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In an adoptive transfer TCL1 mouse model of CLL
with 5-ethynyl-2′-deoxyuridine (EdU) incorporation returning near baseline levels in a dose-dependent manner by 24 hours after administration
O=S(=O)(C1C=CC(=CC=1)C1C=C2N=CC=CC2=CC=1)N1CCC2(CN(C3CC3)C(=O)CO2)CC1
4-dioxopentan-3-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-4-[[(2S)-3-(1H-indol-3-yl)-2-(phenylmethoxycarbonylamino)propanoyl]amino]-5-oxopentanoate
GNF-6231 0636457-O-C3-COOH In an adoptive transfer TCL1GNF 6231 is a potent, selective, and orally bioavailable Porcupine inhibitor that blocks Wnt signaling. 1) GNF 6231 shows IC50s of greater than 10 M on all CYP isoforms tested2) GNF 6231 have favorable potency and a PK profile across preclinical species upon oral administration. 3) The reference for orally in MMTV Wnt1 tumor bearing mice is dosed at 3 mg kg. 4) GNF 6231 showed very robust dose related antitumor efficacy. Product information CAS