2. Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. Apoptosis DNA/RNA Synthesis PARP
  4. Polθ/PARP-IN-1

Polθ/PARP-IN-1 (compound 25d) is a potent dual DNA polymerase theta (Polθ) and PARP inhibitor with IC50 values of 45.6, 5.4 nM, respectively. Polθ/PARP-IN-1 shows antiproliferative activity. Polθ/PARP-IN-1 induces apoptosis and cell cycle arrest at G2/M phase, causes DNA damage. Polθ/PARP-IN-1 shows anti-tumor activity.

For research use only. We do not sell to patients.

Polθ/PARP-IN-1 Chemical Structure

Polθ/PARP-IN-1 Chemical Structure

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 481 In-stock
Solution
10 mM * 1 mL in DMSO USD 481 In-stock
Solid
1 mg USD 144 In-stock
5 mg USD 360 In-stock
10 mg USD 580 In-stock
25 mg USD 1220 In-stock
50 mg USD 1950 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Polθ/PARP-IN-1 Related Antibodies

Top Publications Citing Use of Products

View All PARP Isoform Specific Products:

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Polθ/PARP-IN-1 (compound 25d) is a potent dual DNA polymerase theta (Polθ) and PARP inhibitor with IC50 values of 45.6, 5.4 nM, respectively. Polθ/PARP-IN-1 shows antiproliferative activity. Polθ/PARP-IN-1 induces apoptosis and cell cycle arrest at G2/M phase, causes DNA damage. Polθ/PARP-IN-1 shows anti-tumor activity[1].

In Vitro

Polθ/PARP-IN-1 (compound 25d) (0-80 µM; 3 days) shows antiproliferative activity with IC50s of 20.9, 2.7, 8.9, 2.9, 18.9, >80 µM for HCC1937, MDA-MB-436, HCT116, SW48, SKOV-3, MCF-10A cells, respectively[1].
Polθ/PARP-IN-1 (compound 25d) (2 µM; 3 days) induces apoptosis and cell cycle arrest at G2/M phase, causes DNA damage[1].

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

Polθ/PARP-IN-1 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HCC1937, MDA-MB-436, HCT116, SW48, SKOV-3, MCF-10A cells
Concentration: 0-80 µM
Incubation Time: 5 days
Result: Showed antiproliferative activity with IC50s of 20.9, 2.7, 8.9, 2.9, 18.9, >80 µM for HCC1937, MDA-MB-436, HCT116, SW48, SKOV-3, MCF-10A cells, respectively.

Apoptosis Analysis[1]

Cell Line: MDA-MB-436 cells
Concentration: 2 µM
Incubation Time: 3 days
Result: Induced apoptosis with a higher apoptosis rate (26.7%) and arrested cell cycle progression at the G2/M phase.
In Vivo

Polθ/PARP-IN-1 (20, 40 mg/kg; i.p.; daily for 21 consecutive days) inhibits tumor growth in MDA-MB-436 xenograft model[1].

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

Animal Model: 18-20 g, Six-week-old female BALB/C nude mice (MDA-MB-436 xenograft model)[1]
Dosage: 20, 40 mg/kg
Administration: I.p.; daily for 21 consecutive days
Result: Significantly inhibited the growth of MDA-MB-436 xenografts in a dose-dependent manner, exerted an optimal inhibitory potency with a tumor growth inhibition (TGI) rate of 54.4%, 74.7% at 20, 40 mg/kg, respectively.
Molecular Weight

754.23

Formula

C38H33ClFN7O5S
Appearance

Solid

Color

White to off-white

SMILES

COC1=CC=C(C=C1C2=CC(C)=NC=C2C(NC3=NN=C(S3)OCC4CCN(CC4)C(C5=C(C=CC(CC6=NNC(C7=C6C=CC=C7)=O)=C5)F)=O)=O)Cl
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 : 50 mg/mL (66.29 mM; ultrasonic and warming and heat to 60°C; 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 1.3259 mL 6.6293 mL 13.2586 mL
5 mM 0.2652 mL 1.3259 mL 2.6517 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)

Mass
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Concentration
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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)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (3.31 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (3.31 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
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 1.3259 mL 6.6293 mL 13.2586 mL 33.1464 mL
5 mM 0.2652 mL 1.3259 mL 2.6517 mL 6.6293 mL
10 mM 0.1326 mL 0.6629 mL 1.3259 mL 3.3146 mL
15 mM 0.0884 mL 0.4420 mL 0.8839 mL 2.2098 mL
20 mM 0.0663 mL 0.3315 mL 0.6629 mL 1.6573 mL
25 mM 0.0530 mL 0.2652 mL 0.5303 mL 1.3259 mL
30 mM 0.0442 mL 0.2210 mL 0.4420 mL 1.1049 mL
40 mM 0.0331 mL 0.1657 mL 0.3315 mL 0.8287 mL
50 mM 0.0265 mL 0.1326 mL 0.2652 mL 0.6629 mL
60 mM 0.0221 mL 0.1105 mL 0.2210 mL 0.5524 mL
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Polθ/PARP-IN-1 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:

Polθ/PARP-IN-1ApoptosisDNA/RNA SynthesisPARPpoly ADP ribose polymeraseMDA-MB-436 cellsanti-cancerG2/M phaseapoptosisantiproliferativeInhibitorinhibitorinhibit

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