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Cat. No.: HY-151984

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CDK9-IN-22

CDK9-IN-22 is a potent CDK9 inhibitor with IC₅₀s of 10.4, 876.2 nM for CDK9, CDK, respectively. CDK9-IN-22 induces apoptosis and cell cycle arrests at G2/M phase. CDK9-IN-22 decreases the expression of p-RNAPII (S2) and CDK9 protein. CDK9-IN-22 shows antiproliferative and aiti-tumor activity.

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

CAS No.: 2872677-61-5
Formula: C₂₈H₂₈FN₅O₂
Molecular Weight:485.55

Storage:

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

Data Sheet (271 KB)

CDK9-IN-22 Chemical Structure

CAS No.: 2872677-61-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biological Activity

Description

IC₅₀ & Target^[1]

CDK9/cyclinT1

10.4 nM (IC₅₀)

cdk2/cyclin A

876.2 nM (IC₅₀)

All CDK Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	0.1 μM Compound: 8d	Antiproliferative activity against human A-431 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human A-431 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 36332552]
A549	IC₅₀	0.66 μM Compound: 8d	Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 36332552]
HCT-116	IC₅₀	0.09 μM Compound: 8d	Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 36332552]
L02	IC₅₀	1.43 μM Compound: 8d	Antiproliferative activity against human L02 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human L02 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 36332552]
NCI-H1975	IC₅₀	0.43 μM Compound: 8d	Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1975 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 36332552]
PANC-1	IC₅₀	0.08 μM Compound: 8d	Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human PANC-1 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 36332552]

In Vitro

CDK9-IN-22 (compound 8 d) (0.1, 0.5, 2.5 µM; 24, 48 h) induces apoptosis and cell cycle arrests at G2/M phase in a concentration-dependent manner in PANC-1 cells^[1].
CDK9-IN-22 (0.1, 0.5, 2.5 µM; 24 h) decreases the expression of p-RNAPII (S2) and CDK9 protein in PANC-1 cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

A549, H1975, A431, PANC-1, HCT-116, LO2 cells
Concentration:

0-100 µM
Incubation Time:

72 h
Result:

Showed antiproliferative activity with IC₅₀s of 0.66, 0.43, 0.10, 0.08, 0.09, 1.43 μM for A549, H1975, A431, PANC-1, HCT-116, LO2 cells, respectively.

Apoptosis Analysis^[1]

Cell Line:

PANC-1 cells
Concentration:

0.1, 0.5, 2.5 µM
Incubation Time:

48 h
Result:

Induced apoptosis with the percentage of total apoptotic cells was 43.6, 54.1 and 65.8% at 0.1, 0.5 and 2.5 μM, respectively.

Cell Cycle Analysis^[1]

Cell Line:

PANC-1 cells
Concentration:

0.1, 0.5, 2.5 µM
Incubation Time:

24 h
Result:

Arrested the cell cycle at the G2/M phase in a dose-dependent manner (21.83% for 0.1 μM, 25.85% for 0.5 μM and 34.26% for 2.5 μM).

Western Blot Analysis^[1]

Cell Line:

PANC-1 cells
Concentration:

0.1, 0.5, 2.5 µM
Incubation Time:

24 h
Result:

Decreased the expression of p-RNAPII (S2) and CDK9 protein in a dose-dependent manner.

In Vivo

CDK9-IN-22 (5, 10, 20 mg/kg; i.p.; every other day for four weeks) inhibits tumor growth in xenograft murine model^[1].

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

Animal Model:

BALB/c nude mice (PANC-1 tumor xenograft murine model)^[1]
Dosage:

5, 10, 20 mg/kg
Administration:

I.p.; every other day for four weeks
Result:

Inhibited the tumor growth with the tumor inhibition rate (TIR) was 6.2, 32.6 and 54.2% at the dose of 5, 10 and 20 mg/kg, respectively.

Chemical Information

CAS No. 2872677-61-5
Molecular Weight 485.55
Formula C₂₈H₂₈FN₅O₂
SMILES

CN(CCNC(C1=CC=C(C=C1)NC2=NC(C3=C(C=C(C=C3)F)OCC4=CC=CC=C4)=CC=N2)=O)C
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 (271 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]. Xu Z, et al. Design, synthesis and anticancer evaluation of selective 2,4-disubstituted pyrimidine CDK9 inhibitors. Eur J Med Chem. 2022 Dec 15;244:114875. [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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