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.
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- No. CAS: 2366237-37-6
- Fòrmula: C25H31FN8
- Peso molecular:462.57
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
CDK4 0.3 nM (Ki) |
CDK6 2.2 nM (Ki) |
CDK1 110 nM (Ki) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A 172 | EC50 |
0.27 μM
Compound: 24
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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
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[PMID: 31307887] |
| BT-549 | EC50 |
2.1 μM
Compound: 24
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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
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[PMID: 31307887] |
| BT-549 | EC50 |
4.4 μM
Compound: 24
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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
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[PMID: 31307887] |
| DBTRG-05MG | EC50 |
0.18 μM
Compound: 24
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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
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[PMID: 31307887] |
| M059J | EC50 |
2.46 μM
Compound: 24
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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
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[PMID: 31307887] |
| MCF7 | EC50 |
0.03 μM
Compound: 24
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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
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[PMID: 31307887] |
| MCF7 | EC50 |
4.1 μM
Compound: 24
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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
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[PMID: 31307887] |
| SF-539 | EC50 |
2.74 μM
Compound: 24
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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
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[PMID: 31307887] |
| T98G | EC50 |
0.52 μM
Compound: 24
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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
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[PMID: 31307887] |
| U-87MG ATCC | EC50 |
0.17 μM
Compound: 24
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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
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[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. .
Chemical Information
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No. CAS 2366237-37-6
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Peso molecular 462.57
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Fòrmula C25H31FN8
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SMILES
FC1=CN=C(NC2=NC=C(N3CC4(CN(CC)C4)C3)C=C2)N=C1C5=C([C@H](C)CCCC6)N6N=C5
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CDK4/6-IN-3 Related Classifications
HY-126244 Related Classifications
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