2559759-04-3
Chemical Structure
Tambiciclib dimaleate
Synonym(s): GFH009 dimaleate; JSH-009 dimaleate; SLS009 dimaleate
- CAS No.: 2559759-04-3
- Formula:C33H43ClN6O10S
- Molecular Weight:751.25
IUPAC Name: 4-(((4-(5-chloro-2-(((1R,4r)-4-(((R)-1-methoxypropan-2-yl)amino)cyclohexyl)amino)pyridin-4-yl)thiazol-2-yl)amino)methyl)tetrahydro-2H-pyran-4-carbonitrile dimaleate
InChIKey: XHSYQAXIGPUZJE-OKKMNLQXSA-N
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
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Tambiciclib dimaleate | 99.53% | 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. | ||||||||||||||||||||
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Keywords
