Millipore Sigma Vibrant Logo
Attention: We have moved. Merck Millipore products are no longer available for purchase on MerckMillipore.com.Learn More

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

219492
  
Purchase on Sigma-Aldrich

Overview

Replacement Information

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
Applications
Biological Information
Purity≥95% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
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
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
219492 0

Documentation

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

Title

Safety Data Sheet (SDS) 

Cdk4/6 Inhibitor IV - CAS 359886-84-3 - Calbiochem Certificates of Analysis

TitleLot Number
219492

References

Reference overview
Soni, R., et al. 2001. J. Natl. Cancer Inst. 93, 436.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision25-August-2009 RFH
Synonymstrans-4-((6-(ethylamino)-2-((1-(phenylmethyl)-1H-indol-5-yl)amino)-4-pyrimidinyl)amino)-cyclohexanol, CINK4
DescriptionA 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.).
FormPale amber solid
Intert gas (Yes/No) Packaged under inert gas
CAS number359886-84-3
Chemical formulaC₂₇H₃₂N₆O
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (10 mg/ml)
Storage Protect from light
+2°C to +8°C
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.
Toxicity Standard Handling
ReferencesSoni, R., et al. 2001. J. Natl. Cancer Inst. 93, 436.