Tambiciclib (dimaleate) [CAS 2559759-04-3]

Tambiciclib (GFH009, JSH-009) dimaleate is an orally active, highly potent and selective CDK9 inhibitor (IC50 = 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[1].

[2559759-04-3]

C33H43ClN6O10S

751.25

COC[C@@H](C)N[C@@H](CC1)CC[C@H]1NC2=CC(C3=CSC(NCC4(CCOCC4)C#N)=N3)=C(Cl)C=N2.OC(/C=C\C(O)=O)=O.OC(/C=C\C(O)=O)=O

Apoptosis; Bcl-2 Family; Caspase; CDK; c-Myc; DNA/RNA Synthesis; DYRK; PARP

CDK1; CDK11; CDK14; CDK16; CDK2; CDK3; CDK5; CDK7; CDK8; CDK9

99.99

4°C (Powder, stored under nitrogen)

Room Temperature