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
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
Available Sizes
Frequently Asked Questions
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