1. Cell Cycle/DNA Damage
  2. CDK
  3. CDK4/6-IN-3

CDK4/6-IN-3 is a brain-penetrant CDK4/CDK6 inhibitor with Kis of <0.3 nM and 2.2 nM, respectively. CDK4/6-IN-3 inhibits CDK1 with a Ki of 110 nM. CDK4/6-IN-3 can be used for the treatment of glioblastoma.

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

CDK4/6-IN-3 Chemical Structure

CDK4/6-IN-3 Chemical Structure

CAS No. : 2366237-37-6

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CDK4/6-IN-3 is a brain-penetrant CDK4/CDK6 inhibitor with Kis of <0.3 nM and 2.2 nM, respectively. CDK4/6-IN-3 inhibits CDK1 with a Ki of 110 nM. CDK4/6-IN-3 can be used for the treatment of glioblastoma[1].

IC50 & Target[1]

CDK4

0.3 nM (Ki)

CDK6

2.2 nM (Ki)

CDK1

110 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
A 172 EC50
0.27 μM
Compound: 24
Antiproliferative activity against human A172 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
Antiproliferative activity against human A172 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
[PMID: 31307887]
BT-549 EC50
2.1 μM
Compound: 24
Antiproliferative activity against human BT549 cells assessed as reduction in DNA replication incubated for 16 hours followed by addition of EdU and incubated for 8 hours by Alexa flour488 and HCS dye-based fluorescence imaging method
Antiproliferative activity against human BT549 cells assessed as reduction in DNA replication incubated for 16 hours followed by addition of EdU and incubated for 8 hours by Alexa flour488 and HCS dye-based fluorescence imaging method
[PMID: 31307887]
BT-549 EC50
4.4 μM
Compound: 24
Cytotoxicity against human BT549 cells assessed as reduction in cell count after 24 hrs by high-throughput microscopy
Cytotoxicity against human BT549 cells assessed as reduction in cell count after 24 hrs by high-throughput microscopy
[PMID: 31307887]
DBTRG-05MG EC50
0.18 μM
Compound: 24
Antiproliferative activity against human DBTRG-05MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
Antiproliferative activity against human DBTRG-05MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
[PMID: 31307887]
M059J EC50
2.46 μM
Compound: 24
Antiproliferative activity against human M059J assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
Antiproliferative activity against human M059J assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
[PMID: 31307887]
MCF7 EC50
0.03 μM
Compound: 24
Antiproliferative activity against human MCF7 cells assessed as reduction in DNA replication incubated for 16 hours followed by addition of EdU and incubated for 8 hours by Alexa flour488 and HCS dye-based fluorescence imaging method
Antiproliferative activity against human MCF7 cells assessed as reduction in DNA replication incubated for 16 hours followed by addition of EdU and incubated for 8 hours by Alexa flour488 and HCS dye-based fluorescence imaging method
[PMID: 31307887]
MCF7 EC50
4.1 μM
Compound: 24
Cytotoxicity against human MCF7 cells assessed as reduction in cell count after 24 hrs by high-throughput microscopy
Cytotoxicity against human MCF7 cells assessed as reduction in cell count after 24 hrs by high-throughput microscopy
[PMID: 31307887]
SF-539 EC50
2.74 μM
Compound: 24
Antiproliferative activity against human SF539 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
Antiproliferative activity against human SF539 assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
[PMID: 31307887]
T98G EC50
0.52 μM
Compound: 24
Antiproliferative activity against human T98G assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
Antiproliferative activity against human T98G assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
[PMID: 31307887]
U-87MG ATCC EC50
0.17 μM
Compound: 24
Antiproliferative activity against human U87MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
Antiproliferative activity against human U87MG assessed as reduction in cell viability incubated for 5 days by CyQuantGR dye-based fluorescence assay
[PMID: 31307887]
In Vitro

CDK4/6-IN-3 (Compound 24) inhibits MCF7 and BT549 cell lines proliferation with EC50s of 30 nM and 2.1 μM, respectively[1].

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

Molecular Weight

462.57

Formula

C25H31FN8

CAS No.
SMILES

FC1=CN=C(NC2=NC=C(N3CC4(CN(CC)C4)C3)C=C2)N=C1C5=C([C@H](C)CCCC6)N6N=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
CDK4/6-IN-3
Cat. No.:
HY-126244
Quantity:
MCE Japan Authorized Agent: