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Cat. No.: HY-126244

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CDK4/6-IN-3

CDK4/6-IN-3 is a brain-penetrant CDK4/CDK6 inhibitor with K_is of <0.3 nM and 2.2 nM, respectively. CDK4/6-IN-3 inhibits CDK1 with a K_i 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.

CAS No.: 2366237-37-6
Formula: C₂₅H₃₁FN₈
Molecular Weight:462.57

Storage:

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

Data Sheet (270 KB)

CDK4/6-IN-3 Chemical Structure

CAS No.: 2366237-37-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

CDK4

0.3 nM (Ki)

CDK6

2.2 nM (Ki)

CDK1

110 nM (Ki)

All CDK Isoforms :

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.

Chemical Information

CAS No. 2366237-37-6
Molecular Weight 462.57
Formula C₂₅H₃₁FN₈
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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Bronner SM, et al. Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2294-2301. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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