XRD-0394
Based on 1 Customer Validation
XRD-0394 is a potent and orally active dual ATM and DNA-PKcs inhibitor with IC50s of 0.39 nM and 0.89 nM, respectively. XRD-0394 shows selectivity over other PIKK and PI3K family members. XRD-0394 significantly enhances tumor cell killing in vitro and in vivo under therapeutic ionizing radiation conditions. XRD-0394 can potentiate the effects of PARP and topoisomerase I inhibitors in vitro.
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- Reinheit: 98.54%
- CAS. Nr.: 2595308-10-2
- Formel: C26H30FN5O4S
- Molecular Weight:527.61
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
XRD-0394 (20 nM, 100 nM, 500 nM, 1000 nM; pretreated with 30 minutes and then irradiated with 0-10 Gy for 1 hour) inhibits phosphorylation by ATM and DNA-PK kinases, but not structurally related kinases in MCF7 human tumor cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF7 human breast cancer cells
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Concentration:20 nM, 100 nM, 500 nM, 1000 nM
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Incubation Time:Pretreated with 30 minutes and then irradiated with 0 or 10 Gy (IR) for 1 hour
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Result:Showed potent, dose-dependent inhibition of IR-induced phosphorylation of DNA-PKcs (S2056) and ATM (S1981) and the ATM substrate KAP1 (Ser824), with no change in total ATM and DNA-PKcs protein levels.
Pharmacokinetic analyses show that 10 mg/kg XRD-0394 (oral gavage) resulted in plasma concentration of 840-1,125 ng/mL (1.6-2.1 mM) for 4 hours before declining to undetectable levels by 24 hours 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:Female NCr nu/nu mice [Crl:NU(NCr)-Foxn1nu, Strain 490] were used for MDA-MB-321 subcutaneous tumor implantation, alone or in combination with focal irradiation[1].
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Dosage:3 mg/kg, 6 mg/kg, 10 mg/kg (0.5% HPMC and 0.2% Tween80)
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Administration:Oral gavage; once daily; for 3 consecutive days
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Result:Inhibited phosphorylation of the ATM substrate, KAP1, and autophosphorylation of DNA-PK.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 2595308-10-2
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Appearance Solid
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Molecular Weight 527.61
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Formel C26H30FN5O4S
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Color Light yellow to brown
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SMILES
O=C(C12CCC2)N(C)C3=C1C4=CC(C5=CN=C(OCCNC(C)C)C(NS(C)(=O)=O)=C5)=C(F)C=C4N=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 4.17 mg/mL (7.90 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)
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (273 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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Handling Instructions (2659 KB)
Verweise
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 | 1.8953 mL | 9.4767 mL | 18.9534 mL | 47.3835 mL |
| 5 mM | 0.3791 mL | 1.8953 mL | 3.7907 mL | 9.4767 mL |
XRD-0394 Related Classifications
HY-162472 Related Classifications
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