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CAS No: 1182215-65-1
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生物活性：
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.
体内研究：
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）。Animal Model:Athymic mice (6-week-old) injected with human SK-MEL-2 and SK-MEL-5 melanoma cells
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.
体外研究：
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。Glembatumumab vedotin（1-125 μg/mL；96 小时）表现出骨肉瘤细胞毒活性。
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.
体内研究：
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）。Animal Model:Athymic mice (6-week-old) injected with human SK-MEL-2 and SK-MEL-5 melanoma cells
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.
体外研究：
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。Glembatumumab vedotin（1-125 μg/mL；96 小时）表现出骨肉瘤细胞毒活性。
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