| 生物活性 | Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potentRARagonist, withAC50s of 2.3 nM, 9.3 nM, and 22 nM forRARβ,RARγ,RARα, respectively. Adapalene also inhibits the enzymatic activity ofGOT1in a non-competitive manner. Adapalene exhibits anti-tumor activity[1][2][3]. |
| IC50& Target | AC50: 2.3 nM (RARβ), 9.3 nM (RARγ), and 22 nM (RARα)[1] |
体外研究
(In Vitro) | Adapalene (1-200 μM; 24 h) inhibits the viability of ES-2, HOV-7, MCF-7 , Hela, SW1990, HT1080, and MM-468 cells, with IC50s of 10.36 μM, 10.81 μM, 12.00 μM, 19.08 μM, 19.52 μM, 21.70 μM, and 31.47 μM, respectively[2].
Adapalene (10-40 μM; 24 h) induces ES-2 cells apoptosis and inhibits proliferation in vitro[2].
Adapalene (3-30 μM; 6-24 h) significantly increases the G1-phase population in LoVo or DLD1 cells[3].
Adapalene (1-200 μM) inhibits GOT1 activity, with an IC50 of 21.79 μM[2].
Adapalene (10-6-10-3nM) inhibits the expression of plasma membrane-associated enzyme transglutaminase Type I, with an IC50of 2.5 nM[1].
Cell Viability Assay[2] | Cell Line: | Pancreatic cancer (SW1990, Aspc-1), breast cancer (mm-231, mm-468, MCF-7), liver cancer (Hep3B), cervical cancer (Hela), ovarian cancer (HOV-7, ES-2), normal cells (CHO, L929) | | Concentration: | 1-200 μM | | Incubation Time: | 24 hours | | Result: | Inhibited the viability of cancer cells with higher GOT1 protein expression. |
Apoptosis Analysis[2] | Cell Line: | ES-2 cells[2] | | Concentration: | 10, 20, 40 μM | | Incubation Time: | 24 hours | | Result: | Showed a significant increase in apoptosis compared with the control group.
Down regulated the expression of anti-apoptotic protein Bcl-2 and PARP. |
Cell Cycle Analysis[3] | Cell Line: | LoVo or DLD1 cells | | Concentration: | 3, 10, 30 μM | | Incubation Time: | 6, 12, 24 hours | | Result: | Caused cell cycle arrest in G1 phase in a dose- and time-dependent manner. |
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体内研究
(In Vivo) | Adapalene (15-100 mg/kg; p.o. daily for 21 days) inhibits the growth of DLD1 cell-derived xenograft tumors in BALB/C nude mice[3].
| Animal Model: | Female BALB/C nude mice (15 g, 4-5 weeks) were injected with DLD1 cells[3] | | Dosage: | 15, 20, 65, 100 mg/kg | | Administration: | P.o. daily for 21 days | | Result: | Significantly reduced tumor weight and volume. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : 10 mg/mL(24.24 mM;ultrasonic and warming and heat to 60℃) H2O :< 0.1 mg/mL(insoluble) 配制储备液 | 1 mM | 2.4241 mL | 12.1206 mL | 24.2412 mL | | 5 mM | 0.4848 mL | 2.4241 mL | 4.8482 mL | | 10 mM | 0.2424 mL | 1.2121 mL | 2.4241 mL |
*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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制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 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: 1 mg/mL (2.42 mM); Suspended solution; Need ultrasonic
此方案可获得 1 mg/mL (2.42 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 1 mg/mL (2.42 mM); Clear solution
此方案可获得 ≥ 1 mg/mL (2.42 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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