OM-153
Based on 1 Customer Validation
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.30%
- No. CAS: 2406278-81-5
- Fòrmula: C28H24FN7O2
- Peso molecular:509.53
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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TNKS1 13 nM (IC50) |
TNKS2 2 nM (IC50) |
Wnt/β-catenin 0.63 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| COLO 320DM | GI50 |
10 nM
Compound: 24; OM-153
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Antiproliferative activity against human COLO 320DM cells assessed as growth inhibition incubated for 5 days by MTS assay
Antiproliferative activity against human COLO 320DM cells assessed as growth inhibition incubated for 5 days by MTS assay
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[PMID: 34878777] |
| RKO | GI50 |
>10000 nM
Compound: 24; OM-153
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Antiproliferative activity against human RKO cells assessed as growth inhibition incubated for 5 days by MTS assay
Antiproliferative activity against human RKO cells assessed as growth inhibition incubated for 5 days by MTS assay
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[PMID: 34878777] |
OM-153 shows picomolar IC50 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[1].
OM-153 decreases cell growth in COLO 320DM cells with a GI50 value of 10 nM and a GI25 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[2].
OM-153 inhibits WNT/β-catenin, YAP, and MYC signaling and shows an antiproliferative fffect in human cancer cell lines[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
OM-153 potentiates anti-PD-1 immune checkpoint inhibition and antitumor effect in a B16-F10 mouse melanoma model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB17-SCID mice bearing COLO 320DM cells[2]
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Dosage:10 mg/kg, 3.3 mg/kg, 1 mg/kg, 0.33 mg/kg, or 0.1 mg/kg
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Administration:p.o.; twice daily; for 34 days
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Result:Reduced WNT/β-catenin signaling and tumor progression in COLO 320DM colon carcinoma xenografts.
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Animal Model:C57BL/6N mice injected with B16-F10 tumors[2]
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Dosage:10 mg/kg, 1 mg/kg, and 0.1 mg/kg
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Administration:p.o.; twice daily; for 20 days
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Result:Potentiated anti-PD-1 immune checkpoint inhibition and antitumor effect.
Chemical Information
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No. CAS 2406278-81-5
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Appearance Solid
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Peso molecular 509.53
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Fòrmula C28H24FN7O2
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Color Off-white to light yellow
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SMILES
O=C(C1=C2N=CC=NC2=CC=C1)N[C@H]3C[C@H](C4=NN=C(C5=NC=C(OCC)C=C5)[N@]4[C@]6=CC=CC=C6F)C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (196.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.91 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9626 mL | 9.8130 mL | 19.6259 mL | 49.0648 mL |
| 5 mM | 0.3925 mL | 1.9626 mL | 3.9252 mL | 9.8130 mL | |
| 10 mM | 0.1963 mL | 0.9813 mL | 1.9626 mL | 4.9065 mL | |
| 15 mM | 0.1308 mL | 0.6542 mL | 1.3084 mL | 3.2710 mL | |
| 20 mM | 0.0981 mL | 0.4906 mL | 0.9813 mL | 2.4532 mL | |
| 25 mM | 0.0785 mL | 0.3925 mL | 0.7850 mL | 1.9626 mL | |
| 30 mM | 0.0654 mL | 0.3271 mL | 0.6542 mL | 1.6355 mL | |
| 40 mM | 0.0491 mL | 0.2453 mL | 0.4906 mL | 1.2266 mL | |
| 50 mM | 0.0393 mL | 0.1963 mL | 0.3925 mL | 0.9813 mL | |
| 60 mM | 0.0327 mL | 0.1635 mL | 0.3271 mL | 0.8177 mL | |
| 80 mM | 0.0245 mL | 0.1227 mL | 0.2453 mL | 0.6133 mL | |
| 100 mM | 0.0196 mL | 0.0981 mL | 0.1963 mL | 0.4906 mL |
OM-153 Related Classifications
HY-145267 Related Classifications
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