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Dinaciclib (SCH727965)

CDK inhibitor

Dinaciclib (SCH727965)

Catalog No. A8412
Size Price Stock Qty
Evaluation Sample $28.00  All Inclusive In stock
25mg $594.00 In stock
5mg $216.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Dinaciclib(SCH727965)

Related Biological Data

Dinaciclib
Western Blot data of dinaciclib treated 1205Lu cells treated with 30 nM of dinaciclib for increasing periods of time (0–48 hrs). Along with a decrease in pRBser807/811, dinaciclib induced a marked upregulation of p53, increase in cleaved caspase-3, and down regulation of the pro-survival molecules Bcl-2, XIAP, and Mcl-1. The membrane was probed for actin expression to ensure equal protein loading.

Related Biological Data

Dinaciclib (SCH727965)

Related Biological Data

Dinaciclib (SCH727965)

Biological Activity

Description Dinaciclib (SCH727965) is a novel and potent inhibitor of CDK for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM, respectively.
Targets CDK2 CDK5 CDK1 CDK9    
IC50 1 nM 1 nM 3 nM 4 nM    

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Chemical Properties

Cas No. 779353-01-4 SDF Download SDF
Chemical Name 2-[(2S)-1-[3-ethyl-7-[(1-oxidopyridin-1-ium-3-yl)methylamino]pyrazolo[1,5-a]pyrimidin-5-yl]piperidin-2-yl]ethanol
Canonical SMILES CCC1=C2N=C(C=C(N2N=C1)NCC3=C[N+](=CC=C3)[O-])N4CCCCC4CCO
Formula C21H28N6O2 M.Wt 396.49
Solubility Soluble in DMSO Storage Store at -20°C
Shipping Condition: Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Dinaciclib is a potent cyclin-dependent kinase (CDK) inhibitor with IC50s for CDK2, CDK5, CDK1 and CDK9 at 1 nM, 1 nM, 3 nM, and 4 nM, respectively. [1] It is in phase I or II clinical trials for various cancers.

Dinaciclib interacts with the acetyl-lysine recognition site of bromodomains. [2] Inhibition of CDK 1 suppresses Rb phosphorylation, leading to cell cycle arrest and apoptosis. [3]

Dinaciclib is active against a broad spectrum of human tumor cell lines in vitro and in vivo. It has great potential to improve cancer chemotherapy.

References:
[1]Parry D., et al. (2010). Dinaciclib (SCH 727965), a Novel and Potent Cyclin-Dependent Kinase Inhibitor. Mol Cancer Ther (9): 2344- 2353.
[2]Martin, M. P., et al. (2013). Cyclin-dependent kinase inhibitor dinaciclib interacts with the acetyl-lysine recognition site of bromodomains. ACS Chemical Biology 8 (11): 2360–5.
[3]Payton M., et al. (2006). Discovery and Evaluation of Dual CDK1 and CDK2 Inhibitors. Cancer Res 66: 4299-4308.