LY2606368

• CAT Number: I000926
• CAS Number: 1234015-52-1
• Molecular Formula: C18H19N7O2
• Molecular Weight: 365.4
• Purity: ≥95%
• Target: Chk
• Solubility: DMSO: ≥ 60 mg/mL
• Storage: Store at -20C
• IC50: 1.5 nM (SW1990 cell line) [1]
• IUPAC Name: 5-[[5-[2-(3-aminopropoxy)-6-methoxyphenyl]-1H-pyrazol-3-yl]amino]pyrazine-2-carbonitrile
• InChI: InChI=1S/C18H19N7O2/c1-26-14-4-2-5-15(27-7-3-6-19)18(14)13-8-16(25-24-13)23-17-11-21-12(9-20)10-22-17/h2,4-5,8,10-11H,3,6-7,19H2,1H3,(H2,22,23,24,25)
• InChIKey: DOTGPNHGTYJDEP-UHFFFAOYSA-N
• SMILES: COC1=C(C(=CC=C1)OCCCN)C2=CC(=NN2)NC3=NC=C(N=C3)C#N

LY2606368(CAT: I000926) is a small molecule inhibitor of checkpoint kinase 1 (CHK1) with potential antineoplastic activity. CHK1 is a serine/threonine kinase that is essential for the DNA damage checkpoint pathway. Inhibition of CHK1 may lead to cell cycle arrest and enhanced cell death in cancer cells. LY2606368 has been studied in preclinical and clinical studies for the treatment of various types of cancer, including solid tumors and hematological malignancies.

Overview of Clinical Research

LY2606368 is considered as Checkpoint kinase 1 inhibitor. The preclinical trails in head and neck cancer in USA finished in 2020.

Reference

1. Wenjuan Wu, et al. Abstract 1776: Antitumor activity of Chk1 inhibitor LY2606368 as a single agent in SW1990 human pancreas orthotopic tumor model. Cancer Res April 15, 2012; 72(8 Supplement): 1776
2.King, Constance, et al. "LY2606368 causes replication catastrophe and antitumor effects through CHK1-dependent mechanisms." Molecular cancer therapeutics 14.9 (2015): 2004-2013.
3.McNeely, Samuel C., et al. "Abstract A108: LY2606368, a second generation Chk1 inhibitor, inhibits growth of ovarian carcinoma xenografts either as monotherapy or in combination with standard-of-care agents." (2011): A108-A108.