Tambiciclib

Tambiciclib (GFH009, JSH-009) 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 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 can be used for AML research[1].

Product Specifications

CAS Number

[2247481-08-7]

Product Name Alternative

GFH009; JSH-009; SLS009

UNSPSC

12352005

Target

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

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics; Protein Tyrosine Kinase/RTK

Field of Research

Cancer; Metabolic Disease; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/jsh-009.html

Concentration

10mM

Purity

99.21

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

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

Molecular Formula

C25H35ClN6O2S

Molecular Weight

519.10

References & Citations

[1]Wang L, et al. Discovery of a novel and highly selective CDK9 kinase inhibitor (JSH-009) with potent antitumor efficacy in preclinical acute myeloid leukemia models. Invest New Drugs. 2020 Oct;38 (5) :1272-1281.