Molecular Formula | C23H22ClN5O |
Molar Mass | 419.91 |
Density | 1.46 |
Storage Condition | -20℃ |
In vitro study | CHIR-124 is a small quinolone molecule that is structurally unrelated to other known Chk1 inhibitors. CHIR-124 and topoisomerase toxicants (eg, Camptothecin or SN-38) work synergistically to inhibit the growth of a variety of cancer cell lines, including breast (MDA-MB-231 and MDA-MB-435) and colon (SW-620 and Colo205), these tumors all have p53 mutations. CHIR-124 acts on MDA-MD-435 breast cancer cells, abrogating SN-38-induced S-and G2-M-phase checkpoints, and enhancing apoptosis. p53 deletion enhances CHIR-124 resulting in G2-M checkpoint abrogation and induction of apoptosis. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.381 ml | 11.907 ml | 23.815 ml |
5 mM | 0.476 ml | 2.381 ml | 4.763 ml |
10 mM | 0.238 ml | 1.191 ml | 2.381 ml |
5 mM | 0.048 ml | 0.238 ml | 0.476 ml |
biological activity | CHIR-124 is a novel potent Chk1 inhibitor with an IC50 of 0.3 nM in a cell-free assay. The selectivity was 2000-fold higher than that for Chk2 and 500 to 5000-fold higher than that for CDK2/4 and Cdc2. |
Target | Value |
Chk1 (Cell-free assay) | 0.3 nM |
FLT3 (Cell-free assay) | 5.8 nM |
PDGFR (Cell-free assay) | 6.6 nM |
GSK-3 (Cell-free assay) | 23.3 nM |