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Glembatumumab vedotin

Names

[ CAS No. ]:
1182215-65-1

[ Name ]:
Glembatumumab vedotin

Biological Activity

[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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> Microtubule/Tubulin
Signaling Pathways >> Cytoskeleton >> Microtubule/Tubulin

[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]

[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.  

Chemical & Physical Properties

No Any Chemical & Physical Properties

Related Compounds