 mL 1.3118 mL
50 mM 0.0420 mL 0.2099 mL 0.4198 mL 1.0494 mL
60 mM 0.0350 mL 0.1749 mL 0.3498 mL 0.8745 mL
80 mM 0.0262 mL 0.1312 mL 0.2624 mL 0.6559 mL
100 mM 0.0210 mL 0.1049 mL 0.2099 mL 0.5247 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

产品名称:
RD162
目录号:
HY-111145
需求量: