Adjudin (also known as AF-2364) is a potent Cl- channel blocker, with a superior mitochondria-inhibitory effect. Adjudin inhibits cell proliferation in a dose dependent manner in SGC-7901 (human gastric adenocarcinoma cell), MDA-MB-231 (human breast adenocarcinoma cell), Smmc-7721 (human hepatoma cell) and MIA Paca-2 (human pancreatic adenocarcinoma cell) cells. The IC50 of Adjudin is determined to be 58.0 µM, 13.8 µM, 72.3 µM and 52.7 µM against SGC-7901, MDA-MB-231, Smmc-7721 and MIA Paca-2 cells, respectively, after treatment for 24 h. Similar results are obtained in other human and mice cancer cell lines. The IC50 of Adjudin in A549 cells and PC3 cells is 63.1 µM and 93.0 µM, respectively. Adjudin-treated mice show significant tumor growth inhibition compared with the control group (P<0.0001 in the human lung carcinoma cells A549 and P=0.006 in the prostate carcinoma cells PC3).
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO: ≥ 30 mg/mL|
Inhibition of sperm capacitation and fertilizing capacity by adjudin is mediated by chloride and its channels in humans.
Li K, et al. Hum Reprod. 2013 Jan;28(1):47-59. PMID: 23117128.
EC5026 (BPN-19186) is a first-in-class, potent and orally active soluble inhibitor of Epoxide Hydrolase (sEH). EC5026 has the potential to relieve pain by stabilizing natural analgesic and anti-inflammatory mediators.
VPC-80051 is a novel inhibitor of hnRNP A1 that targets the hnRNP A1 RBD.
|D-Ribose 5-phosphate disodium
D-Ribose 5-phosphate disodium is an intermediate of the oxidative branch of the pentose phosphate pathway (PPP) and an end product of the nonoxidative branch of the PPP.
|Oleic acid (Liquid)
Oleic acid (9-cis-Octadecenoic acid) is an abundant monounsaturated fatty acid. Oleic acid is also a Na+/K+ ATPase activator.
1,2-Dimyristoyl-sn-glycero-3-phosphocholine (DMPC) has the ability to enhance the constancy and in vitro antiproliferative effect of carmofur.
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