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Glembatumumab vedotin (CDX-011) is an antibody-drug conjugate (ADC) 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 binds to GPNMB on tumors, the complex is internalized and MMAE is released via proteolytic cleavage of the vc linker in a lysosomal compartment. Tumor cell death occurs as a result of microtubule inhibition by MMAE with resultant cell cycle arrest.
Immobilized human GPNMB His at 2 ug/mL can bind Glembatumumab vedotin, the EC50 is 0.05407 ug/mL.
Glembatumumab vedotin (CR011-vcMMAE; 1.25-80 mg/kg; i.v.; every 4 days; for 16 days) shows short-term anti-tumor effects (inhibition of tumor growth) and long-term effects (complete regression) in human SK-MEL-2 and SK-MEL-5 melanoma xenografts.
CAS Number | 1182215-65-1 |
Solubility (25°C) | For Powder, reconstitute with sterile, distilled water to a final concentration of 1 mg/ml. |
Storage | Store at ≤ -20℃ for up to 24 months. Avoid repeated freeze-thaw cycles. |
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