Powder: -20°C for 3 years | In solvent: -80°C for 1 year
JNJ-63576253 free base (TRC253) 是具有口服活性的、有效的雄激素受体的完全拮抗剂,在 LNCaP 细胞中对 F877L 突变型 AR 和野生型 AR 的 IC50值分别为 37 和 54 nM。它可用于研究去势抵抗性前列腺癌 (CRPC) 。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 382 | 现货 | ||
2 mg | ¥ 548 | 现货 | ||
5 mg | ¥ 783 | 现货 | ||
10 mg | ¥ 1,330 | 现货 | ||
25 mg | ¥ 2,730 | 现货 | ||
50 mg | ¥ 3,970 | 现货 | ||
100 mg | ¥ 5,790 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,130 | 现货 |
产品描述 | JNJ-63576253 free base (TRC253) is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 can be used for the research of castration-resistant prostate cancer (CRPC). |
靶点活性 | Androgen receptor:37 nM(F877L mutant AR in LNCaP cells), Androgen receptor:54 nM(wild-type AR in LNCaP cells) |
体外活性 | JNJ-63576253 is stable in human liver microsomes, with an T1/2 of >180 min. It(0.0003-100 μM; 5 d) inhibits the growth of VCaP cells, with an IC50 of 265 nM. |
体内活性 | JNJ-63576253 (30 mg/kg;?p.o. once daily for 72 days) significantly inhibits the growth of prostate LNCaP SRα F877L tumor in mice.?JNJ-63576253 (30 mg/kg;?p.o. once daily for 10 days) inhibits the five androgen sensitive organs (ASOs) under stimulation by testosterone propionate (TP) in mice.?JNJ-63576253 (10 mg/kg;?p.o.) exhibits moderate oral bioavailability (45%), Cmax (0.66 μM) and AUClast (4.9 μg h/mL) in mice.?JNJ-63576253 (2 mg/kg;?i.v.) exhibits reasonable half-life (5.99 h), CL (15.0 mL/min/kg) and Vdss (6.11 L/kg) in mice. |
别名 | TRC253, JNJ-63576253 |
分子量 | 502.51 |
分子式 | C23H21F3N6O2S |
CAS No. | 2110426-27-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45 mg/mL (89.55 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.99 mL | 9.9501 mL | 19.9001 mL | 49.7503 mL |
5 mM | 0.398 mL | 1.99 mL | 3.98 mL | 9.9501 mL | |
10 mM | 0.199 mL | 0.995 mL | 1.99 mL | 4.975 mL | |
20 mM | 0.0995 mL | 0.4975 mL | 0.995 mL | 2.4875 mL | |
50 mM | 0.0398 mL | 0.199 mL | 0.398 mL | 0.995 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
JNJ-63576253 free base 2110426-27-0 Endocrinology/Hormones Androgen Receptor JNJ63576253 JNJ 63576253 free base resistant CRPC JNJ63576253 free base wild-type TRC253 prostate JNJ 63576253 cancer TRC-253 JNJ-63576253 TRC 253 castration androgen LNCaP Inhibitor inhibit mutant inhibitor