Polθ-IN-4
Based on 1 Customer Validation
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.
- Purity: 98.71%
- CAS No.: 3043810-73-4
- Formula: C17H17ClN5O7PS
- Molecular Weight:501.84
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Cell Cycle/DNA Damage Compound Library
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Anti-Cancer Compound Library
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Anti-Aging Compound Library
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Orally Active Compound Library
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Anti-Breast Cancer Compound Library
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Anti-Ovarian Cancer Compound Library
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Bioactive Compound Library Max
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MCE Bioactive Compound Library
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Bioactive Compound Library
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High-Efficiency Gene Editing Compound Library
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All DNA/RNA Synthesis Isoforms
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Biological Activity
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DNA Polymerase |
| Species | Dose | Route | Cmax | AUClast |
|---|---|---|---|---|
| Rat[1] | 30 mg/kg | i.g. | 14 μg/mL | 128 μg·h/mL |
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.
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Animal Model:134-T HR deficient PDX model established in mice[1]
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Dosage:1 mg/kg
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Administration:Oral administration (p.o.), once daily for 36 days
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Result:Demonstrated robust combination efficacy with Niraparib.
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Animal Model:TNBC MDA-MB 436 CDX model established in 5-7 weeks old NSG mice[1]
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Dosage:1 mg/kg
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Administration:Oral administration (p.o.), once daily (2 mg/kg) or twice daily (1 mg/kg) for 42 days
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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.
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Animal Model:HR deficient human cell line xenograft model established in female NOD SCID mice (6-8 weeks)[1]
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Dosage:1 mg/kg
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Administration:Oral administration (p.o.), once daily for 80 days
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Result:Produced a mean TV of 23.7 mm3 and 100% tumor regressions with Niraparib.
Chemical Information
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CAS No. 3043810-73-4
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Appearance Solid
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Molecular Weight 501.84
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Formula C17H17ClN5O7PS
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Color White to light yellow
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
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)
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)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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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 | 1.9927 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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