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Tambiciclib (dimaleate)

CAT: 0804-HY-X0009A-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-X0009A-01Size:5 mg
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Description
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].
CAS Number
2559759-04-3
Product Name Alternative
GFH009 (dimaleate) ; JSH-009 (dimaleate) ; SLS009 (dimaleate)
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
Applications
Neuroscience-Neuromodulation
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/jsh-009-dimaleate.html
Purity
99.99
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.OC(/C=C\C(O)=O)=O.OC(/C=C\C(O)=O)=O
Molecular Formula
C33H43ClN6O10S
Molecular Weight
751.25
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, stored under nitrogen)
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
CDK1; CDK11; CDK14; CDK16; CDK2; CDK3; CDK5; CDK7; CDK8; CDK9

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