DinaciclibA novel and potent cyclin-dependent kinase inhibitor for Cdk2, Cdk5, Cdk1, and Cdk9

Dinaciclib (CAS 779353-01-4)

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Synonym: SCH727965
Application: A novel and potent cyclin-dependent kinase inhibitor for Cdk2, Cdk5, Cdk1, and Cdk9
CAS Number: 779353-01-4
Purity: ≥98%
Molecular Weight: 396.49
Molecular Formula: C21H28N6O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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Dinaciclib (SCH727965) is a novel and potent cyclin-dependent kinase inhibitor for Cdk2 (IC50 = 1 nM), Cdk5 (IC50 = 1 nM), Cdk1 (IC50 = 3 nM), and Cdk9 (IC50 = 4 nM). Dinaciclib is also a potent DNA replication inhibitor that blocks thymidine (dThd) DNA incorporation in A2780 cells (IC50 = 4 nM). Dinaciclib strongly suppresses phosphorylation of Rb on Ser807/811 at concentrations >6.25 nM. Significantly, complete suppression of Rb phosphorylation is correlated with the onset of apoptosis, as indicated by the appearance of the p85 PARP cleavage product in cells exposed to >6.25 nM Dinaciclib. Dinaciclib is active against a broad spectrum of human tumor cell lines.

Appearance :
Powder
Physical State :
Solid
Solubility :
Soluble in water (<1 mg/ml at 25 °C), DMSO (79 mg/ml at 25 °C), ethanol (26 mg/ml at 25 °C), DMF (~25 mg/ml), and methanol.
Storage :
Store at -20° C
Melting Point :
107-111° C
IC50 :
CDK2: IC50 = 1 nM; CDK5: IC50 = 1 nM; CDK1: IC50 = 3 nM; CDK9: IC50 = 4 nM; DNA synthesis: IC50 = 4 nM
pK Values :
pKb: 6.71 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
46926350
MDL Number :
MFCD16037702
SMILES :
CCC1=C2N=C(C=C(N2N=C1)NCC3=C[N+](=CC=C3)[O-])N4CCCC[C@H]4CCO

Download SDS (MSDS)

Certificate of Analysis

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