HazMat Fee + There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
| Type | HazMat fee for 500 gram (Estimated) |
| Excepted Quantity | USD 0.00 |
| Limited Quantity | USD 15-60 |
| Inaccessible (Haz class 6.1), Domestic | USD 80+ |
| Inaccessible (Haz class 6.1), International | USD 150+ |
| Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
| Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |


| 规格 | 价格 | 会员价 | 库存 | 数量 | |||
|---|---|---|---|---|---|---|---|
| {[ item.pr_size ]} |
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{[ getRatePriceInt(item.pr_rmb, 1,1) ]} {[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} |
{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]} | 现货 | 1周 咨询 | - + |
快速发货 顺丰冷链运输,1-2 天到达
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| 产品名称 | Androgen Receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Cyproterone acetate |
++++
Androgen Receptor, IC50: 7.1 nM |
98% | |||||||||||||||||
| Apalutamide |
+++
Androgen Receptor, IC50: 16 nM |
98% | |||||||||||||||||
| AZD3514 |
+
Androgen Receptor, Ki: 2.2 μM |
99% | |||||||||||||||||
| Darolutamide |
++++
Androgen receptor, Ki: 11 nM |
98% | |||||||||||||||||
| Flutamide |
+++
Androgen Receptor, Ki: 55 nM |
98% | |||||||||||||||||
| Galeterone |
++
Androgen Receptor, IC50: 384 nM |
98% | |||||||||||||||||
| Enzalutamide |
+++
Androgen Receptor, IC50: 36 nM |
98% | |||||||||||||||||
| Megestrol | ✔ | 98% | |||||||||||||||||
| Spironolactone |
++
Androgen Receptor, IC50: 77 nM |
98+% | |||||||||||||||||
| Bicalutamide |
++
Androgen Receptor, IC50: 0.16 μM |
99% | |||||||||||||||||
| EPI-001 |
+
Androgen Receptor, IC50: ~6 μM |
98% | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 靶点 |
|
| 描述 | The androgen receptor (AR) and the androgen-AR signaling pathway play a significant role in male sexual differentiation and the development and function of male reproductive and non-reproductive organs [7]. ARN-509 is a competitive AR inhibitor (IC50=16 nM) which is fully antagonistic to AR overexpression, a common and important feature of castration-resistant prostate cancer (CRPC). In castration-resistant LNCaP/AR cells, ARN-509 (< 10 μM; 3d) antagonized androgen-mediated induction or repression of mRNA expression-levels for 13 endogenous genes including PSA and TMPRSS2, and ARN-509 (< 10 μM) also antagonized the proliferative effect of R1881 (30pM). Following 17 days of treatment with ARN-509 (10 mg/kg/day) in a model of castration-resistant prostate cancer, androgen-driven luciferase reporter-gene activity was consistently reduced compared to vehicle, indicating AR inhibition by ARN-509 in vivo. In castrate mice bearing LNCaP/AR (cs) xenograft tumors, 8/10 ARN-509-treated (10 mg/kg/day) tumors regressed by >50% (volume) on day 28 [8]. |
| Concentration | Treated Time | Description | References | |
| Calu-3 cells | 10, 25 µM | 48 hours | To evaluate the effect of Apalutamide on SARS-CoV-2 infection, results showed that Apalutamide significantly reduced SARS-CoV-2 infection in Calu-3 cells. | Int J Mol Sci. 2023 Feb 7;24(4):3288. |
| Calu-3 cells | 1, 5, 10, 25 µM | 72 hours | To evaluate the effect of Apalutamide on TMPRSS2 protein levels, results showed a non-significant modulation of TMPRSS2 protein levels after apalutamide treatment. | Int J Mol Sci. 2023 Feb 7;24(4):3288. |
| LNCaP | 45.48 µM | 8 weeks | Establish apalutamide-resistant prostate cancer cell lines and confirm that apalutamide activates the release of calcium ions and endoplasmic reticulum stress to enhance autophagy. | J Transl Med. 2024 Jun 6;22(1):538. |
| C4-2 | 20.16 µM | 8 weeks | Establish apalutamide-resistant prostate cancer cell lines and confirm that apalutamide activates the release of calcium ions and endoplasmic reticulum stress to enhance autophagy. | J Transl Med. 2024 Jun 6;22(1):538. |
| Dose | Mice: 10 mg/kg - 100 mg/kg[3] (p.o.), 2 mg/kg[4] (p.o. or i.v.); 1 mg/kg[5] (i.v.) | |||||||||||||||||||||||||||||||||
| Administration | p.o., i.v. | |||||||||||||||||||||||||||||||||
| Pharmacokinetics |
|
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.09mL 0.42mL 0.21mL |
10.47mL 2.09mL 1.05mL |
20.95mL 4.19mL 2.09mL |
|
| CAS号 | 956104-40-8 |
| 分子式 | C21H15F4N5O2S |
| 分子量 | 477.43 |
| SMILES Code | O=C(NC)C1=CC=C(N(C(N(C2=CC(C(F)(F)F)=C(C#N)N=C2)C3=O)=S)C43CCC4)C=C1F |
| MDL No. | MFCD22380626 |
| 别名 | |
| 运输 | 蓝冰 |
| InChI Key | HJBWBFZLDZWPHF-UHFFFAOYSA-N |
| Pubchem ID | 24872560 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, room temperature |
| 溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
|
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