Tambiciclib

• Description :

  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 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.

• Shipping Conditions :

  Room Temperature

• Storage Conditions :

  4°C (Powder, protect from light)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 2

• Isoform :

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

• CAS Number :

  [2247481-08-7]