Inhibitors?Screening Libraries?ProteinsMedChemExpressGlembatumumab ved
otinCat. No.:HY-141604CAS No.:1182215-65-1Synonyms:CDX-011; CR011
-vcMMAE作用靶点:Antibody-Drug Conjugates (ADCs); Microtubule/Tubulin作
用通路:Antibody-drug Conjugate/ADC Related; Cell Cycle/DNADamage; Cy
toskeleton储存方式:Please store the product under the recommended con
ditions inthe Certificate of Analysis.BIOLOGICAL ACTIVITY生物活性Glem
batumumab vedotin (CDX-011) 是一种 ADC (Antibody-Drug Conjugates (AD
Cs))，包含针对糖蛋白NMB (GPNMB) 的全人 IgG2 单克隆抗体 (CR011)，并通过蛋白酶敏感的 vc 接头与强效
微管蛋白结合细胞毒剂MMAE 偶联。Glembatumumab vedotin 具有强大的抗癌作用 [1]。体外研究Glembat
umumab vedotin binds to GPNMB on tumors, the complex is internali
zed and MMAE is released viaproteolytic cleavage of the vc linker
in a lysosomal compartment. Tumor cell death occurs as a result
ofmicrotubule inhibition by MMAE with resultant cell cycle arrest
[1].Glembatumumab vedotin (1-125 μg/mL; 96 hours) demonstrates o
steosarcoma cytotoxic activity [3].Cell Viability Assay [3]Cell L
ine:Osteosarcoma cell linesConcentration:1 μg/mL to 125 μg/mLIncu
bation Time:96 hoursResult:Demonstrated osteosarcoma cytotoxic ac
tivity.体内研究Glembatumumab vedotin (CR011-vcMMAE; 1.25-80 mg/kg; i.
v.; every 4 days; for 16 days) shows short-termanti-tumor effects
(inhibition of tumor growth) and long-term effects (complete reg
ression) in human SK-MEL-2 and SK-MEL-5 melanoma xenografts [2].A
nimal Model:Athymic mice (6-week-old) injected with human SK-MEL-
2 and SK-MEL-5 melanoma1/2MedChemExpresswww.MedChemExpress.cncell
s [2]Dosage:1.25 mg/kg, 2.5 mg/kg, 5 mg/kg, 10 mg/kg, 20 mg/kg, 4
0 mg/kg, 60 mg/kg, 80 mg/kgAdministration:i.v.; every 4 days; for
16 daysResult:Showed inhibition of tumor growth.REFERENCESChrist
opher H Keir, et al. The use of an antibody drug conjugate, glemb
atumumab vedotin (CDX-011), for the treatment of breast cancer. E
xpert Opin Biol Ther. 2012 Feb;12(2):259-63.Vincent A Pollack, et
al. Treatment parameters modulating regression of human melanoma
xenografts by an antibody-drug conjugate (CR011-vcMMAE) targetin
g GPNMB. Cancer Chemother Pharmacol. 2007 Aug;60(3):423-35.Michae
l Roth, et al. Targeting Glycoprotein NMB With Antibody-Drug Conj
ugate, Glembatumumab Vedotin, for the Treatment of Osteosarcoma.
Pediatr Blood Cancer. 2016 Jan;63(1):32-8.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.2/2MedChemExpress |
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