Identification | Back Directory | [Name]
5-Quinoxalinecarboxamide, N-[trans-3-[5-(5-ethoxy-2-pyridinyl)-4-(2-fluorophenyl)-4H-1,2,4-triazol-3-yl]cyclobutyl]- | [CAS]
2406278-81-5 | [Synonyms]
OM-153 5-Quinoxalinecarboxamide, N-[trans-3-[5-(5-ethoxy-2-pyridinyl)-4-(2-fluorophenyl)-4H-1,2,4-triazol-3-yl]cyclobutyl]- | [Molecular Formula]
C28H24FN7O2 | [MOL File]
2406278-81-5.mol | [Molecular Weight]
509.53 |
Chemical Properties | Back Directory | [density ]
1.42±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (196.26 mM; Need ultrasonic) | [form ]
Solid | [pka]
12.16±0.40(Predicted) | [color ]
Off-white to light yellow |
Hazard Information | Back Directory | [Uses]
OM-153 is a potent and orally active tankyrase inhibitor with IC50s 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 IC50 value of 0.63 nM. OM-153 shows inhibition of Wnt/β-catenin signaling and proliferation in COLO 320DM[1][2]. | [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[2].
OM-153 potentiates anti-PD-1 immune checkpoint inhibition and antitumor effect in a B16-F10 mouse melanoma model[2].
Animal Model: | CB17-SCID mice bearing COLO 320DM cells[2] | Dosage: | 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 tumors[2] | Dosage: | 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. |
| [IC 50]
TNKS1: 13 nM (IC50); TNKS2: 2 nM (IC50); Wnt/β-catenin: 0.63 nM (IC50) | [storage]
Store at -20°C | [References]
[1] Leenders RGG, et al. Development of a 1,2,4-Triazole-Based Lead Tankyrase Inhibitor: Part II. J Med Chem. 2021;64(24):17936-17949. DOI:10.1021/acs.jmedchem.1c01264 [2] Shoshy A. Brinch, et al. The Tankyrase Inhibitor OM-153 Demonstrates Antitumor Efficacy and a Therapeutic Window in Mouse Models. Cancer Research Communications (2022) 2 (4): 233-245. |
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