In vitro: Miriplatin suspended in LPD (miriplatin/LPD, 100 μg/mL) inhibits the growth of AH109A cells, forms platinum-DNA adducts, and induces apoptosis.
In vivo: Miriplatin (0.02-0.4 mg/20 μL) in lipiodol reduces tumor growth rates in a dose dependent manner in rats bearing AH109A tumor cells. Miriplatin/LPD (400 μg/head) significantly reduces the growth of tumor in rats bearing AH109A cells.
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO: 0.01 mg/mL (0.01 mM)|
Intra-hepatic arterial administration with miriplatin suspended in an oily lymphographic agent inhibits the growth of tumors implanted in rat livers by inducing platinum-DNA adducts to form and massive apoptosis.
Hanada M, et al. Cancer Chemother Pharmacol. 2009 Aug;64(3):473-83. PMID: 19104812.
Antitumor effects of a novel lipophilic platinum complex (SM-11355) against a slowly-growing rat hepatic tumor after intra-hepatic arterial administration.
Kishimoto S, et al. Biol Pharm Bull. 2000 Mar;23(3):344-8. PMID: 10726891.
LB-100 is a water soluble protein phosphatase 2A (PP2A) inhibitor, with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.
Compstatinis is a 13-residue cyclic peptide, binds to complement component C3 and inhibits complement activation with IC50 of 12 μM.
Azaserine is an inhibitor of the rate limiting step of the hexosamine biosynthethic pathway (HBP) and an irreversible inhibitor of GGT1 (gamma-Glutamyltranspeptidase).
TM6008 is a novel PHD inhibitor, which inhibited PHD and stabilized HIF activity in vitro.
ASP9521 is a novel, selective, orally bioavailable inhibitor of 17β-hydroxysteroid dehydrogenase type 5 (17βHSD5; AKR1C3).
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