Glembatumumab vedotin

Modify Date: 2024-01-03 13:59:01

Glembatumumab vedotin Structure
Glembatumumab vedotin structure
Common Name Glembatumumab vedotin
CAS Number 1182215-65-1 Molecular Weight N/A
Density N/A Boiling Point N/A
Molecular Formula N/A Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Glembatumumab vedotin


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].

 Names

Name Glembatumumab vedotin

 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
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