| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| B409228-1ml |
1ml |
现货  |
|
| 英文别名 | Targretin | 4-(1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)vinyl)benzoic acid |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Bexarotene (LGD1069) |
| 生化机理 | 贝沙罗汀（Targretin，LGD1069）是一种对视黄醇 X 受体具有特异选择性的视黄醇类药物，可作为口服抗肿瘤药物用于治疗皮肤 T 细胞淋巴瘤。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 激动剂 |
| 作用机制 | 维甲酸 X 受体激动剂 |
| 产品介绍 |
Bexarotene (贝沙罗汀; Targretin)是维甲酸X受体（RXR）激动剂，可作用于CTCL。A selective agonist of retinoid X receptors Information Bexarotene (LGD1069) Bexarotene (Targretin, LGD1069) is a retinoid specifically selective for retinoid X receptors, used as an oral antineoplastic agent in the treatment of cutaneous T-cell lymphoma. Bexarotene treatment at 1 mM and 10 mM for 96 h increases the number of cells with sub-G1 populations and annexin V binding in a dose-dependent manner compared with vehicle controls (DMSO) in well-established CTCL cell lines (MJ, Hut78, and HH), respectively. Bexarotene treatment suppresses the expression of retinoid X receptor alpha and retinoic acid receptor alpha proteins in all three lines compared with untreated controls. Bexarotene treatment decreases the protein levels of survivin, activates caspase-3, and cleaved poly(ADP-Ribose) polymerase, but has no obvious effect on expression of Fas/Fas ligand and bcl-2 proteins in all three CTCL lines. Bexarotene induces a loss of viability and more pronounced inhibition of clonogenic proliferation in HH and Hut-78 cells, whereas the MJ line exhibits resistance. Bexarotene upregulates and activates Bax in sensitive lines, although not enough to signal significant apoptosis. Bexarotene signals both G(1) and G(2)/M arrest by the modulation of critical checkpoint proteins. Bexarotene activates p53 by phosphorylation at Ser15, which influences the binding of p53 to promoters for cell cycle arrest, induces p73 upregulation, and, in concordance, also modulates some p53/p73 downstream target genes, such as p21, Bax, survivin and cdc2. In vivo Bexarotene significantly prevents ER-negative mammary tumorigenesis with less toxicity than naturally occurring retinoids in animal models. Bexarotene inhibits the development of preinvasive mammary lesions such as hyperplasias and carcinoma-in-situ in MMTV-erbB2 mice. cell lines： Concentrations： Incubation Time： Powder Purity:≥97% |
| ALogP | 7.6 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CC1=CC2=C(C=C1C(=C)C3=CC=C(C=C3)C(=O)O)C(CCC2(C)C)(C)C |
| 分子量 | 348.48 |
| Reaxy-Rn | 7041961 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7041961&ln= |
| 折光率 | 1.56 |
|---|---|
| 沸点 | 489.67° C at 760 mmHg |
| 熔点 | 220-225℃ |
| 象形图 | GHS08, GHS07 |
|---|---|
| 信号词 | Warning |
| 危险声明 |
H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害 H361: 怀疑破坏生育力或未出生的孩子 |
| 预防措施声明 |
P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染：用水充分清洗。 P321: 特殊处理（请参阅此标签上的...）。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P271: 仅在室外或通风良好的地方使用。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P304+P340: 如误吸入：将人转移到空气新鲜处，保持呼吸舒适体位。 P403+P233: 存放在通风良好的地方。保持容器密闭。 P362+P364: 脱掉沾污的衣服，清洗后方可重新使用。 P330: 漱口 P203: 使用前，获取、阅读并遵守所有安全说明。 P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。 P301+P317: 如果被吞咽：请寻求医疗帮助。 P318: 如果暴露或担心，请就医。 P337+P317: 如果眼睛刺激持续：寻求医疗帮助。 P332+P317: 如果出现皮肤刺激：请寻求医疗帮助。 P319: 如果你感到不适，请寻求医疗帮助。 |
| WGK Germany | 3 |
| Merck Index | 1194 |
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