BMS 453
(Synonyms: BMS-189453) 目录号 : GC10656
An RARβ agonist, RARα/γ antagonist
Cas No.:166977-43-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
BMS 453 is a synthetic RAR (retinoic acid receptor) antagonist [1].
The retinoic acid receptors (RARα, RARβ, RARγ) belong to steroid nuclear receptor superfamily and the expressions of retinoid receptor RARα and RARβ are correlated with the antiproliferative effects of retinoids.
In normal breast cells, BMS453 inhibited the cell proliferation without significantly apoptosis. BMS 453 blocked the G1/S transition of the cell cycle with an increase in the amount of cells in G0/G1 and a decrease in the amount of cells in S phase. Also, BMS453 increased active TGFβ activity by 33-fold, which show BMS453 induces conversion of latent TGFβ to active TGFβ. TGFβ mediates the anti-proliferative effect of BMS453 in breast cells [1]. BMS 453 transrepresses AP-1 but does not activate RAR-dependent gene expression. In normal breast cells (HMEC and 184) and T47D breast cancer cells, BMS453 inhibited the growth of T47D breast cancer cells and normal breast cells (HMEC and 184). Breast cancer cells were resistant to BMS453 and normal human breast cells were most sensitive to BMS453. BMS453 may suppress growth by inhibiting transcription factors such as AP-1 [2].
References:
[1]. Yang L, Ostrowski J, Reczek P, et al. The retinoic acid receptor antagonist, BMS453, inhibits normal breast cell growth by inducing active TGFbeta and causing cell cycle arrest. Oncogene, 2001, 20(55): 8025-8035.
[2]. Yang L, Munoz-Medellin D, Kim HT, et al. Retinoic acid receptor antagonist BMS453 inhibits the growth of normal and malignant breast cells without activating RAR-dependent gene expression. Breast Cancer Res Treat, 1999, 56(3): 277-291.
| Cas No. | 166977-43-1 | SDF | |
| 别名 | BMS-189453 | ||
| 化学名 | (E)-4-(2-(5,5-dimethyl-8-phenyl-5,6-dihydronaphthalen-2-yl)vinyl)benzoic acid | ||
| Canonical SMILES | OC(C1=CC=C(C=C1)/C=C/C2=CC=C3C(C)(C)CC=C(C4=CC=CC=C4)C3=C2)=O | ||
| 分子式 | C27H24O2 | 分子量 | 380.48 |
| 溶解度 | DMF: 5 mg/ml,DMSO: 10 mg/ml | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6283 mL | 13.1413 mL | 26.2826 mL |
| 5 mM | 0.5257 mL | 2.6283 mL | 5.2565 mL |
| 10 mM | 0.2628 mL | 1.3141 mL | 2.6283 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。