AZD-5438
Based on 16 publication(s) in Google Scholar
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 .
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.91%
- CAS No.: 602306-29-6
- Formule: C18H21N5O2S
- Masse moléculaire:371.46
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Publications Citing Use of MedChemExpress (MCE) AZD-5438
More- J Am Chem Soc. 2026 Jun 3;148(23):24333-24344.
- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- J Exp Clin Cancer Res. 2025 Nov 6;44(1):300. [Abstract]
- Sci Adv. Sci Adv. 2024 Jun 21;10(25):eadk2299. d [Abstract]
- Sci Adv. 2022 Jan 28;8(4):eabk2116. [Abstract]
- J Am Soc Nephrol. 2024 Jan 1;35(1):22-40. [Abstract]
- J Transl Med. 2022 Oct 2;20(1):444. [Abstract]
- Oncogene. 2026 Jun 10. [Abstract]
- Cell Chem Biol. 2018 Feb 15;25(2):135-142.e5. [Abstract]
- JACC Basic Transl Sci. 2023 Jul 19;8(9):1215-1239. [Abstract]
- Melanoma Res. 2022 Dec 1;32(6):419-427. [Abstract]
- bioRxiv. 2026 Jan 17.
- SSRN. 2025 Sep 19.
- Sci Total Environ. 2024 Oct 10:946:174246. [Abstract]
- University of Kiel. 2023 Jul 20.
- bioRxiv. 2023 Jun 9:2023.06.07.544128. [Abstract]
Customer Validation & Images
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Cell Imaging/Staining
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WB
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Apoptosis Analysis
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In Vivo Efficacy Study
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IHC
Activité biologique
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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) |
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Cell Line
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Type | Value | Description | References |
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| HCT-116 | GI50 |
0.45 μM
Compound: AZD5438
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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
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[PMID: 38488882] |
| HCT-116 | IC50 |
0.47 μM
Compound: AZD5438
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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
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[PMID: 31254921] |
| HeLa | IC50 |
0.73 μM
Compound: AZD5438
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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
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[PMID: 31254921] |
| HeLa | IC50 |
1.2 μM
Compound: 6; MMV676604
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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
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[PMID: 30647879] |
| HT-29 | GI50 |
0.96 μM
Compound: AZD5438
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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
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[PMID: 38488882] |
| LoVo | IC50 |
0.63 μM
Compound: 6c, AZD-5438
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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
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[PMID: 18815031] |
| LoVo | IC50 |
0.8 μM
Compound: 1, AZD-5438
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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
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[PMID: 18996007] |
| LoVo | IC50 |
0.8 μM
Compound: 6
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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
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[PMID: 18986805] |
| MCF7 | IC50 |
10.67 μM
Compound: AZD5438
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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
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[PMID: 31254921] |
| MDA-MB-231 | IC50 |
7.2 μM
Compound: AZD5438
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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
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[PMID: 31254921] |
| PC-3 | IC50 |
0.36 μM
Compound: AZD5438
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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
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[PMID: 31254921] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 602306-29-6
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Appearance Solid
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Masse moléculaire 371.46
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Formule C18H21N5O2S
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Color White to light yellow
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SMILES
O=S(C1=CC=C(NC2=NC(C3=CN=C(N3C(C)C)C)=CC=N2)C=C1)(C)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months
Publications (16)
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Journal Impact Factor
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Most Recent
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Sci Transl Med
PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]2018 Jul 18;10(450):eaaq1093. PMID: 30021885 -
J Exp Clin Cancer Res
Dual CDK and MEK Inhibition potentiates CD8+ T cell-mediated antitumor immunity by inducing pyroptotic cell death in high-mutational head and neck cancer. [Abstract]2025 Nov 6;44(1):300. PMID: 41194215
AZD-5438 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Nov 6;44(1):300. [Abstract]
Effect of AZD5438 (2 μM) and/or PD0325901 treatment on clonogenic ability of four HNSCC cell lines. HNSCC cells were treated with the drug for 10 days before analysis.
AZD-5438 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Nov 6;44(1):300. [Abstract]
Effect of AZD5438 (2 μM) and/or PD0325901 treatment on the phosphorylation levels of ERK1/2 and Rb and c-PARP cleavage in Cal27 and HN12 cells.
AZD-5438 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Nov 6;44(1):300. [Abstract]
Effect of AZD5438 (2 μM) and/or PD0325901 treatment on apoptosis of Cal27 and HN12 cells determined by Annexin V staining,
AZD-5438 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Nov 6;44(1):300. [Abstract]
Tumor images in different treatment groups An orthotopic HN12 tumor model was established in the buccal mucosa of NSG mice, followed by oral administration of vehicle, PD0325901, AZD5438 (50 mg/kg, i.g.), or their combination once daily for 14 days.
AZD-5438 purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2025 Nov 6;44(1):300. [Abstract]
Immunostaining of Ki67 and TUNEL assays for tumor tissues derived from the groups treated with vehicle, AZD5438, PD0325901, or the AZD5438 (50 mg/kg, i.g.) and PD0325901 combination.
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Sci Adv
In silico transcriptome screens identify epidermal growth factor receptor inhibitors as therapeutics for noise-induced hearing loss. [Abstract]Sci Adv. 2024 Jun 21;10(25):eadk2299. d PMID: 38896614 -
Sci Adv
2022 Jan 28;8(4):eabk2116. PMID: 35089781 -
J Am Soc Nephrol
2024 Jan 1;35(1):22-40. PMID: 37962623 -
J Transl Med
CDK1 serves as a therapeutic target of adrenocortical carcinoma via regulating epithelial-mesenchymal transition, G2/M phase transition, and PANoptosis. [Abstract]2022 Oct 2;20(1):444. PMID: 36184616 -
Oncogene
DNA replication stress and translational repression converge to drive CDK1- and caspase-dependent apoptosis in Ewing sarcoma. [Abstract]2026 Jun 10. PMID: 42270776 -
Cell Chem Biol
2018 Feb 15;25(2):135-142.e5. PMID: 29276047 -
JACC Basic Transl Sci
Syntaxin 17 Protects Against Heart Failure Through Recruitment of CDK1 to Promote DRP1-Dependent Mitophagy. [Abstract]2023 Jul 19;8(9):1215-1239. PMID: 37791317 -
Melanoma Res
LS-007 inhibits melanoma growth via inducing apoptosis and cell cycle arrest and regulating macrophage polarization. [Abstract]2022 Dec 1;32(6):419-427. PMID: 36094494 -
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Sci Total Environ
Voltage-dependent anion channel 1 mediates mitochondrial fission and glucose metabolic reprogramming in response to ionizing radiation. [Abstract]2024 Oct 10:946:174246. PMID: 38955266 -
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bioRxiv
In Silico Transcriptome-based Screens Identify Epidermal Growth Factor Receptor Inhibitors as Therapeutics for Noise-induced Hearing Loss. [Abstract]2023 Jun 9:2023.06.07.544128. PMID: 37333346
Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
AZD5438 is tested against solid tumor cell lines as previously described. Briefly, cells are incubated for 48 h with AZD5438 at a range of concentrations. At the end of incubation, the cells are pulsed with 5-bromo-2'-deoxyuridine (BrdUrd) and the amount of DNA synthesis is measured. The IC50 for inhibition of proliferation is specifically determined independently of cell death. Multiple myeloma cell lines are seeded into 96-well plates in RPMI 1640 supplemented with 10% FCS and glutamine and dosed with AZD5438 for 72 h. Cell growth is measured using AlamarBlue and GI50 values are calculated with reference to pretreatment control values.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
All human tumor xenografts except HX147 are established by s.c. injecting 100 μL of tumor cells (between 1×106 and 1×107 cells mixed 1:1 with Matrigel). HX147 tumors are derived from fragment implants (1 mm3 pieces) from tumors taken from mice initially implanted s.c. with 1×107 cells. These tumor fragments are passaged in mice thrice before implant for antitumor work. Tumors are measured up to three times per week with calipers, tumor volumes are calculated, and the data are plotted as geometric mean for each group versus time, as previously described. Animals are randomized into treatment groups (typically n=10) when tumors reach a mean size of approximately >0.2 cm3 and >0.5 cm3 for mice and rats, respectively. AZD5438 is prepared in hydroxy-propyl-methyl-cellulose. Animals are given either AZD5438 (37.5-75 mg/kg) or vehicle control once or twice daily by oral gavage for appr 3 wk in each case. Tumor volume and percentage tumor growth inhibition (% TGI) are calculated as described previously. Statistical analysis of any change in tumor volume is carried out using a standard t test (P<0.05 is considered to be statistically significant).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Byth KF, et al. AZD5438, a potent oral inhibitor of cyclin-dependent kinases 1, 2, and 9, leads to pharmacodynamic changes and potent antitumor effects in human tumor xenografts. Mol Cancer Ther. 2009 Jul;8(7):1856-66. Epub 2009 Jun 9. [Content Brief]
[2]. Raghavan P, et al. AZD5438, an Inhibitor of Cdk1, 2, and 9, Enhances the Radiosensitivity of Non-Small Cell Lung Carcinoma Cells. Int J Radiat Oncol Biol Phys. 2012 Jul 12. [Content Brief]
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6921 mL | 13.4604 mL | 26.9208 mL | 67.3020 mL |
| 5 mM | 0.5384 mL | 2.6921 mL | 5.3842 mL | 13.4604 mL | |
| 10 mM | 0.2692 mL | 1.3460 mL | 2.6921 mL | 6.7302 mL | |
| 15 mM | 0.1795 mL | 0.8974 mL | 1.7947 mL | 4.4868 mL | |
| 20 mM | 0.1346 mL | 0.6730 mL | 1.3460 mL | 3.3651 mL | |
| 25 mM | 0.1077 mL | 0.5384 mL | 1.0768 mL | 2.6921 mL | |
| 30 mM | 0.0897 mL | 0.4487 mL | 0.8974 mL | 2.2434 mL | |
| 40 mM | 0.0673 mL | 0.3365 mL | 0.6730 mL | 1.6825 mL | |
| 50 mM | 0.0538 mL | 0.2692 mL | 0.5384 mL | 1.3460 mL | |
| 60 mM | 0.0449 mL | 0.2243 mL | 0.4487 mL | 1.1217 mL | |
| 80 mM | 0.0337 mL | 0.1683 mL | 0.3365 mL | 0.8413 mL | |
| 100 mM | 0.0269 mL | 0.1346 mL | 0.2692 mL | 0.6730 mL |
AZD-5438 Related Classifications
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