阿达帕林钠盐（1-200 μM；24 h）抑制 ES-2、HOV-7、MCF-7、Hela、SW1990、HT1080 和 MM-468 细胞的活力，IC50 值为 10.36 μM、10.81分别为μM和12.00。分别为 19.08、19.52、21.70、31.47 和 μM[2]。在体外，阿扎普林钠盐（10–40 μM；24 小时）可抑制 ES-2 细胞生长并诱导细胞凋亡 [2]。在 LoVo 或 DLD1 细胞中，阿达帕林钠盐（3–30 μM；6–24 小时）可显着增强 G1 期细胞群 [3]。 GOT1 活性被阿达帕林钠盐 (1-200 μM) 抑制，IC50 为 21.79 μM[2]。阿达帕林钠盐 (10-6-10-3 nM) 的 IC50 为 2.5 nM，可抑制与质膜相关的 I 型转谷氨酰胺酶的表达[1]。细胞活力检测 [2]

阿贾帕林钠盐（15-100 mg/kg；每天口服，持续 21 天）可抑制 BALB/C 裸鼠中 DLD1 细胞来源的异种移植肿瘤的发展 [3]。

细胞活力检测[2]
细胞类型：胰腺癌（SW1990、Aspc-1）、乳腺癌（mm-231、mm-468、MCF-7）、肝癌（Hep3B） 、宫颈癌 (Hela)、卵巢癌 (HOV -7、ES-2)、正常细胞 (CHO、L929)
测试浓度： 1-200 μM
孵育持续时间：24小时
实验结果：抑制癌细胞的活力，GOT1蛋白表达较高。

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细胞凋亡分析 [2]
细胞类型： ES-2 细胞
测试浓度： 10、20、40 μM
孵育时间：24小时
实验结果：与对照组相比，细胞凋亡显着增加。下调抗凋亡蛋白 Bcl-2 和 PARP 的表达。

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细胞周期分析 [3]
细胞类型： LoVo 或 DLD1 细胞
测试浓度： 3、10、30 μM
孵育持续时间：6、12、24 小时
实验结果：在剂量和时间范围内导致细胞周期停滞在 G1 期-依赖方式。

Animal/Disease Models: Female BALB/C nude mice (15 g, 4-5 weeks) injected with DLD1 cells [3]
Doses: 15, 20, 65, 100 mg/kg
Route of Administration: Po daily for 21 days
Experimental Results: Tumor Significant reduction in weight and size.

[1]. Shroot B, et, al. Pharmacology and chemistry of adapalene. J Am Acad Dermatol. 1997 Jun;36(6 Pt 2):S96-103.
[2]. Wang Q, et, al. Adapalene inhibits ovarian cancer ES-2 cells growth by targeting glutamic-oxaloacetic transaminase 1. Bioorg Chem. 2019 Dec;93:103315.
[3]. Shi XN, et, al. Adapalene inhibits the activity of cyclin-dependent kinase 2 in colorectal carcinoma. Mol Med Rep. 2015 Nov;12(5):6501-8.

C28H27O3-.NA+

434.502

911110-93-5

Adapalene;106685-40-9

O=C(C1=CC2=CC=C(C3=CC=C(OC)C(C45C[C@@H](C[C@H](C6)C5)C[C@@H]6C4)=C3)C=C2C=C1)[O-].[Na+]

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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请根据您的实验动物和给药方式选择适当的溶解配方/方案：
1、请先配制澄清的储备液(如：用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液，按从左到右的顺序依次添加助溶剂，澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明，并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀/澄清；向上述体系中加入50 μL Tween-80，混合均匀/澄清；然后继续加入450 μL ddH2O (或 saline)定容至 1 mL；
3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出，可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果，工作液请现配现用！
6、如不确定怎么将母液配置成体内动物实验的工作液，请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。