LT-626 inhibits PARP-1 activity.LT-626 is a PARP inhibitor that is able to inhibit PARP enzymatic activity and cellular PAR synthesis in the same nanomolar range as the previously characterized PARP inhibitors veliparib and olaparib while demonstrating greater potency than both of them in a cellular cytotoxicity assay.
|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.
Cancer Lett 2014 Feb 28;217-23.
Poly (ADP-ribose) polymerase inhibitor LT-626: Sensitivity correlates with MRE11 mutations and synergizes with platinums and irinotecan in colorectal cancer cells.
McPherson LA, et al. Cancer Lett. 2014 Feb 28;343(2):217-23. PMID: 24215868.
Abstract 5490: Poly (ADP-ribose) polymerase inhibitor LT-626 sensitizes lung and pancreatic cancers to fractionated radiation therapy
Kedar Hastak, et al. Cancer Research. 2014 Oct 1.
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Daidzein is an inactive analogue of genistein, a tyrosine kinase inhibitor and an estrogen receptor activator.
NMS-P118 is a potent, orally available, and highly selective PARP-1 inhibitor endowed with excellent ADME and pharmacokinetic profiles, showing 150-fold selectivity for PARP-1 over PARP-2 (Kd 0.009 μM vs 1.39 μM, respectively).
E7449 is an orally bioavailable, brain penetrable, small molecule dual inhibitor of PARP1/2 that also inhibits PARP5a/5b, otherwise known as tankyrase1 and 2 (TNKS1/2), important regulators of canonical Wnt/β-catenin signaling. It has IC50 values of 1.0 and 1.2 nM for PARP1 and 2, respectively.
BMN-673 (8R,9S) is the (8R,9S) enantiomer of BMN-673.BMN673 is a potent inhibitor of poly (ADP-ribose) polymerases (PARP)-1 and -2.
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