M3814 (MSC2490484A)
Nedisertib
CAS: 1637542-33-6
Molecular Formula: C24H21ClFN5O3
M3814 (MSC2490484A) - Names and Identifiers
M3814 (MSC2490484A) - Physico-chemical Properties
| Molecular Formula | C24H21ClFN5O3 |
| Molar Mass | 481.91 |
| Density | 1.405±0.06 g/cm3(Predicted) |
| Melting Point | >198°C (dec.) |
| Boling Point | 716.0±60.0 °C(Predicted) |
| Solubility | Soluble in DMSO |
| Appearance | Solid |
| Color | Pale Yellow to Light Green |
| pKa | 11.35±0.20(Predicted) |
| Storage Condition | -20°C Freezer |
| Use | Nedisertib (M3814, Peposertib, MSC2490484A) is an orally bioavailable, highly potent and selective inhibitor of DNA activated protein kinase (DNA-PK) with IC50 of < 3 nM |
| Target | DNA-PK |
M3814 (MSC2490484A) - Reference
| Reference Show more | 1: Fu YW, Dai XY, Wang WT, Yang ZX, Zhao JJ, Zhang JP, Wen W, Zhang F, Oberg KC, Zhang L, Cheng T, Zhang XB. Dynamics and competition of CRISPR-Cas9 ribonucleoproteins and AAV donor-mediated NHEJ, MMEJ and HDR editing. Nucleic Acids Res. 2021 Jan 25;49(2):969-985. doi: 10.1093/nar/gkaa1251. PMID: 33398341; PMCID: PMC7826255. 2: van Bussel MTJ, Awada A, de Jonge MJA, Mau-Sørensen M, Nielsen D, Schöffski P, Verheul HMW, Sarholz B, Berghoff K, El Bawab S, Kuipers M, Damstrup L, Diaz- Padilla I, Schellens JHM. A first-in-man phase 1 study of the DNA-dependent protein kinase inhibitor peposertib (formerly M3814) in patients with advanced solid tumours. Br J Cancer. 2021 Feb;124(4):728-735. doi: 10.1038/s41416-020-01151-6. Epub 2020 Nov 24. PMID: 33230210; PMCID: PMC7884679. 3: Wu ZX, Peng Z, Yang Y, Wang JQ, Teng QX, Lei ZN, Fu YG, Patel K, Liu L, Lin L, Zou C, Chen ZS. M3814, a DNA-PK Inhibitor, Modulates ABCG2-Mediated Multidrug Resistance in Lung Cancer Cells. Front Oncol. 2020 May 12;10:674. doi: 10.3389/fonc.2020.00674. PMID: 32477940; PMCID: PMC7235170. 4: Zenke FT, Zimmermann A, Sirrenberg C, Dahmen H, Kirkin V, Pehl U, Grombacher T, Wilm C, Fuchss T, Amendt C, Vassilev LT, Blaukat A. Pharmacologic Inhibitor of DNA-PK, M3814, Potentiates Radiotherapy and Regresses Human Tumors in Mouse Models. Mol Cancer Ther. 2020 May;19(5):1091-1101. doi: 10.1158/1535-7163.MCT-19-0734. Epub 2020 Mar 27. PMID: 32220971. |
M3814 (MSC2490484A) - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.075 ml | 10.375 ml | 20.751 ml |
| 5 mM | 0.415 ml | 2.075 ml | 4.15 ml |
| 10 mM | 0.208 ml | 1.038 ml | 2.075 ml |
| 5 mM | 0.042 ml | 0.208 ml | 0.415 ml |
Last Update：2024-01-02 23:10:35
M3814 (MSC2490484A) - Animal Experiment
The efficacy of Nedisertib in combination with IR is evaluated in 6 human xenograft models (NCI-H460, A549, HCT116, FaDu, 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 mm^3 ). 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 .
Last Update：2023-08-16 21:32:38
M3814 (MSC2490484A) - Introduction
Nedisertib is a novel small molecule inhibitor commonly used in cancer therapy. Its chemical structure is similar to that of natural products such as mitomycin (paclitaxel) and nortrimefacine (vincristine).
Nedisertib can inhibit cell proliferation and division by inhibiting intracellular Aurora kinase. Aurora kinases are a class of kinases that regulate the process of cell mitosis, and their abnormal activity is often associated with the occurrence and development of tumors. Therefore, Nedisertib, as an Aurora kinase inhibitor, is widely studied as an anti-tumor drug.
Nedisertib synthesis methods generally use organic synthetic chemical methods, but the details of its specific preparation method may be subject to exclusive rights. In general, the preparation method requires specialized chemical synthesis experimental equipment and techniques, and may require multiple steps from the starting material to the final product.
No nonclinical and clinical study results have been publicly reported regarding the safety of Nedisertib. However, as a candidate therapeutic drug in the drug development process, its use safety is generally verified by Drug Toxicology and safety evaluation studies. Prior to clinical trials, Nedisertib is subjected to rigorous toxicological assessment to determine its toxicity and safety parameters.
However, it should be emphasized that the use of any drug needs to follow the doctor's advice. If you are interested in Nedisertib or any drug, you should consult a professional medical specialist for more specific and accurate information.
Nedisertib can inhibit cell proliferation and division by inhibiting intracellular Aurora kinase. Aurora kinases are a class of kinases that regulate the process of cell mitosis, and their abnormal activity is often associated with the occurrence and development of tumors. Therefore, Nedisertib, as an Aurora kinase inhibitor, is widely studied as an anti-tumor drug.
Nedisertib synthesis methods generally use organic synthetic chemical methods, but the details of its specific preparation method may be subject to exclusive rights. In general, the preparation method requires specialized chemical synthesis experimental equipment and techniques, and may require multiple steps from the starting material to the final product.
No nonclinical and clinical study results have been publicly reported regarding the safety of Nedisertib. However, as a candidate therapeutic drug in the drug development process, its use safety is generally verified by Drug Toxicology and safety evaluation studies. Prior to clinical trials, Nedisertib is subjected to rigorous toxicological assessment to determine its toxicity and safety parameters.
However, it should be emphasized that the use of any drug needs to follow the doctor's advice. If you are interested in Nedisertib or any drug, you should consult a professional medical specialist for more specific and accurate information.
Last Update：2024-04-09 21:54:55
Supplier List
Spot supply
Product Name: Nedisertib Visit Supplier Webpage Request for quotationCAS: 1637542-33-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: Nedisertib Visit Supplier Webpage Request for quotationCAS: 1637542-33-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History