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2406278-81-5

2406278-81-5 Structure

2406278-81-5 Structure
IdentificationBack 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 PropertiesBack 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 InformationBack 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.
2406278-81-5 suppliers list
Company Name: Aladdin Scientific
Tel:
Website: www.aladdinsci.com/
Company Name: TargetMol Chemicals Inc.  
Tel: 15002134094
Website: https://www.targetmol.cn/
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