219503

Cdk4 Inhibitor V

The Cdk4 Inhibitor V, also referenced under CAS 943746-57-4, controls the biological activity of Cdk4. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Synonym(s): Cdk4 Inhibitor V, 4-(((4-Hydroxy-5-propoxy-pyridin-2-ylmethyl)-amino)-methylene)-6-iodo-4H-isoquinoline-1,3-dione
• Empirical Formula (Hill Notation): C₁₉H₁₈IN₃O₄
• CAS Number: 943746-57-4
• Molecular Weight: 479.27
• MDL number: MFCD16495770
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• assay: ≥98% (HPLC)
• form: powder
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: caramel
• solubility: DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• SMILES string: O=C(/C1=C\NCC2=CC(O)=C(OCCC)C=N2)NC(C3=C1C=C(I)C=C3)=O

Description

General description

A cell-permeable and metabolically stable (t_1/2 >30 min at 37 °C in rat liver microsomes stability assays) pyridinylmethylamino-isoquinoline dione that acts as a potent, ATP-binding site-targeting Cdk4/D1 inhibitor (IC₅₀ = 30 nM) and an effective antiproliferative agent against HCT116 and MCF-7 cancer cells (IC₅₀ = 0.73 and 0.88 µM, respectively), affecting Cdk2/E and Cdk1/B only at much higher concentrations (IC₅₀ = 1.6 and 25.3 µM, respectively).

A cell-permeable and metabolically stable (t_1/2 >30 min at 37 °C in the presence of rat liver microsomes, NADPH, and UDPGA) pyridinylmethylamino-isoquinoline dione that acts as a potent, ATP-binding site-targeting inhibitor against Cdk4/D1 kinase activity (IC₅₀ = 30 nM in cell-free Rb c-terminal fragment phosphorylation assays) and an effective antiproliferative agent against HCT116 colorectal and MCF-7 breast cancer cultures (IC₅₀ = 0.73 and 0.88 µM, respectively), while affecting Cdk2/E and Cdk1/B kinase activities only at much higher concentrations (IC₅₀ = 1.6 and 25.3 µM, respectively).

Packaging

Packaged under inert gas

Warning

Toxicity: Regulatory Review (Z)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Tsou, H.R., et al. 2009. J. Med. Chem.52, 2289.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2
• flash_point_f: Not applicable
• flash_point_c: Not applicable