CDK6/9-IN-1

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CDK6/9-IN-1 (compound 66) is an orally active active and dual CDK 6 and CDK 9 inhibitor, with IC₅₀ values of 40.5 nM and 39.5 nM for CDK6 anmd CDK9, respectively.

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

CDK6/9-IN-1 Chemical Structure

CAS No. : 2414373-55-8

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Biological Activity
Purity & Documentation
References
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Description

CDK6/9-IN-1 (compound 66) is an orally active active and dual CDK 6 and CDK 9 inhibitor, with IC₅₀ values of 40.5 nM and 39.5 nM for CDK6 anmd CDK9, respectively^[1].

IC₅₀ & Target^[1]

CDK6

40.5 nM (IC₅₀)

CDK9

39.5 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
Jurkat	IC₅₀	4.01 μM Compound: 66	Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay Antiproliferative activity against human Jurkat cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay	[PMID: 32129996]
L02	GI₅₀	> 100 μM Compound: 66	Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay	[PMID: 32129996]
MCF7	IC₅₀	4.01 μM Compound: 66	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay	[PMID: 32129996]
MDA-MB-231	IC₅₀	4.01 μM Compound: 66	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by CCK8 assay	[PMID: 32129996]
Sf9	IC₅₀	> 10 μM Compound: 66	Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 10 mins by ADP-glo assay Inhibition of recombinant human full-length N-terminal GST-tagged CDK2/cyclinA2 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 10 mins by ADP-glo assay	[PMID: 32129996]
Sf9	IC₅₀	0.0395 μM Compound: 66	Inhibition of recombinant human full-length N-terminal GST-tagged CDK9/cyclinK expressed in baculovirus infected Sf9 insect cells using PDKtide as substrate measured after 120 mins by ADP-glo assay Inhibition of recombinant human full-length N-terminal GST-tagged CDK9/cyclinK expressed in baculovirus infected Sf9 insect cells using PDKtide as substrate measured after 120 mins by ADP-glo assay	[PMID: 32129996]
Sf9	IC₅₀	0.0405 μM Compound: 66	Inhibition of recombinant human full-length N-terminal His-tagged CDK6/cyclinD3 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 60 mins by ADP-glo assay Inhibition of recombinant human full-length N-terminal His-tagged CDK6/cyclinD3 expressed in baculovirus infected Sf9 insect cells using histone H1 as substrate measured after 60 mins by ADP-glo assay	[PMID: 32129996]

In Vitro

CDK6/9-IN-1 (compound 66, 4 or 8 μM in MDA-MB-231 cells) treatment induces G0/G1 cell cycle arrest (71.85% and 77.51%, respectively), when compared with the control (57.65%)^[1].

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

In Vivo

CDK6/9-IN-1 (compound 66) significantly inhibits tumor growth in an xenograft mouse model with no obvious toxicity, indicating the promising therapeutic potential of CDK6/9 dual inhibitors for cancer treatment^[1].

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

Molecular Weight

452.94

Formula

C₂₂H₂₅ClN₈O

CAS No.

2414373-55-8

SMILES

CC(NC1=CC=CC(NC2=NC(NC3=NC=C(N4CCN(C)CC4)C=C3)=NC=C2Cl)=C1)=O

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

Handling Instructions (2659 KB)

References

[1]. Yang Wang, et al. Discovery and SARs of 5-Chloro- N4-phenyl- N2-(pyridin-2-yl)pyrimidine-2,4-diamine Derivatives as Oral Available and Dual CDK 6 and 9 Inhibitors With Potent Antitumor Activity. J Med Chem. 2020 Mar 26;63(6):3327-3347. [Content Brief]

CDK6/9-IN-1 Related Classifications

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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.

Keywords:

CDK6/9-IN-12414373-55-8CDKCyclin dependent kinaseG0G1cellcyclearrestInhibitorinhibitorinhibit

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