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
质量水平
方案
≥95% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
pale amber
溶解性
DMSO: 10 mg/mL
运输
ambient
储存温度
2-8°C
一般描述
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.).
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.).
包装
Packaged under inert gas
其他说明
Soni, R., et al. 2001. J. Natl. Cancer Inst.93, 436.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Standard Handling (A)
储存分类代码
11 - Combustible Solids
WGK
WGK 2
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