BMS-265246 - Moligand™, 10mM in DMSO , Inhibitor of cyclin dependent kinase 1;Inhibitor of cyclin dependent kinase 2, CAS No.582315-72-8, Inhibitor of cyclin dependent kinase 1;Inhibitor of cyclin dependent kinase 2

CAS: 582315-72-8 Cat. No.: B409183 Molecular Weight: 345.34

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

(4-butoxy-1H-pyrazolo[3,4-b]pyridin-5-yl)(2,6-difluoro-4-methylphenyl)methanone

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

BMS-265246 is a potent and selective CDK1/2 inhibitor withIC50of 6 nM/9 nM in a cell-free assay. It is 25-fold more selective for CDK1/2 than CDK4.
In vitro

BMS265246 inhibits the activity of CDK4/cycD with IC50 of 0.23 μM and prevents A2780 Cytox with IC50 of 0.76 μM. BMS265246 which binds to CDK2 shows the inhibitor resides coincident with the ATP purine binding site and forms important H-bonds with Leu83 on the protein backbone. BMS265246 exhibits CDK1 and CDK2 potency that is 25- and 11-fold more potent versus CDK1 and CDK2, respectively. BMS265246 represents the most potent CDK/CDK2 selective analogue from this chemotype. A recent study shows that BMS-265246 inhibits cell proliferation with EC50 ranging from 0.293 μM-0.492 μM in HCT-116 cells. After treatment of BMS-265246, the dominant cell populations are G2-arrested cells having 4N DNA content, large round nuclei, and low DNA intensity.

In vivo

Cell Data

cell lines：

Concentrations：0-5 μM

Incubation Time：24 hours

Powder Purity:≥98%

Specifications

Synonyms

(4-butoxy-1H-pyrazolo[3, 4-b]pyridin-5-yl)(2, 6-difluoro-4-methylphenyl)methanone

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

BMS-265246 is a potent and selective CDK1/2 inhibitor with IC50 of 6 nM/9 nM in a cell-free assay. It is 25-fold more selective for CDK1/2 than CDK4.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Inhibitor of cyclin dependent kinase 1;Inhibitor of cyclin dependent kinase 2

Names and Identifiers

• Isomeric SMILES: CCCCOC1=C(C=NC2=NNC=C12)C(=O)C3=C(C=C(C=C3F)C)F
• Molecular Weight: 345.34
• Reaxy-Rn: 36321669
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=36321669&ln=

Associated Targets(Human)

CDK1 Tchem Cyclin-dependent kinase 1 (1 Activities)

Discover Target: CDK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 (1 Activities)

Discover Target: CDK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro Water: 63 mg/mL (198.51 mM); DMSO: 1 mg/mL (3.15 mM); Ethanol: Insoluble