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.
|all-trans 4-Keto Retinoic Acid
all-trans 4-Keto Retinoic Acid is an active metabolite of vitamin A, induces gene transcription via binding to nuclear retinoic acid receptors (RARs).
GK921 is a transglutaminase 2 (TGase 2) inhibitor.
Miridesap is a ligand for serum amyloid P component (SAP) and intends to inhibit and dissociate SAP binding to amyloid fibrils and tangles.
Aramchol is a cholesterol solubilizer that prevents gallstone formation in inbred mice.
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