1. Cell Cycle/DNA Damage
  2. CDK

CDK4/6/1 Inhibitor 

Cat. No.: HY-112280
Handling Instructions

CDK4/6/1 Inhibitor is a CDK4/6 inhibitor with IC50s of 3 and 1 nM, respectively.

For research use only. We do not sell to patients.

CDK4/6/1 Inhibitor Chemical Structure

CDK4/6/1 Inhibitor Chemical Structure

CAS No. : 2099128-41-1

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

CDK4/6/1 Inhibitor is a CDK4/6 inhibitor with IC50s of 3 and 1 nM, respectively.

IC50 & Target

IC50: 3 nM (CDK4), 1 nM (CDK6)[1]

In Vitro

CDK4/6/1 Inhibitor is a potent anti-proliferative agent that arrests U87MG cell line exclusively in G1 (IC50=15.3 ± 2.9 nM in the anti-proliferation assay). U87MG cells exposed to varying concentrations of CDK4/6/1 Inhibitor for 24 hours show a dose-related increase in G1 arrest, and a significant increase in the percentage of cells in G1 is found in as little as 13.72 nM of CDK4/6/1 Inhibitor[1].

In Vivo

CDK4/6/1 Inhibitor has tumor growth inhibition values ranging from 62% to 99% for doses ranging from 3.125 to 50 mg/kg in an orthotopic xenograft mouse model of glioblastoma multiforme, and no significant body weight loss is observed. The increase in life span based on the median survival time of vehicle-treated animals in mice administered a dose of 50 mg/kg is significant at 162%[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0468 mL 10.2339 mL 20.4679 mL
5 mM 0.4094 mL 2.0468 mL 4.0936 mL
10 mM 0.2047 mL 1.0234 mL 2.0468 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

The U87MG glioblastoma cells are treated with CDK4/6/1 and incubated for 72 h at 37°C. Then the medium is removed, 4% paraformaldehyde (50 µL/well) is added to the wells, and the cells are fixed for 30 min at RT. Cells are washed twice with phosphate-buffered saline (PBS) solution, and permeabilized in 0.2% Triton-X100 for 5 min. Cells are ished twice with PBS, after which 50 µL DAPI (1 µg/mL) is added to the wells, followed by incubation of the cells in the dark for 20 min. After ishing three times with PBS, PBS (100 µL/well) is added to the wells. The plates are scanned using IN Cell Analyzer 2200[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]

In the U87MG-Luc orthotopic xenograft mouse model, mice are treated with 3.125, 6.25, 12.5, 25, 50 mg/kg QD CDK4/6/1 Inhibitor for 28 days

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

488.57

Formula

C₂₈H₃₀F₂N₆

CAS No.

2099128-41-1

SMILES

CC(C1(CCCC1)C2=CC(C3=NC(NC4=CC=C(C5CCN(C)CC5)C=N4)=NC=C3F)=C6)=NC2=C6F

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
CDK4/6/1 Inhibitor
Cat. No.:
HY-112280
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CDK4/6/1 Inhibitor

Cat. No.: HY-112280