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 320DM In Vitro OM-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 Vivo OM-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:Solid IC50& Target:TNKS1|13 nM (IC|50|)|TNKS2|2 nM (IC|50|)|Wnt/β-catenin|0.63 nM (IC|50|)
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
OM-153
CAS number：2406278-81-5 molecular formula：C28H24FN7O2
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 2406278-81-5 | molecular formula | C28H24FN7O2 |
| molecular weight | 509.53 g/mol | Exact mass | ≥99% |
| PSA | - | logp | - |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
