2. Cell Cycle/DNA Damage
  3. DNA/RNA Synthesis
  4. Polθ-IN-4

Polθ-IN-4 is an orally active prodrug of a DNA polymerase θ (Polθ) inhibitor with Kms of 3.7, 3.7 and 5.2 μM in human, mouse and rat recombinant alkaline phosphatases. Polθ-IN-4 that inhibits Polθ activity by targeting its ATP-dependent helicase domain. Polθ-IN-4 demonstrates significant anti-tumor activity in multiple animal experiments. Polθ-IN-4 can be used for the studies of breast cancer and ovarian cancer.

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

Polθ-IN-4

Polθ-IN-4 Chemical Structure

CAS No. : 3043810-73-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

Polθ-IN-4 Related Antibodies

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Description

Polθ-IN-4 is an orally active prodrug of a DNA polymerase θ (Polθ) inhibitor with Kms of 3.7, 3.7 and 5.2 μM in human, mouse and rat recombinant alkaline phosphatases. Polθ-IN-4 that inhibits Polθ activity by targeting its ATP-dependent helicase domain. Polθ-IN-4 demonstrates significant anti-tumor activity in multiple animal experiments. Polθ-IN-4 can be used for the studies of breast cancer and ovarian cancer[1].

Parmacokinetics[1]
Species Dose Route Indicator value
Rat 30 mg/kg i.g. Cmax 14 μg/mL
Rat 30 mg/kg i.g. AUClast 128 μg·h/mL
In Vivo

Polθ-IN-4 (Example 1) (1 mg/kg, twice daily for 36 days) demonstrates robust combination efficacy with Niraparib (HY-10619) in 134-T HR deficient PDX model in mice[1].
Polθ-IN-4 (1-2 mg/kg, p.o., once or twice daily for 42 days) induces a significant but modest monotherapy 31% tumor growth inhibition in TNBC MDA-MB 436 CDX model in mice[1].
Polθ-IN-4 (1 mg/kg, p.o., twice daily for 80 days) combined Niraparib produces 100% tumor regressions in HR deficient human cell line xenograft model MDA-MB-436 in mice[1].
Polθ-IN-4 (1 mg/kg, p.o., twice daily at 21 and 27 days) significantly delays disease progression with Niraparib in 031-T PDX and 134-T PDX tumors progressing in mice[1].

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

Animal Model: 134-T HR deficient PDX model established in mice[1]
Dosage: 1 mg/kg
Administration: Oral administration (p.o.), once daily for 36 days
Result: Demonstrated robust combination efficacy with Niraparib.
Animal Model: TNBC MDA-MB 436 CDX model established in 5-7 weeks old NSG mice[1]
Dosage: 1 mg/kg
Administration: Oral administration (p.o.), once daily (2 mg/kg) or twice daily (1 mg/kg) for 42 days
Result: Induced a significant but modest monotherapy 31% tumor growth and in combination with Olaparib (HY-10162) induced significant tumor volume difference with 96% TGI at day 42.
Animal Model: HR deficient human cell line xenograft model established in female NOD SCID mice (6-8 weeks)[1]
Dosage: 1 mg/kg
Administration: Oral administration (p.o.), once daily for 80 days
Result: Produced a mean TV of 23.7 mm3 and 100% tumor regressions with Niraparib.
Molecular Weight

501.84

Formula

C17H17ClN5O7PS
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

ClC1=NC=C(OC)C(C2=C(C(/N=C3N(COP(O)(O)=O)N=C(OC)S/3)=O)C=NC(C)=C2)=C1
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 : 17.5 mg/mL (34.87 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 1.9927 mL 9.9633 mL 19.9267 mL
5 mM 0.3985 mL 1.9927 mL 3.9853 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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

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g

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
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 1.9927 mL 9.9633 mL 19.9267 mL 49.8167 mL
5 mM 0.3985 mL 1.9927 mL 3.9853 mL 9.9633 mL
10 mM 0.1993 mL 0.9963 mL 1.9927 mL 4.9817 mL
15 mM 0.1328 mL 0.6642 mL 1.3284 mL 3.3211 mL
20 mM 0.0996 mL 0.4982 mL 0.9963 mL 2.4908 mL
25 mM 0.0797 mL 0.3985 mL 0.7971 mL 1.9927 mL
30 mM 0.0664 mL 0.3321 mL 0.6642 mL 1.6606 mL
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Polθ-IN-4 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-IN-43043810-73-4DNA/RNA SynthesisPolθATP-dependent helicase domaincancerInhibitorinhibitorinhibit

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