Cys-McMMAF

Names

[ CAS No. ]:
1160590-05-5

[ Name ]:
Cys-McMMAF

Biological Activity

[Description]:

Cys-McMMAF is the released payload of AlMcMMAF, an anti-5T4 humanized A1 antibody conjugated to the microtubule disrupting MMAF (HY-15579) via a maleimidocaproyl linker. Cys-McMMAF has antitumor efficacy in two tumor mouse models (H1975 and MDA-MB-361-DYT2 models)[1].

[Related Catalog]:

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

[In Vivo]

Cys-McMMAF (0.3 mg/kg, 3 mg/kg; 静脉注射; 单剂量) 在食蟹猴体内的稳定性一般，衰退时间短[1]。 在裸鼠 (nu/nu) 中的药代动力学分析[1] Model/IV Dose (mg/kg) Cmax (ng/mL) Tmax (hr) AUC0-336 (ng·h/mL) t1/2 (day) Non-Tumor 1 0.192 8 14.6 2.1 Tumor 1 0.146 8 28.2 6.0 Non-Tumor 10 0.951 8 58.5 3.0 Tumor 10 0.945 8 81.9/td> 2.9

[References]

[1]. Leal M, et al. Preclinical Development of an anti-5T4 Antibody-Drug Conjugate: Pharmacokinetics in Mice, Rats, and NHP and Tumor/Tissue Distribution in Mice. Bioconjug Chem. 2015 Nov 18;26(11):2223-32.  

Chemical & Physical Properties

[ Molecular Formula ]:
C52H83N7O13S

[ Molecular Weight ]:
1046.32

Related Compounds