Tanzisertib(CC-930) (C09-1074-455)

InformationTanzisertib(CC-930) Tanzisertib (CC-930, JNK-930, JNKI-1) is kinetically competitive with ATP in the JNK -dependent phosphorylation of the protein substrate c-Jun and potent against all isoforms of JNK (Ki(JNK1) = 44 ± 3 nM, IC50(JNK1) = 61 nM, Ki(JNK2) = 6.2 ± 0.6 nM, IC50(JNK2) = 5 nM, IC50(JNK3) = 5 nM) and selective against MAP kinases ERK1 and p38a with IC50 of 0.48 and 3.4 μM respectively.TargetsJNK3 (Cell-free assay); JNK2 (Cell-free assay); JNK1 (Cell-free assay) 0.006 μM; 0.007 μM; 0.061 μMIn vitroCC-930 inhibits the formation of phospho-cJun in human PBMC stimulated by phorbol-12-myristate-13-acetate and phytohemeagglutinin (IC50 = 1 μM). CC-930 shows remarkable selectivity in a panel of 240 kinases, EGFR being the only non-MAP kinase inhibited more than 50% at 3 μM (IC50 = 0.38 μM). It inhibits no receptor at greater than 50% at 10 μM concentration in a panel of 75 receptors, ion channels and neurotransmitter transporters. CC-930 does not inhibit CYP P450 enzymes significantly and is metabolized by CYP 3A4 and 2D6.In vivoIn the acute rat LPS-induced TNFα production PK-PD model, the compound inhibits the production of TNFα by 23% and 77% at 10 and 30 mg/kg oral dose respectively. CC-930 is well-tolerated and exposure is dose-proportional.Cell Research(from reference)Cell lines：Jurkat T cells Incubation Time：30 minutes. Specifications and Purity: 99%. Molecular Formula: C21H23F3N6O2.HCl. Molecular Weight: 484.9.