For research use only. Not for therapeutic Use.
MK-4965（Cat No.:I008068）is an investigational small molecule being developed by Merck for the treatment of cancer. It is a selective inhibitor of the protein CHK1 (Checkpoint Kinase 1), which plays a crucial role in regulating cell cycle checkpoints and DNA repair mechanisms. By inhibiting CHK1, MK-4965 aims to disrupt the DNA damage response in cancer cells, making them more vulnerable to DNA-damaging agents like chemotherapy and radiation. Preclinical studies suggest that MK-4965 could enhance the efficacy of existing cancer therapies, though further clinical trials are needed to evaluate its safety and effectiveness.
| Catalog Number | I008068 |
| CAS Number | 920035-77-4 |
| Synonyms | MK4965; MK 4965; MK-4965;3-(5-((6-amino-1H-pyrazolo[3,4-b]pyridin-3-yl)methoxy)-2-chlorophenoxy)-5-chlorobenzonitrile |
| Molecular Formula | C20H13Cl2N5O2 |
| Purity | ≥95% |
| Solubility | Soluble in DMSO, not in water |
| Storage | 0 - 4 °C for short term, or -20 °C for long term |
| IUPAC Name | 3-[5-[(6-amino-2H-pyrazolo[3,4-b]pyridin-3-yl)methoxy]-2-chlorophenoxy]-5-chlorobenzonitrile |
| InChI | InChI=1S/C20H13Cl2N5O2/c21-12-5-11(9-23)6-14(7-12)29-18-8-13(1-3-16(18)22)28-10-17-15-2-4-19(24)25-20(15)27-26-17/h1-8H,10H2,(H3,24,25,26,27) |
| InChIKey | KXDIHAQCVNNLIB-UHFFFAOYSA-N |
| SMILES | C1=CC(=C(C=C1OCC2=C3C=CC(=NC3=NN2)N)OC4=CC(=CC(=C4)C#N)Cl)Cl |
| Reference | </br>1:Antiviral activity of MK-4965, a novel nonnucleoside reverse transcriptase inhibitor. Lai MT, Munshi V, Touch S, Tynebor RM, Tucker TJ, McKenna PM, Williams TM, DiStefano DJ, Hazuda DJ, Miller MD.Antimicrob Agents Chemother. 2009 Jun;53(6):2424-31. doi: 10.1128/AAC.01559-08. Epub 2009 Mar 16. PMID: 19289522 Free PMC Article</br>2:Discovery of 3-{5-[(6-amino-1H-pyrazolo[3,4-b]pyridine-3-yl)methoxy]-2-chlorophenoxy}-5-chlorobenzonitrile (MK-4965): a potent, orally bioavailable HIV-1 non-nucleoside reverse transcriptase inhibitor with improved potency against key mutant viruses. Tucker TJ, Sisko JT, Tynebor RM, Williams TM, Felock PJ, Flynn JA, Lai MT, Liang Y, McGaughey G, Liu M, Miller M, Moyer G, Munshi V, Perlow-Poehnelt R, Prasad S, Reid JC, Sanchez R, Torrent M, Vacca JP, Wan BL, Yan Y.J Med Chem. 2008 Oct 23;51(20):6503-11. doi: 10.1021/jm800856c. Epub 2008 Oct 1. PMID: 18826204 |
