Bexarotene
(Synonyms: 贝沙罗汀; LGD1069) 目录号 : GC10037
An RXR agonist
Cas No.:153559-49-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
MJ, Hut78 and HH cell lines |
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Preparation method |
The solubility of this compound in DMSO is > 10.4 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months. |
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Reacting condition |
0.1, 1 and 10 μM; 24, 48, 72 and 96 hrs |
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Applications |
In MJ, Hut78 and HH cell lines, Bexarotene treatment for 96 hrs dose-dependently inhibited cell growth. In addition, Bexarotene increased the number of cells in the sub-G1 phase in a dose-dependent manner, which was accompanied by a loss of cells in the G1, S, and G2-M phases. However, Bexarotene did not show significant inhibition effect on cell growth and apoptosis at the dose of 0.1 to 10 μM over the period of 24 to 72 hrs in all 3 cell lines. |
| Animal experiment [2]: | |
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Animal models |
MMTV-erbB2 mice |
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Dosage form |
100 mg/kg; p.o.; q.d., 6 days per week |
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Applications |
In MMTV-erbB2 mice, Bexarotene treatment prevented the development of hyperplasias or mammary intraepithelial neoplasia (MIN) lesions. Moreover, Bexarotene significantly inhibited mammary gland proliferation after 2- and 4- month treatments. The immunohistochemical results showed that less than 1% of mammary epithelial cells in the Bexarotene treatment group showed positive caspase 3 staining, indicating that the cancer preventive effect of Bexarotene was not attributed to the induction of apoptosis. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Zhang C, Hazarika P, Ni X, Weidner DA, Duvic M. Induction of apoptosis by bexarotene in cutaneous T-cell lymphoma cells: relevance to mechanism of therapeutic action. Clin Cancer Res. 2002 May;8(5):1234-40. [2]. Li Y, Zhang Y, Hill J, Kim HT, Shen Q, Bissonnette RP, Lamph WW, Brown PH. The rexinoid, bexarotene, prevents the development of premalignant lesions in MMTV-erbB2 mice. Br J Cancer. 2008 Apr 22;98(8):1380-8. | |
Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma.
References:
[1]. Vakeva L, Ranki A, Hahtola S.Ten-year experience of bexarotene therapy for cutaneous T-cell lymphoma in Finland.Acta Derm Venereol. 2012 May;92(3):258-63. doi: 10.2340/00015555-1359.
[2]. Gui Y, et al. Bexarotent attenuated CCI-induced spinal neuroinflammation and neuropathic pain by targeting MKP-1. J Pain. 2019 Jan 17. pii: S1526-5900(18)30607-2.
[3]. Zhang X, Schlaak M, Fabri M, Mauch C, Kurschat P.Successful Treatment of a Panniculitis-Like Primary Cutaneous T-Cell Lymphoma of the α/β Type with Bexarotene.Case Rep Dermatol. 2012 Jan;4(1):56-60.
[4]. Orendas P, Kubatka P, Kajo K, Stollarova N, Kassayova M, Bojkova B, Pec M, Nosal V, Kiskova T, Zihlavnikova K, Karsnakova R.Melatonin enhanced bexarotene efficacy in experimental mammary carcinogenesis.Neoplasma. 2012;59(4):469-74.
[5]. Cras A, Politis B, Balitrand N, Darsin-Bettinger D, Boelle PY, Cassinat B, Toubert ME, Chomienne C.Bexarotene via CBP/p300 induces suppression of NF-κB-dependent cell growth and invasion in thyroid cancer.Clin Cancer Res. 2012 Jan 15;18(2):442-53.
| Cas No. | 153559-49-0 | SDF | |
| 别名 | 贝沙罗汀; LGD1069 | ||
| 化学名 | 4-[1-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)ethenyl]benzoic acid | ||
| Canonical SMILES | CC1=CC2=C(C=C1C(=C)C3=CC=C(C=C3)C(=O)O)C(CCC2(C)C)(C)C | ||
| 分子式 | C24H28O2 | 分子量 | 348 |
| 溶解度 | ≥ 10.35mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8736 mL | 14.3678 mL | 28.7356 mL |
| 5 mM | 0.5747 mL | 2.8736 mL | 5.7471 mL |
| 10 mM | 0.2874 mL | 1.4368 mL | 2.8736 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。