Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AZD9496 是口服有效的选择性雌激素受体降解剂,是一种选择性的雌激素受体拮抗剂(IC50:0.28 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 452 | 现货 | ||
2 mg | ¥ 659 | 现货 | ||
5 mg | ¥ 1,090 | 现货 | ||
10 mg | ¥ 1,820 | 现货 | ||
25 mg | ¥ 3,730 | 现货 | ||
50 mg | ¥ 5,290 | 现货 | ||
100 mg | ¥ 7,270 | 现货 | ||
500 mg | ¥ 14,500 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,050 | 现货 |
产品描述 | AZD9496 is an orally available selective estrogen receptor(ERα) antagonist, with potential antineoplastic activity. |
靶点活性 | ERα:0.28 nM. |
体外活性 | AZD9496 showed pmol/L equipotent binding to both ERα and ERβ isoforms. AZD9496 directly targets ERα for downregulation in vitro. And it also antagonizes and downregulates mutant ER in vitro and in vivo. The IC50s of ERα binding, ERα downregulation, ERα antagonism for AZD9496 are 0.82, 0.14 and 0.28 nM, respectively[1]. |
体内活性 | AZD9496 showed high oral bioavailability across three species (F% 63, 91, and 74, rat, mouse, and dog, respectively) with generally low volume and clearance across species, albeit a higher clearance in mouse. The percent free levels in human plasma of 0.15% were 5-fold higher than those measured for fulvestrant. AZD9496 is a potent, oral inhibitor of breast tumor growth in vivo. AZD9496 causes tumor regressions in combination with PI3K pathway and CDK4/6 inhibitors and in an estrogen-deprived ER+ model of resistance. This effect was accompanied by a dose-dependent decrease in PR protein levels. AZD9496 is currently being evaluated in a phase I Clinicalal trial[1]. |
细胞实验 | Cells were grown in steroid-free conditions in SILAC media containing 13C615N4 L-arginine to label ERα peptide as "heavy" and then switched to grow in media containing unlabeled l-arginine to label newly synthesized protein as "normal" with 0.1% DMSO, 300 nmol/L tamoxifen, 100 nmol/L AZD9496, or 100 nmol/L fulvestrant for the time indicated. (Only for Reference) |
分子量 | 442.47 |
分子式 | C25H25F3N2O2 |
CAS No. | 1639042-08-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 82 mg/mL (185.3 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 82 mg/mL (185.3 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.26 mL | 11.3002 mL | 22.6004 mL | 56.501 mL |
5 mM | 0.452 mL | 2.26 mL | 4.5201 mL | 11.3002 mL | |
10 mM | 0.226 mL | 1.13 mL | 2.26 mL | 5.6501 mL | |
20 mM | 0.113 mL | 0.565 mL | 1.13 mL | 2.8251 mL | |
50 mM | 0.0452 mL | 0.226 mL | 0.452 mL | 1.13 mL | |
100 mM | 0.0226 mL | 0.113 mL | 0.226 mL | 0.565 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。
AZD9496 1639042-08-2 Endocrinology/Hormones Estrogen Receptor/ERR Estrogen/progestogen Receptor AZD 9496 AZD-9496 inhibit Inhibitor inhibitor