LY-2603618 is an inhibitor of checkpoint kinase 1 (Chk1) that exhibits anticancer chemotherapeutic activity. In various animal models with tumor xenografts, this compound inhibits the S phase DNA damage checkpoint and increases DNA damage. In lung cancer cells, LY-2603618 induces G2/M phase cell cycle arrest and autophagy. LY-2603618 also enhances activity of other co-administered chemotherapeutics such as gemcitabine.
| Cas No. | 911222-45-2 |
|---|---|
| Purity | ≥98% |
| Formula | C18H22BrN5O3 |
| Formula Wt. | 436.31 |
| IUPAC Name | 1-{5-Bromo-4-methyl-2-[(2S)-2-morpholinylmethoxy]phenyl}-3-(5-methyl-2-pyrazinyl)urea |
| Synonym | Rabusertib |
| Solubility | 13mg/mL in DMSO, insoluble in water and ethanol |
| Store Temp | -20°C |
|---|---|
| Ship Temp | Ambient |
| MSDS | |
|---|---|
| Info Sheet |
Barnard D, Diaz HB, Burke T, et al. LY2603618, a selective CHK1 inhibitor, enhances the anti-tumor effect of gemcitabine in xenograft tumor models. Invest New Drugs. 2015 Nov 27. [Epub ahead of print]. PMID: 26612134.
Wang FZ, Fei HR, Cui YJ, et al. The checkpoint 1 kinase inhibitor LY2603618 induces cell cycle arrest, DNA damage response and autophagy in cancer cells. Apoptosis. 2014 Sep;19(9):1389-98. PMID: 24928205.
King C, Diaz H, Barnard D, et al. Characterization and preclinical development of LY2603618: a selective and potent Chk1 inhibitor. Invest New Drugs. 2014 Apr;32(2):213-26. PMID: 24114124.
