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| 描述 | Adapalene (CD271) is a third-generation synthetic retinoid commonly used in acne research. It functions as a potent agonist of retinoic acid receptors (RAR), demonstrating AC50 values of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, and RARα, respectively. Additionally, adapalene inhibits the enzymatic activity of glutamate oxaloacetate transaminase 1 (GOT1) in a non-competitive manner and has shown anti-tumor activity in various studies[1].[2].[3]. |
| 体内研究 | In vivo, adapalene at dosages of 15 to 100 mg/kg administered orally daily for 21 days inhibits the growth of DLD1 cell-derived xenograft tumors in BALB/C nude mice, highlighting its potential for clinical use in cancer therapy[3]. |
| 体外研究 | In cell viability assays, adapalene impacts several cancer cell lines, reducing the viability of ES-2, HOV-7, MCF-7, Hela, SW1990, HT1080, and MM-468 cells. The IC50 values range from 10.36 μM for ES-2 cells to 31.47 μM for MM-468 cells over a 24-hour treatment period at concentrations between 1 and 200 μM[2]. In further experiments, adapalene at 10-40 μM induces apoptosis and inhibits the proliferation of ES-2 cells in vitro[2]. Adapalene also affects cell cycle distribution, significantly increasing the G1-phase population in LoVo and DLD1 cells when applied in concentrations ranging from 3 to 30 μM over periods of 6 to 24 hours[3]. Additionally, adapalene demonstrates inhibition of GOT1 activity with an IC50 of 21.79 μM[2]. Otherwise, Adapalene also effectively suppresses the expression of transglutaminase Type I, a plasma membrane-associated enzyme, with an IC50 of 2.5 nM at concentrations from 10-6 -10-3 nM[1]. |
| Concentration | Treated Time | Description | References | |
| DLD1 human colon cancer cells | 1, 3, 10, 30 µM | 6, 12, 24, 48, 72 hours | Evaluate the effect of Adapalene on the viability of DLD1 cells, results showed Adapalene significantly inhibited cell proliferation with IC50 of 4.43 µM | Mol Med Rep. 2015 Nov;12(5):6501-8. |
| LoVo human colon cancer cells | 1, 3, 10, 30 µM | 6, 12, 24, 48, 72 hours | Evaluate the effect of Adapalene on the viability of LoVo cells, results showed Adapalene significantly inhibited cell proliferation with IC50 of 7.135 µM | Mol Med Rep. 2015 Nov;12(5):6501-8. |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | HCC tumor model | Oral | 10 mg/kg | Twice administration | ADA treatment significantly reduced tumor formation and tumor growth, and increased the survival rate of snord88b KO mice | Nat Commun. 2024 Aug 7;15(1):6730 |
| BALB/C nude mice | DLD1 human colon cancer xenograft model | Oral | 15, 20, 65, 100 mg/kg | Once daily for 21 days | Evaluate the effect of Adapalene on DLD1 xenograft tumor growth, results showed Adapalene significantly inhibited tumor growth, with 20 mg/kg dose comparable to oxaliplatin 40 mg/kg | Mol Med Rep. 2015 Nov;12(5):6501-8. |
| Dose | Pregnant rat: 0.1 mg/kg, 1 mg/kg[3] (p.o.) |
| Administration | p.o. |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02731105 | Acne Vulgaris | Phase 4 | Completed | - | Germany ... 展开 >> Universitätsklinikum Carl Gustav Carus; Klinik und Poliklinik für Dermatologie Dresden, Saxony, Germany, 01307 收起 << |
| NCT02620813 | Acne Vulgaris | Phase 4 | Recruiting | May 2019 | United States, California ... 展开 >> Dermatology Research Area Recruiting Davis, California, United States, 95616 Contact: Negar Foolad, MAS 916-734-1509 nfoolad@ucdavis.edu Contact: Lauren A Hassoun, BS 916-734-6550 lahassoun@ucdavis.edu Principal Investigator: Raja K Sivamani, MD UC Davis Department of Dermatology Recruiting Sacramento, California, United States, 95816 Contact: Raja Sivamani, MD rajasivamani@gmail.com 收起 << |
| NCT02442817 | Schizophrenia | Phase 4 | Unknown | May 2017 | United States, Nevada ... 展开 >> University of Nevada School of Medicine Recruiting Reno, Nevada, United States, 89503 Contact: Brian Kirkpatrick, MD 775-682-8449 bkirkpatrick@medicine.nevada.edu Principal Investigator: Brian Kirkpatrick, MD 收起 << |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.42mL 0.48mL 0.24mL |
12.12mL 2.42mL 1.21mL |
24.24mL 4.85mL 2.42mL |
|
| CAS号 | 106685-40-9 |
| 分子式 | C28H28O3 |
| 分子量 | 412.52 |
| SMILES Code | C4=C(C12CC3CC(C1)CC(C2)C3)C(=CC=C4C6=CC5=CC=C(C=C5C=C6)C(O)=O)OC |
| MDL No. | MFCD03106112 |
| 别名 | CD271 |
| 运输 | 蓝冰 |
| InChI Key | LZCDAPDGXCYOEH-UHFFFAOYSA-N |
| Pubchem ID | 60164 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 9 mg/mL(21.82 mM),配合低频超声,并水浴加热至45℃助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 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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