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Background Information:
CC-671 is a potent and selective dual inhibitor of TTK (Human Protein Kinase Monopolar Spindle 1 (hMps1)) / CLK2 (CDC2-like Kinase), with IC50 values of 5 nM and 3 nM, respectively (ref 1), a unique feature targeting both TTK (mitotic exit) and CLK2 (mRNA splicing). It displays a strong single agent in vivo antitumor efficacy in multiple TNBC (Triple negative breast cancer) xenograft models (ref 1, 2). It is currently in IND-enabling studies as a single agent TNBC therapy.
Reference:
1. Jennifer R. Riggs, et al, The Discovery of a Dual TTK Protein Kinase/CDC2-Like Kinase (CLK2) Inhibitor for the Treatment of Triple Negative Breast Cancer Initiated from a Phenotypic Screen, J. Med. Chem., 2017, 60 (21), pp 8989–9002.
2. D. Zhu, et al, Synthetic lethal approach identifies potent and selective TTK and CLK inhibitor with preclinical anticancer activity in triple-negative breast cancer model: Proceedings of the AACR-NCI-EORTC International Conference: Molecular Targets and Cancer Therapeutics; 2017 Oct 26-30; Philadelphia, PA. Philadelphia (PA): AACR; Mol Cancer Ther 2018;17(1 Suppl):Abstract No B177.
APIM050028: CC-671
CAS No.: 1618658-88-0.
Molecular Formula: C28H28N6O4.
Molecular Weight: 512.6.
Purity: 99.5% purity by HPLC.
QC: HPLC-MS, NMR, and Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
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