Citatuzumab bogatox (VB6-845) 是一种重组免疫毒素，由靶向EpCAM的人源化抗体的 Fab 片段和改良的细胞毒素 Bouganin 组成。Citatuzumab bogatox 能结合并选择性诱导EpCAM阳性细胞系凋亡，并在EpCAM阳性人肿瘤异种移植模型中显示良好活性。
| 生物活性 | Citatuzumab bogatox (VB6-845) isrecombinant immunotoxinthat composed of Fab fragment of humanized antibody targetingEpCAMand a modified cytotoxin bouganin. Citatuzumab bogatox binds to and selectively inducesapoptosisinEpCAM-positive cell lines and shows good activity inEpCAM-positive human tumour xenograft models[1][2][3]. |
体外研究
(In Vitro) | Citatuzumab bogatox (0-100 nM; 5 days) 抑制 NIH:OVCAR-3 和 CAL-27 细胞的生长，IC50值均为 3 nM[1]。
Citatuzumab bogatox 内化到 EpCAM 表达细胞的细胞质中，然后释放的 Bouganin 通过核糖体失活抑制蛋白质合成，导致癌细胞凋亡[2]。
Cell Viability Assay[1] | Cell Line: | NIH:OVCAR-3 and CAL-27 cells | | Concentration: | 0-100 nM | | Incubation Time: | 5 days | | Result: | Exhibited an IC50of 3 nM to against the EpCAM-positive cell lines. |
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体内研究
(In Vivo) | Citatuzumab bogatox (10, 20 mg/kg; i.v./i.p.) 抑制小鼠体内肿瘤生长[1]。
Citatuzumab bogatox (10, 20 mg/kg) 在小鼠体内显示很好的耐受性，并无任何明显的体重下降[1]。
| Animal Model: | Female CB.17 SCID mice (~20 g; OVCAR-3 Xenograft model)[1]. | | Dosage: | 10, 20 mg/kg | | Administration: | Tail vein (until day 26 when due to tail swelling, route of administration was changed to intraperitoneal for the remaining 7 doses); single daily for 5 consecutive days for 3 weeks and then received maintenance dosing on Monday and Friday for 4 weeks. | | Result: | Showed an average of 40 mm3(control group was 750 mm3) on day 75, and with 3/15 mice being tumor free, when at 10 mg/kg.
Almost completely inhibited tumour growth when at 20 mg/kg. |
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| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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