Dinaciclib (SCH727965) (779353-01-4) Description
Dinaciclib, also known as SCH727965, is a potent CDK inhibitor with potential antineoplastic activity. Dinaciclib selectively inhibits cyclin dependent kinases CDK1, CDK2, CDK5, and CDK9 activity in vitro with IC(50) values of 1, 1, 3, and 4 nmol/L, respectively. Compared with flavopiridol, Dinaciclib exhibits superior activity with an improved therapeutic index. Dinaciclib induced regression of established solid tumors in a range of mouse models following intermittent scheduling of doses below the maximally tolerated level.
In vitro cell growth of pancreatic cancer cells is inhibited by Dinaciclib (SCH727965) in a dose-dependent manner. Upon incubation with Dinaciclib for 72 h, the GI50s are approximately 10 and 20 nM for MIAPaCa-2 and Pa20C cells, respectively. These results are consistent with studies of Dinaciclib in other cancer cell lines. In soft agar assays, 5 to 10 nM of Dinaciclib significantly reduces colony formation and anchorage independent growth of MIAPaCa-2 cells. Moreover, in vitro cell migration of Pa20C and MIAPaCa-2 cells is significantly reduced by Dinaciclib-concentrations starting from 2-5 nM, as demonstrated using BD FluoroChrom, modified Boyden Chamber and wound healing assays.
Dinaciclib (SCH727965) (779353-01-4) Specifications
|Product Name||Dinaciclib (SCH727965)|
|Synonyms||SCH 727965; SCH727965; SCH-727965; PS095760; PS 095760; PS-095760; Dinaciclib.|
|Chemical Names||(S)-3-(((3-ethyl-5-(2-(2-hydroxyethyl)piperidin-1-yl)pyrazolo[1,5-a]pyrimidin-7-yl)amino)methyl)pyridine 1-oxide|
|Monoisotopic Mass||396.22737 g/mol|
|Color||Light brown solid|
|Solubility||DMSO (>20 mg/ml)|
|Shelf life||>2 years if stored properly.|
|Handling||Protect from air and light|
|Application||A novel and potent CDK inhibitor|