Nedisertib (GMP) (Peposertib (GMP)) is Nedisertib (HY-101570) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Nedisertib is an orally active selective DNA-dependent protein kinase (DNA-PK) inhibitor with an IC50 value of less than 3 nM. Nedisertib also acts as a modulator of ABCG2, capable of reversing ABCG2-mediated multidrug resistance (MDR), thus providing new strategies for combination therapy. By inhibiting DNA double-strand break repair, Nedisertib can enhance the efficacy of chemotherapy and radiotherapy. Nedisertib exhibits antitumor activity.
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- No. CAS: 1637542-33-6
- Fòrmula: C24H21ClFN5O3
- Peso molecular:481.91
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
In Vitro
Nedisertib (GMP) (0.3-1 µM; 72 h) significantly enhances the cytotoxicity of ABCG2 substrate drugs Mitoxantrone (HY-13502) and Doxorubicin (HY-15142A) in ABCG2-overexpressing lung cancer cell lines NCI-H460/MX20 and A549/MX10, reversing multidrug resistance[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6 human xenograft models (HCT116, FaDu, NCI-H460, A549, Capan-1, BxPC3) in mice representing 4 different cancer types (colon, head and neck, lung, and pancreas) treated ionizing radiation (IR)[2]
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Dosage:25-300 mg/kg
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Administration:Oral administration; single dose; 10 min prior to IR
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Result:Significantly inhibited tumor growth in all 6 models in combination with IR.
Induced tumor regression in FaDu and NCI-H460 models, and showed no tumor regrowth in the FaDu model with the combination of 25 and 50 mg/kg and IR (total 60 Gy).
Had no significant weight loss or visual signs of toxicity in mice.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1637542-33-6
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Peso molecular 481.91
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Fòrmula C24H21ClFN5O3
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SMILES
FC1=CC(Cl)=C([C@@H](C2=CC=C(N=N2)OC)O)C=C1C3=NC=NC4=C3C=CC(N5CCOCC5)=C4
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Synonyms
Peposertib (GMP); M3814 (GMP)
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Nedisertib (GMP) Related Classifications
HY-101570G Related Classifications
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