Molecular Formula | C18H19N7O2 |
Molar Mass | 365.39 |
Density | 1.37±0.1 g/cm3(Predicted) |
Boling Point | 608.5±55.0 °C(Predicted) |
Solubility | Soluble in DMSO |
pKa | 11.89±0.10(Predicted) |
Storage Condition | -20℃ |
Use | Prexasertib, also know LY2606368, is a n inhibitor of checkpoint kinase 1 (chk1) with potential antineoplastic activity. Upon administration, LY2606368 selectively binds to chk1, thereby preventing activity of chk1 and abrogating the repair of damaged DNA. This may lead to an accumulation of damaged DNA and may promote genomic instability and apoptosis. LY2606368 may potentiate the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapeutic agents. |
Reference Show more | 1: Koppenhafer SL, Goss KL, Terry WW, Gordon DJ. mTORC1/2 and protein translation regulate levels of CHK1 and the sensitivity to CHK1 inhibitors in Ewing sarcoma cells. Mol Cancer Ther. 2018 Oct 3. pii: molcanther.0260.2018. doi: 10.1158/1535-7163.MCT-18-0260. [Epub ahead of print] PubMed PMID: 30282812. 2: Iwasa S, Yamamoto N, Shitara K, Tamura K, Matsubara N, Tajimi M, Lin AB, Asou H, Cai Z, Inoue K, Shibasaki Y, Saito K, Takai H, Doi T. Dose-finding study of the checkpoint kinase 1 inhibitor, prexasertib, in Japanese patients with advanced solid tumors. Cancer Sci. 2018 Oct;109(10):3216-3223. doi: 10.1111/cas.13750. PubMed PMID: 30040168. 3: Zhong B, Maharaj A, Davis A, Roussel MF, Stewart CF. Development and validation of a sensitive LC MS/MS method for the measurement of the checkpoint kinase 1 inhibitor prexasertib and its application in a cerebral microdialysis study. J Pharm Biomed Anal. 2018 Jul 15;156:97-103. doi: 10.1016/j.jpba.2018.04.018. Epub 2018 Apr 17. PubMed PMID: 29698863; PubMed Central PMCID: PMC5984718. 4: Hong DS, Moore K, Patel M, Grant SC, Burris HA 3rd, William WN Jr, Jones S, Meric-Bernstam F, Infante J, Golden L, Zhang W, Martinez R, Wijayawardana S, Beckmann R, Lin AB, Eng C, Bendell J. Evaluation of Prexasertib, a Checkpoint Kinase 1 Inhibitor, in a Phase Ib Study of Patients with Squamous Cell Carcinoma. Clin Cancer Res. 2018 Jul 15;24(14):3263-3272. doi: 10.1158/1078-0432.CCR-17-3347. Epub 2018 Apr 11. PubMed PMID: 29643063; PubMed Central PMCID: |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.737 ml | 13.684 ml | 27.368 ml |
5 mM | 0.547 ml | 2.737 ml | 5.474 ml |
10 mM | 0.274 ml | 1.368 ml | 2.737 ml |
5 mM | 0.055 ml | 0.274 ml | 0.547 ml |