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7(4):609-26
having MTDs in mice and rats of >150 mg/ kg and 90 mg/kg in rats
Smiles: CN1C2=CN=C3C=CC(=NC3=C2N(C2CCN(CC2)C(=O)[C@H](C)O)C1=O)C1=CN=C(C)C=C1
InChiKey: HZCOFZVJMJRKIB-UHFFFAOYSA-N
NVP-TNKS656 - Wnt / Tankyrase Inhibitor. CAS# 1419949-20-4 0255 7(4):609-26NVP TNKS656, CAS No. 1419949 20 4, is a highly potent, selective and oral bioavailable tankyrase inhibitor with IC50 of 6 nM for TNKS2. It has 300 fold selectivity against PARP1 and PARP2. In MMTV Wnt1 tumor models, NVP TNKS656 was dosed to mice orally to stabilize Axin1 protein and reduce the Wnt beta catenin target gene Axin2 mRNA level by 70 80%. In colorectal cancer PDX models, NVP TNKS656 reduces nuclear catenin, reverts such resistance, and
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