219492

Cdk4/6 Inhibitor IV

The Cdk4/6 Inhibitor IV, also referenced under CAS 359886-84-3, controls the biological activity of Cdk4/6. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• Sinónimos: Cdk4/6 Inhibitor IV, trans-4-((6-(ethylamino)-2-((1-(phenylmethyl)-1H-indol-5-yl)amino)-4-pyrimidinyl)amino)-cyclohexanol, CINK4
• Fórmula empírica (notación de Hill): C₂₇H₃₂N₆O
• Número de CAS: 359886-84-3
• Peso molecular: 456.58
• UNSPSC Code: 12352200

Propiedades

• Quality Level: 100
• assay: ≥95% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: pale amber
• solubility: DMSO: 10 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Descripción

General description

A cell-permeable triaminopyrimidine compound that acts as a reversible and ATP-competitive inhibitor against Cyclin D1-complexed, but not Cyclin D2-complexed, Cdk4 and Cdk6 (IC₅₀ = 1.5 & 5.6 µM, respectively) with much reduced activity against Cdk5/p35 (IC₅₀ = 25 µM) and little or no activity towards Cdk1/CycB,

Cdk2/CycA, Cdk2/CycE, v-abl, c-met, IGF-1R, or IR (IC₅₀ >10 µM). CINK4 (at 5 & 10 µM) effectively inhibits cellular Cdk4 substrate pRb phosphorylation and prevents serum-stimulated G₁/S transition of serum starved pRb-positive, but not pRb-negative, cultures. CINK4 is shown to exert a ~46% suppression of human colon carcinoma HCT116-derived tumor growth in mice in vivo (30 mg/kg; twice a day i.p.).

A cell-permeable triaminopyrimidine compound that acts as a reversible and ATP-competitive inhibitor against Cyclin D1-complexed, but not Cyclin D2-complexed, Cdk4 and Cdk6 (IC₅₀ = 1.5 and 5.6 µM, respectively) with much reduced activity against Cdk5/p35 (IC₅₀ = 25 µM) and little or no activity towards Cdk1/CycB, Cdk2/CycA, Cdk2/CycE, v-abl, c-met, IGF-1R, or IR (IC₅₀ >10 µM). CINK4 (at 5 and 10 µM) effectively inhibits cellular Cdk4 substrate pRb phosphorylation and prevents serum-stimulated G₁/S transition of serum starved pRb-positive, but not pRb-negative, cultures. CINK4 is shown to exert a ~46% suppression of human colon carcinoma HCT116-derived tumor growth in mice in vivo (30 mg/kg; twice a day, i.p.).

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Other Notes

Soni, R., et al. 2001. J. Natl. Cancer Inst.93, 436.

Legal Information

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

Información de seguridad

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 2