| Company Name: |
TargetMol Chemicals Inc.
|
| Tel: |
15002134094 |
| Email: |
marketing@targetmol.cn |
| Products Intro: |
Product Name:OM-153
CAS:2406278-81-5
Package:50mg/RMB 19420;25mg/RMB 14900;100mg/RMB 24625
|
|
| | 5-Quinoxalinecarboxamide, N-[trans-3-[5-(5-ethoxy-2-pyridinyl)-4-(2-fluorophenyl)-4H-1,2,4-triazol-3-yl]cyclobutyl]- Basic information |
| | 5-Quinoxalinecarboxamide, N-[trans-3-[5-(5-ethoxy-2-pyridinyl)-4-(2-fluorophenyl)-4H-1,2,4-triazol-3-yl]cyclobutyl]- Chemical Properties |
| 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 |
| | 5-Quinoxalinecarboxamide, N-[trans-3-[5-(5-ethoxy-2-pyridinyl)-4-(2-fluorophenyl)-4H-1,2,4-triazol-3-yl]cyclobutyl]- Usage And Synthesis |
| 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) | | 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. |
| | 5-Quinoxalinecarboxamide, N-[trans-3-[5-(5-ethoxy-2-pyridinyl)-4-(2-fluorophenyl)-4H-1,2,4-triazol-3-yl]cyclobutyl]- Preparation Products And Raw materials |
|