Name | Glembatumumab vedotin |
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Description | Glembatumumab vedotin (CDX-011) is an ADC (antibody-drug conjugates (ADCs)) comprising a fully human IgG2 monoclonal antibody (CR011) directed against glycoprotein NMB (GPNMB) and conjugated to the potent tubulinbinding cytotoxic agent MMAE via a protease-sensitive vc linker. Glembatumumab vedotin has potent anticancer effects[1]. |
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Related Catalog | |
In Vitro | Glembatumumab vedotin 与肿瘤上的 GPNMB 结合,复合物被内化,MMAE 通过溶酶体区室中 vc 接头的蛋白水解切割释放。MMAE 抑制微管并导致细胞周期停滞导致肿瘤细胞死亡[1]。 Glembatumumab vedotin(1-125 μg/mL;96 小时)表现出骨肉瘤细胞毒活性[3]。 Cell Viability Assay[3] Cell Line: Osteosarcoma cell lines Concentration: 1 μg/mL to 125 μg/mL Incubation Time: 96 hours Result: Demonstrated osteosarcoma cytotoxic activity. |
In Vivo | Glembatumumab vedotin(CR011-vcMMAE;1.25-80 mg/kg;静脉注射;每 4 天一次;持续 16 天)在人类 SK-MEL-2 和 SK-MEL-5 黑色素瘤异种移植模型中显示出短期抗肿瘤作用(抑制肿瘤生长)和长期作用(完全消退)[2]。 Animal Model: Athymic mice (6-week-old) injected with human SK-MEL-2 and SK-MEL-5 melanoma cells[2] Dosage: 1.25 mg/kg, 2.5 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg, 40 mg/kg, 60 mg/kg, 80 mg/kg Administration: i.v.; every 4 days; for 16 days Result: Showed inhibition of tumor growth. |
References |
No Any Chemical & Physical Properties |