EBE-A22 is a derivative of PD 153035. EBE-A22, has no effect on EGF-R TK but maintains a high cytotoxic profile. EBE-A22 binds to DNA and behave as typical intercalating agents. EBE-A22 unwinds supercoiled plasmid, stabilizes duplex DNA against heat denaturation, and produces negative CD and ELD signals, as expected for an intercalating agent.
|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.
Upregulation of retinoic acid receptor-beta by the epidermal growth factor-receptor inhibitor PD153035 is not mediated by blockade of ErbB pathways.
Grunt TW, et al. J Cell Physiol. 2007 Jun;211(3):803-15. PMID: 17286282.
DNA interaction of the tyrosine protein kinase inhibitor PD153035 and its N-methyl analogue.
Goossens JF, et al. Biochemistry. 2001 Apr 17;40(15):4663-71. PMID: 11294633.
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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