Tambiciclib (GFH009, JSH-009) dimaleate is an orally active, highly potent and selective CDK9 inhibitor ( IC 50 = 1 nM), demonstrating >200-fold selectivity over other CDKs, >100-fold selectivity over DYRK1A / B , and excellent selectivity over 468 kinases/mutants. Tambiciclib dimaleate demonstrates potent in vitro and in vivo antileukemic efficacy in acute myeloid leukemia (AML) mouse models by inhibiting RNA Pol II phosphorylation, downregulating MCL1 and MYC , and inducing apoptosis . Tambiciclib dimaleate can be used for AML research.
Products | Products > Disease Areas > Cancer | Products > Signaling Pathways > Cell Cycle/DNA Damage | Products > Signaling Pathways > Protein Tyrosine Kinase/RTK | Products > Signaling Pathways > Apoptosis | Products > Signaling Pathways > Epigenetics | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Signaling Pathways > c-Myc | Products > Signaling Pathways > Caspase | Products > Signaling Pathways > PARP | Products > Signaling Pathways > DNA/RNA Synthesis | Products > Signaling Pathways > CDK | Products > Signaling Pathways > DYRK | Products > Signaling Pathways > Apoptosis | Products > Signaling Pathways > Bcl-2 Family
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