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> AZD-5438 [602306-29-6]

AZD-5438 [602306-29-6]

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Cat# HY-10012-10mg

Size : 10mg

Brand : MedChemExpress

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Description

AZD-5438 is a potent CDK1, CDK2, and CDK9 inhibitor, with IC50s of 16 nM, 6 nM, and 20 nM in cell-free assays, respectively. AZD-5438 shows less inhibition activity against GSK3β, CDK5 and CDK6 [1].

IC50 & Target[1]

cdk2-cyclin E

6 nM (IC50)

cdk2-cyclin A

45 nM (IC50)

cdk5-p25

14 nM (IC50)

cdk1-cyclin B1

16 nM (IC50)

cdk9-cyclin T

20 nM (IC50)

cdk6-cyclin D3

21 nM (IC50)

cdk4-cyclin D1

449 nM (IC50)

cdk7-cyclin H

821 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
HCT-116 GI50
0.45 μM
Compound: AZD5438
Growth inhibition of human HCT-116 cells incubated for 48 hrs by CCK-8 assay
Growth inhibition of human HCT-116 cells incubated for 48 hrs by CCK-8 assay
[PMID: 38488882]
HCT-116 IC50
0.47 μM
Compound: AZD5438
Antiproliferative activity against human HCT116 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells incubated for 48 hrs by MTT assay
[PMID: 31254921]
HeLa IC50
0.73 μM
Compound: AZD5438
Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay
[PMID: 31254921]
HeLa IC50
1.2 μM
Compound: 6; MMV676604
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by resazurin dye based fluorescence assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 48 hrs by resazurin dye based fluorescence assay
[PMID: 30647879]
HT-29 GI50
0.96 μM
Compound: AZD5438
Growth inhibition of human HT-29 cells incubated for 48 hrs by CCK-8 assay
Growth inhibition of human HT-29 cells incubated for 48 hrs by CCK-8 assay
[PMID: 38488882]
LoVo IC50
0.63 μM
Compound: 6c, AZD-5438
Antiproliferative activity against human LoVo cells assessed as BrdU incorporation after 48 hrs
Antiproliferative activity against human LoVo cells assessed as BrdU incorporation after 48 hrs
[PMID: 18815031]
LoVo IC50
0.8 μM
Compound: 1, AZD-5438
Antiproliferative activity against human LoVo cells assessed as inhibition of BrdU incorporation after 48 hrs
Antiproliferative activity against human LoVo cells assessed as inhibition of BrdU incorporation after 48 hrs
[PMID: 18996007]
LoVo IC50
0.8 μM
Compound: 6
Antiproliferative activity against human LoVo cells assessed as inhibition of BrdU incorporation after 48 hrs
Antiproliferative activity against human LoVo cells assessed as inhibition of BrdU incorporation after 48 hrs
[PMID: 18986805]
MCF7 IC50
10.67 μM
Compound: AZD5438
Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTT assay
[PMID: 31254921]
MDA-MB-231 IC50
7.2 μM
Compound: AZD5438
Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells incubated for 48 hrs by MTT assay
[PMID: 31254921]
PC-3 IC50
0.36 μM
Compound: AZD5438
Antiproliferative activity against human PC3 cells incubated for 48 hrs by MTT assay
Antiproliferative activity against human PC3 cells incubated for 48 hrs by MTT assay
[PMID: 31254921]
In Vitro

AZD5438 potently inhibits the kinase activity of cyclin E-cdk2, cyclin A-cdk2, cyclin B1-cdk1, p25-cdk5, cyclin D3-cdk6, and cyclin T-cdk9 (IC50, 6, 45, 16, 21, and 20 nM, respectively). AZD5438 potently inhibits the kinase activity of cyclin E-cdk2, cyclin A-cdk2, cyclin B1-cdk1, p25-cdk5, cyclin D3-cdk6, and cyclin T-cdk9 (IC50, 6, 45, 16, 21, and 20 nM, respectively). In common with many other cdk inhibitors, AZD5438 also inhibits the kinase activity of p25-cdk5 and glycogen synthase kinase 3β in vitro (IC50, 14 and 17 nM, respectively)[1]. AZD5438 significantly augments cellular radiosensitivity in NSCLC cells. Combined treatment with AZD5438 and irradiation also enhances tumor growth delay, with an enhancement factor ranging from 1.2-1.7[2].

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

AZD-5438 Related Antibodies

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (269.21 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6921 mL 13.4604 mL 26.9208 mL
5 mM 0.5384 mL 2.6921 mL 5.3842 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.73 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Purity & Documentation
References

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