For research use only. Not for therapeutic Use.
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].
Nedisertib (Compound 136) is a potent and selective inhibitor of DNA-PK,? with an IC50 of <3 nM for DNA-PK and <0.5 μΜ for cellular pDNA-PK[3].
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].
| Catalog Number | I046315 |
| CAS Number | 1637542-33-6 |
| Synonyms | (S)-[2-chloro-4-fluoro-5-(7-morpholin-4-ylquinazolin-4-yl)phenyl]-(6-methoxypyridazin-3-yl)methanol |
| Molecular Formula | C24H21ClFN5O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H21ClFN5O3/c1-33-22-5-4-20(29-30-22)24(32)16-11-17(19(26)12-18(16)25)23-15-3-2-14(10-21(15)27-13-28-23)31-6-8-34-9-7-31/h2-5,10-13,24,32H,6-9H2,1H3/t24-/m0/s1 |
| InChIKey | MOWXJLUYGFNTAL-DEOSSOPVSA-N |
| SMILES | COC1=NN=C(C=C1)C(C2=C(C=C(C(=C2)C3=NC=NC4=C3C=CC(=C4)N5CCOCC5)F)Cl)O |
| Reference | [1]. L. Damstrup, et al. M3814, a DNA-dependent Protein Kinase Inhibitor (DNA-PKi), Potentiates the Effect of Ionizing Radiation (IR) in Xenotransplanted Tumors in Nude Mice. IJROBP. 2016; 94, 940-941. [2]. Frank T. Zenke, et al. Abstract 1658: M3814, a novel investigational DNA-PK inhibitor: enhancing the effect of fractionated radiotherapy leading to complete regression of tumors in mice. AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 1658. [3]. Thomas Fuchss, et al. Arylchinazoline. WO2014183850A1. |
