CA-3

CA-3

货号:
IC2240

品牌:
Jinpan

CA-3

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CA-3

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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
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