| Bioactivity | 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]. |
| Invitro | 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: |
| 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: |
| Name | Glembatumumab vedotin |
| CAS | 1182215-65-1 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Christopher H Keir, et al. The use of an antibody drug conjugate, glembatumumab vedotin (CDX-011), for the treatment of breast cancer. Expert Opin Biol Ther. 2012 Feb;12(2):259-63. [2]. Vincent A Pollack, et al. Treatment parameters modulating regression of human melanoma xenografts by an antibody-drug conjugate (CR011-vcMMAE) targeting GPNMB. Cancer Chemother Pharmacol. 2007 Aug;60(3):423-35. [3]. Michael Roth, et al. Targeting Glycoprotein NMB With Antibody-Drug Conjugate, Glembatumumab Vedotin, for the Treatment of Osteosarcoma. Pediatr Blood Cancer. 2016 Jan;63(1):32-8. |