CA-3
货号：
IC2240
品牌：
Jinpan
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产品简介
| 有效期 | 2年 |
| 描述 | 是一种有效的选择性ferroptosis 诱导剂。 |
| 别名 | CIL-56 |
| CAS | 300802-28-2 |
| 分子式 | C23H27N3O5S2 |
| 分子量 | 489.61 |
| 储存条件 | -20℃ |
| 纯度 | ≥98% |
| 外观（性状） | Solid |
| 单位 | 瓶 |
| 生物活性 | CA3 (CIL56) 对YAP1/Tead转录活性具有有效的抑制作用，主要靶向高表达YAP1、具有癌症干细胞属性的、难治疗的食管腺癌细胞。CA3(CIL56)可诱导铁死亡和铁依赖的活性氧自由基。[1] |
| In Vitro | CA3可强有效地抑制食管腺癌细胞生长。CA3抑制肿瘤细胞的增殖、诱导凋亡、减少肿瘤球的形成以及ALDH1+细胞群体数量。在293T细胞中，CA3特别地抑制Tead/YAP1转录活性，但对其他转录因子Super-TOP/Wnt、CBF1/Notch和AP-1没有抑制活性。在耐辐射的食管腺癌细胞中，CA3优先抑制其癌症干细胞属性[1]。 |
| In Vivo | 在移植瘤模型中，CA3可发挥强有效的抗肿瘤活性，而不具有明显毒性作用[1]。 |
| SMILES | O=S(C1=CC2=C(C=C1)C3=C(C=C(S(=O)(N4CCCCC4)=O)C=C3)/C2=NO)(N5CCCCC5)=O |
| 靶点 | Ferroptosis |
| 动物实验 | SKGT-4 (PIN20YAP1) cells (1 x 106) without (Dox- ) or with (Dox+) YAP1 induction by doxycycline were inoculated into nude mice (n= 5/group). The mice in the Dox+ group were fed drinking water containing 2.5% sucrose and 2.5% doxycycline, whereas those in the Dox- group were fed water containing only 2.5% sucrose. After 10 days, CA3 was intraperitoneally injected into the animals in the Dox+ group at 1 mg/kg/mouse three times a week for total 3 weeks. In a JHESO xenograft model of esophageal adenocarcinoma, 2×106 JHESO cells were subcutaneously injected into nude mice (n=5/group). After about 10 days, the mice underwent intra_x005fperitoneal injection of CA3 at 1 mg/kg/mouse, 5-FU at 30 mg/kg/mouse, or a combination of them three times a week for total 3 weeks. A control group was given PBS at 100 mL/mouse. The mice’s tumor volumes, tumor weights, and body weights were measured as described previously. All measurements were compared using an unpaired Student t test.[1] |
| 细胞实验 | The esophageal adenocarcinoma cells and their resistant counterparts were treated with 0.1% DMSO (control), CA3 at different doses. For combination treatment experiments, treatment of the cells with CA3, 5-FU, or a combination at different concentrations was administered for 6 days as indicated, and the cell viability was assessed using an MTS assay as described previously. All assays were performed in triplicate and repeated at least three times.[1] |
| 数据来源文献 | [1] Song S, et al. Mol Cancer Ther. 2018, 17(2):443-454. |
| 规格 | 2mg 5mg |