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Chemical Structure : Multikinase inhibitor 108600
Catalog No.: PC-72647Not For Human Use, Lab Use Only.
Multikinase inhibitor 108600 (108600) is a novel multi-kinase inhibitor and inhibitor of TNBC growth (GI50=0.12-0.75 uM), inhibits CK2α1/α2, DYRK1A, 1B, and DYRK2 and TNIK (IC50=5-50 nM).
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Multikinase inhibitor 108600 (ON 108600) is a novel multi-kinase inhibitor and inhibitor of TNBC growth (GI50=0.12-0.75 uM), inhibits CK2α1/α2, DYRK1A, 1B, and DYRK2 and TNIK (IC50=5-50 nM).
108600 decreased phosphorylation AKT1 Serine 129, CYCLIN D1 Thr 286 and p27 Ser10 in MDA-MB231 and Hs578T cells, as well as decreased levels of autophosphorylated DYRK1A/B, supressed AXIN2 expression induced by activated Wnt/TCF/LEF.
108600 inhibits viability of TNBC CD44high/CD24low breast cancer stem cells.
108600 binds to CK2α1 and induce a conformational change, which represents a state that is not conducive to holoenzyme formation.
108600 inhibits tubulin polymerization and causes abnormal mitosis in HeLa cells, induces G2/M arrest and apoptosis of TNBC cells and organoids, suppresses the growth of chemotherapy-resistant TNBC cells.
108600 (100 mg/kg) suppresses growth of TNBC cell line and PDX tumor grafts as a single dose or in combination with chemotherapy, synergizes paclitaxel to inhibit established TNBC metastases in vivo.
| M.Wt | 537.382 | |
| Formula | C22H14Cl2N2O6S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Katsutoshi Sato, et al. Nat Commun. 2021 Aug 3;12(1):4671.
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