Dinaciclib free base · Synonyms: SCH 727965

Dinaciclib is a potent inhibitor of CDK.

For research use only. Not for human or veterinary use.

Target CDK Apoptosis

Research area Cancer

Purity >98% Stock Inquire

Dinaciclib structure

CAS No.: 779353-01-4

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
100 mg	USD 750.00	BP-02333-100mg	In stock	Get quote
250 mg	USD 1,150.00	BP-02333-250mg	In stock	Get quote
500 mg	USD 1,650.00	BP-02333-500mg	In stock	Get quote
1 g	USD 2,350.00	BP-02333-1g	In stock	Get quote
2 g	Inquire	BP-02333-2g	In stock	Inquire

Need another size or custom synthesis? Request a quote.

Description

Dinaciclib (SCH 727965) is a potent inhibitor of CDK, with IC50s of 1 nM, 1 nM, 3 nM, and 4 nM for CDK2, CDK5, CDK1, and CDK9, respectively.

Biological activity

SCH727965 (Dinaciclib) is a novel small molecule multi-CDK inhibitor with low nanomolar potency against CDK1, CDK2, CDK5 and CDK9 that has shown favorable toxicity and efficacy in preliminary mouse experiments, and has been well tolerated in Phase I clinical trials. Cyclin-dependent kinases (CDK) are key positive regulators of cell cycle progression and attractive targets in oncology. SCH727965 was selected as a clinical candidate using a functional screen in vivo that integrated both efficacy and safety parameters. Compared with flavopiridol, SCH727965 exhibits superior activity with an improved therapeutic index. In cell-based assays, SCH727965 completely suppressed retinoblastoma phosphorylation, which correlated with apoptosis onset and total inhibition of bromodeoxyuridine incorporation in >100 tumor cell lines of diverse origin and background. Moreover, short exposures to SCH727965 were sufficient for long-lasting cellular effects. SCH727965 induced regression of established solid tumors in a range of mouse models following intermittent scheduling of doses below the maximally tolerated level. These results suggest that SCH727965 is a potent and selective CDK inhibitor and a novel cytotoxic agent.

Identifiers

SMILES: CCC1=C2N=C(C=C(N(C)C3=C[N+]([O-])=CC=C3)N2N=C1)N1CCCC[C@H]1CCO
InChIKey: QLQDYKJGBOTOKL-KRWDZBQOSA-N

Specifications

MW (average): 396.4860
Formula: C₂₁H₂₈N₆O₂
CAS No.: 779353-01-4
Physical state: Solid
Color: Off-white to yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

CoA On request
Handling Instructions

References

[1]. Parry D, et al. Dinaciclib (SCH 727965), a novel and potent cyclin-dependent kinase inhibitor. Mol Cancer Ther. 2010 Aug;9(8):2344-53.

[2]. Feldmann G, et al. Cyclin-dependent kinase inhibitor Dinaciclib (SCH727965) inhibits pancreatic cancer growth and progression in murine xenograft models. Cancer Biol Ther. 2011 Oct 1;12(7):598-609.

Same target

Search CDK

Same research area

Search Cancer