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.
For research use only. We do not sell to patients.
- CAS No.: 1637542-33-6
- Formula: C24H21ClFN5O3
- Molecular Weight:481.91
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
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. Further protocols information, click here.
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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1637542-33-6
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Molecular Weight 481.91
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)