| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| Targets |
TNKS1 ( IC50 = 13 nM ); TNKS2 ( IC50 = 2 nM ); Wnt/β-catenin ( IC50 = 0.63 nM )
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|---|---|
| ln Vitro |
OM-153 exhibits favorable absorption, distribution, metabolism, and excretion (ADME) properties, no off-target liabilities, improved pharmacokinetic profile in mice, and picomolar IC50 inhibition (0.63 nM) in a cellular (HEK293) WNT/β-catenin signaling reporter assay[1].
OM-153 significantly inhibits the growth of COLO 320DM cells at GI50 values of 10 nM and GI25 values of 2.5 nM (concentrations that result in 50% and 25% growth inhibition, respectively), but has no effect on the growth of RKO cells[2]. OM-153 exhibits an antiproliferative effect and inhibits WNT/β-catenin, YAP, and MYC signaling in human cancer cell lines[2]. |
| ln Vivo |
OM-153 (0.1–10 mg/kg; p.o.; twice daily; for 34 days) decreases WNT/β-catenin signaling and tumor progression in COLO 320DM colon carcinoma xenografts[2].
OM-153 enhances anti-PD-1 immune checkpoint inhibition and antitumor effect in a B16-F10 mouse melanoma model[2]. |
| Animal Protocol |
CB17-SCID mice bearing COLO 320DM cells
10 mg/kg, 3.3 mg/kg, 1 mg/kg, 0.33 mg/kg, or 0.1 mg/kg p.o.; twice daily; for 34 days |
| References |
| Molecular Formula |
C28H24FN7O2
|
|---|---|
| Molecular Weight |
509.53
|
| Exact Mass |
509.2
|
| CAS # |
2406278-81-5
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| Appearance |
Powder
|
| SMILES |
CCOC1=CN=C(C=C1)C2=NN=C(N2C3=CC=CC=C3F)C4CC(C4)NC(=O)C5=C6C(=CC=C5)N=CC=N6
|
| InChi Key |
ARCOJIXZDJYBCH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H24FN7O2/c1-2-38-19-10-11-23(32-16-19)27-35-34-26(36(27)24-9-4-3-7-21(24)29)17-14-18(15-17)33-28(37)20-6-5-8-22-25(20)31-13-12-30-22/h3-13,16-18H,2,14-15H2,1H3,(H,33,37)
|
| Chemical Name |
N-[3-[5-(5-ethoxypyridin-2-yl)-4-(2-fluorophenyl)-1,2,4-triazol-3-yl]cyclobutyl]quinoxaline-5-carboxamide
|
| Synonyms |
OM-153
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~196.3 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (4.91 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9626 mL | 9.8130 mL | 19.6259 mL | |
| 5 mM | 0.3925 mL | 1.9626 mL | 3.9252 mL | |
| 10 mM | 0.1963 mL | 0.9813 mL | 1.9626 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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