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MedChemExpress - Model Nedisertib -1637542-33-6
Nedisertib (M3814) is a potent, orally available and selective inhibitor of DNA-PK, with an IC50 of <3 nM. Anti-tumor activity[1][2][3].MCE products for research use only. We do not sell to patients.
Nedisertib
MCE China：Nedisertib
Brand：MedChemExpress (MCE)
Cat. No.HY-101570
CAS：1637542-33-6
Synonyms：Peposertib; M3814
Purity：99.70%
Storage：-20°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Shipping：Room temperature in continental US; may vary elsewhere.
Description：Nedisertib (M3814) is a potent, orally available and selective inhibitor of DNA-PK, with an IC50 of <3 nM. Anti-tumor activity.
In Vitro：Nedisertib (Compound 136) is a potent and selective inhibitor of DNA-PK,? with an IC50 of DNA-PK and [3].
In Vivo：In combination with IR, Nedisertib shows efficacy in all of the 6 mouse models of human cancer. In all models, a dose of 2 Gy administered daily for 1 week in combination with Nedisertib induces statically significant tumor growth inhibition compare to IR alone. Nedisertib, alone or in combination with IR, does not induce significant weight loss or visual signs of toxicity in the mice in any study[1].
Animal Administration：The efficacy of Nedisertib in combination with IR is evaluated in 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). Tumor cells are injected s.c. into nude mice, and treatment starts when palpable tumors are established (~100 to 200 mm3 ). Nedisertib is given orally at different doses (25 to 300 mg/kg) 10 min prior to IR. IR is applied using a radiation therapy device for small rodents calibrated to deliver 2 Gy. Autophosphorylation of DNA-PK (serine2056 ) in FaDu tumor lysates is measured by immunoassay to assess pharmacological inhibition by Nedisertib[1].
IC50 & Target：DNA-PK 50)
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References：
Brand introduction:
• MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
• More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
• The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
• Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
• It has a professional experimental center and strict quality control and verification system；
• Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
• The biological activity of the products has been verified by the experiments of customers in various countries；
• A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
• Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
• It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。