2. Cell Cycle/DNA Damage Epigenetics Stem Cell/Wnt
  3. PARP Wnt
  4. OM-153

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.

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OM-153 Chemical Structure

OM-153 Chemical Structure

CAS No. : 2406278-81-5

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Based on 1 publication(s) in Google Scholar

OM-153 Related Antibodies

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  • Purity & Documentation

  • References

  • Customer Review

Description

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].

IC50 & Target[1][2]

TNKS1

13 nM (IC50)

TNKS2

2 nM (IC50)

Wnt/β-catenin

0.63 nM (IC50)

In Vitro

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 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

509.53

Formula

C28H24FN7O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.59%

COA (253 KB) HNMR (142 KB) RP-HPLC (155 KB)

Handling Instructions (2659 KB)
References

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
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OM-153 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

OM-1532406278-81-5OM153OM 153PARPWntpoly ADP ribose polymeraseTNKS1TNKS2HEK293WNT/β-catenin signalingcell growthcolon cancer cell lineCOLO 320DMInhibitorinhibitorinhibit

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