OM-153 (C09-1160-067)

OM-153 is a potent and orally active tankyrase inhibitor with IC 50 s of 13 nM and 2 nM for tankyrase 1 and tankyrase 2 ( TNKS1/2 ), respectively. OM-153 inhibits luciferase-based Wnt/β-catenin signaling reporter activity with an IC 50 value of 0.63 nM. OM-153 shows inhibition of Wnt/β-catenin signaling and proliferation in COLO 320DMIn VitroOM-153 shows picomolar IC 50 inhibition (0.63 nM) in a cellular (HEK293) WNT/β-catenin signaling reporter assay, no off-target liabilities, overall favorable absorption, distribution, metabolism, and excretion (ADME) properties, and an improved pharmacokinetic profile in mice. OM-153 decreases cell growth in COLO 320DM cells with a GI 50 value of 10 nM and a GI 25 value of 2.5 nM (concentrations resulting in 50% and 25% growth inhibition, respectively), while cell growth in RKO cells was insubstantially affected by the treatment. OM-153 inhibits WNT/β-catenin, YAP, and MYC signaling and shows an antiproliferative fffect in human cancer cell lines. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoOM-153 (0.1-10 mg/kg; p.o.; twice daily; for 34 days) reduces WNT/β-catenin signaling and tumor progression in COLO 320DM colon carcinoma xenografts. OM-153 potentiates anti-PD-1 immune checkpoint inhibition and antitumor effect in a B16-F10 mouse melanoma model. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: CB17-SCID mice bearing COLO 320DM cellsDosage: 10 mg/kg, 3.3 mg/kg, 1 mg/kg, 0.33 mg/kg, or 0.1 mg/kg Administration: p.o.; twice daily; for 34 days Result: Reduced WNT/β-catenin signaling and tumor progression in COLO 320DM colon carcinoma xenografts. Animal Model: C57BL/6N mice injected with B16-F10 tumorsDosage: 10 mg/kg, 1 mg/kg, and 0.1 mg/kg Administration: p.o.; twice daily; for 20 days Result: Potentiated anti-PD-1 immune checkpoint inhibition and antitumor effect.Form:SolidIC50& Target:TNKS1|13 nM (IC|50|)|TNKS2|2 nM (IC|50|)|Wnt/β-catenin|0.63 nM (IC|50|). Specifications and Purity: 99%. Molecular Formula: C28H24FN7O2. Molecular Weight: 509.53.