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SR 11302

目录号 : GC12810

An inhibitor of retinoid-induced AP-1 signaling

SR 11302 Chemical Structure

Cas No.:160162-42-5

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,269.00
现货
1mg
¥439.00
现货
5mg
¥1,154.00
现货
10mg
¥1,803.00
现货
50mg
¥6,345.00
现货
100mg
¥10,094.00
现货

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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment [1]:

Cell lines

T-47D, Calu-6 and HeLa cell lines

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10-6 M

Applications

SR 11302 inhibits effectively the proliferation of T-47D, Calu-6 and HeLa cell lines, and could serve as a candidate for new retinoid therapeutic agent with reduced side effects.

Animal experiment [2]:

Animal models

AP-1-luciferase transgenic mice

Dosage form

four times over 7 days with 34 nmol dissolved in 300 μl acetone

Application

SR 11302 is one of the most promising drug candidate for chemotherapy and chemoprevention of cancer, and its effect is mediated by blocking AP-1 activity.

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.

References:

[1] Fanjul A, Dawson MI, Hobbs PD, et al. A new class of retinoids with selective inhibition of AP-1 inhibits proliferation. Nature, 1994, 372(6501): 107-111.

[2] Huang C, Ma WY, Dawson MI, et al. Blocking activator protein-1 activity, but not activating retinoic acid response element, is required for the antitumor promotion effect of retinoic acid. Proc Natl Acad Sci U S A, 1997, 94(11): 5826-5830.

产品描述

SR 11302 is an inhibitor of activator protein-1 (AP-1) [1].AP-1 is a transcription factor that displays antitumor effects in vivo.

SR 11302 is an inhibitor of AP-1 but don’t activate RARs and RXR. SR11302 failed to inhibit the proliferation of F9 cells, the embryonal carcinoma cell line. While, it can inhibit the growth of breast cancer cell line T-47D, the lung cancer line Calu-6 and HeLa cells[1]. SR 11302 had very little effect on either the proliferation or the differentiation of HL-60, fresh APL and NB4 cells, which indicate that AP-1 may not be involved in the signaling pathway of proliferation and differentiation of HL-60, fresh APL and NB4 cells [2].

In an AP-1-luciferase transgenic mouse carcinogenesis model, SR11302 significantly inhibit both AP-1 activation in 7,12-dimethyl benz(a)anthracene-initiated mouse skin and 12-O-tetradecanoylphorbol-13-acetate-induced papilloma formation. While, SR11235, a retinoid with RARE transactivating activity, but lack of AP-1 inhibiting effect, didn’t inhibit papilloma formation and AP-1 activation. These results show that the antitumor effect of retinoids is mediated by blocking AP-1 activity in vivo [3].

References:
[1]. Fanjul A, Dawson MI, Hobbs PD, et al. A new class of retinoids with selective inhibition of AP-1 inhibits proliferation. Nature, 1994, 372(6501): 107-111.
[2]. Shiohara M, Dawson MI, Hobbs PD, et al. Effects of novel RAR- and RXR-selective retinoids on myeloid leukemic proliferation and differentiation in vitro. Blood, 1999, 93(6): 2057-2066.
[3]. Huang C, Ma WY, Dawson MI, et al. Blocking activator protein-1 activity, but not activating retinoic acid response element, is required for the antitumor promotion effect of retinoic acid. Proc Natl Acad Sci U S A, 1997, 94(11): 5826-5830.


Chemical Properties

Cas No. 160162-42-5 SDF
化学名 3-methyl-7-(4-methylphenyl)-9-(2,6,6-trimethylcyclohexen-1-yl)nona-2,4,6,8-tetraenoic acid
Canonical SMILES CC1=C(C(CCC1)(C)C)C=CC(=CC=CC(=CC(=O)O)C)C2=CC=C(C=C2)C
分子式 C26H32O2 分子量 376.54
溶解度 0.5 mg/ml in ethanol; 10mg/ml in DMSO; 20mg/mL in DMF 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。
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。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.6558 mL 13.2788 mL 26.5576 mL
5 mM 0.5312 mL 2.6558 mL 5.3115 mL
10 mM 0.2656 mL 1.3279 mL 2.6558 mL
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