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Merck
CN

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.

别名:

Cdk4/6 Inhibitor IV, trans-4-((6-(ethylamino)-2-((1-(phenylmethyl)-1H-indol-5-yl)amino)-4-pyrimidinyl)amino)-cyclohexanol, CINK4

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关于此项目

经验公式(希尔记法):
C27H32N6O
化学文摘社编号:
分子量:
456.58
UNSPSC Code:
12352200
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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

Quality Level

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.).

Packaging

Packaged under inert gas

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

Disclaimer

Toxicity: Standard Handling (A)

存储类别

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable


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