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219492 Cdk4/6 Inhibitor IV - CAS 359886-84-3 - Calbiochem

219492
  
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Overview

Key Spec Table

CAS #Empirical Formula
359886-84-3C₂₇H₃₂N₆O
Description
Overview

This product has been discontinued.



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.).

Catalogue Number219492
Brand Family Calbiochem®
Synonymstrans-4-((6-(ethylamino)-2-((1-(phenylmethyl)-1H-indol-5-yl)amino)-4-pyrimidinyl)amino)-cyclohexanol, CINK4
References
ReferencesSoni, R., et al. 2001. J. Natl. Cancer Inst. 93, 436.
Product Information
CAS number359886-84-3
FormPale amber solid
Hill FormulaC₂₇H₃₂N₆O
Chemical formulaC₂₇H₃₂N₆O
Structure formula ImageStructure formula Image
Quality LevelMQ100
Biological Information
Purity≥95% by HPLC
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Global Trade Item Number
Catalogue Number GTIN
219492 0