For research use only.

Catalog No.S2621

18 publications

AZD5438 Chemical Structure

CAS No. 602306-29-6

AZD5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM in cell-free assays. It is less potent to CDK5/6 and also inhibits GSK3β. Phase 1.

Selleck's AZD5438 has been cited by 18 publications

6 Customer Reviews

  • (a) HEK-293 cells expressing V5-EXO1 were synchronized in different phases of the cell cycle. EXO1 was immunoprecipitated (IP) with anti-V5 antibody and Western blotted with anti-phospho-Ser (p-SP) or anti-phospho-Thr (p-TP) CDK substrate antibodies, as indicated. “+AZD” indicates cells pre-treated with the CDK inhibitor AZD5438 prior to analysis. (b) HEK-293 cells expressing V5-EXO1, synchronized in G2, were pre-treated with CDK inhibitors, AZD5438 or Roscovitine, prior to analysis of EXO1 phosphorylation by IP-Western.

    Nat Commun 2014 5, 3561. AZD5438 purchased from Selleck.

  • J558 cells were treated with RO3306 (5-15 umol/L), AZD5438 (0.2-4 umol/L), or JNJ7706621 (0.2-4 umol/L) for 6 hours, after which Western blot analysis was performed to monitor XBP-1s expression.

    Mol Cancer Ther 2014 13(3), 662-74. AZD5438 purchased from Selleck.

  • The CDK inhibitor AZD5438 also sensitizes L. monocytogenes to β-lactam treatment through inhibition of PrkA. Autophosphorylation (arrow) and MBP phosphorylation (asterisk) activities were assayed for PrkA in the presence or absence of 2-fold serial dilutions of AZD5438.

    Antimicrob Agents Chemother 2014 58(8), 4486-94. AZD5438 purchased from Selleck.

  • Different breast cancer cell lines were seeded in 96 well plates and treated with different concentrations of AZD5438. After 72h, cell viability was assessed by MTT. Data shows that these cancer cell lines were sensitive to CDK1/2/9 inhibition, however the most aggressive (SUM159 and MDA-MB-231) cells were less susceptible.

    Helen Sadik from Johhns Hopkins University. AZD5438 purchased from Selleck.

  • AZD5438 exerted antitumor effect in case 168 accompanied by reduction of expression of CDK2, CCNE1, and phosphorylated retinoblastoma (pRb). Whereas in case number 111, slight reduction of CDK2 but no impact on level of CCNE1 or pRB.

    J Hematol Oncol, 2018, doi:10.1186/s13045-018-0563-y. AZD5438 purchased from Selleck.

  • Western blot illustrating PARP1 cleavage in SW48 KRAS WT and p.G12V mutant cells after 72h of AZD5438 exposure. Cells were exposed to AZD5438 for two hours after which total cell lysates were generated and western blotted as shown. Exposure to camptothecin was used as a positive control.

    PLoS One, 2016, 11(2):e0149099. AZD5438 purchased from Selleck.

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Biological Activity

Description AZD5438 is a potent inhibitor of CDK1/2/9 with IC50 of 16 nM/6 nM/20 nM in cell-free assays. It is less potent to CDK5/6 and also inhibits GSK3β. Phase 1.
Features A potent inhibitor of cyclin-dependent kinase (CDK) 1, 2, and 9.
CDK2 [1]
(Cell-free assay)
CDK1 [1]
(Cell-free assay)
CDK9 [1]
(Cell-free assay)
6 nM 16 nM 20 nM
In vitro

AZD5438 exhibits the potent inhibitory effect on activity of cyclin-dependent kinases including cyclin E-cdk2, cyclin A-cdk2, cyclin B1-cdk1, cyclin D3-cdk6, and cyclin T-cdk9 with IC50 of 6 nM, 45 nM, 16 nM, 21 nM, and 20 nM, respectively. Besides, AZD5438 also inhibits the kinase activity of p25-cdk5 and glycogen synthase kinase 3β with IC50 of 14 nM and 17 nM, respectively. [1] AZD5438 induces cell cycle arrest by inhibiting phosphorylation of cdk-dependent substrates, and exhibits the broad antiproliferative activity against a range of tumor cell lines including lung, colorectal, breast, prostate, and hematologic tumors with IC50 ranging from 0.2 μM (MCF-7) to 1.7 μM (ARH-77). [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human LoVo cells MojZVJJwdGmoZYLheIlwdiCjc4PhfS=> NFPhSo81QCCq NEPueW5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFzvWo8h[2WubIOgZZN{\XO|ZXSgZZMhSnKmVTDpcoNwenCxcnH0bY9vKGGodHXyJFQ5KGi{czygTWM2OD1yLk[zJO69VQ>? NXPJV3A6OTh6MUWwN|E>
human LoVo cells MYXQdo9tcW[ncnH0bY9vKGG|c3H5 NGLUOoo1QCCq NUHGfFA{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMc3ZwKGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gRpJlXSCrbnPvdpBwemG2aX;uJIFnfGW{IES4JIhzeyxiSVO1NF0xNjhizszN MlmxNVg6QTZyMEe=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-Chk2 / Chk2 / p-Chk1 / Chk1 ; 

PubMed: 22795803     

AZD5438 does not abrogate Chk1/2 activation. Both A549 (250 nM) and H460 (435 nM) cells were treated with AZD5438 for 24 h and treated with IR (5 Gy) for 30 min. Immunoblot analysis using pChk1(Ser317) and pChk2 (T68). Total Chk1 and Chk2 proteins and actin were used for loading control.

Growth inhibition assay
Cell viability; 

PubMed: 22795803     

Clonogenic survival assay for drug sensitivity determination. NSCLC cells were plated with or without AZD5438 (5 nM, 50 nM, 500 nM, 5 µM, and 50 µM). Colonies were counted and percentage of survival was plotted against log [Dose].

In vivo In vivo, oral treatment of AZD5438 leads to statistically significant inhibition against the growth of human tumor xenografts derived from a wide range of different cancer types including breast, colon, lung, prostate, and ovarian with maximum TGI ranging from 38% to 153%. [1] In the SW620 xenograft model, AZD5438 causes the inhibition of several cell cycle proteins such as, phH3, phosphonucleolin, PP1a, and several phospho-pRb epitopes in a dose-dependent manner. [1]


Kinase Assay:[1]
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Recombinant Kinase Assays [1]:

The ability of AZD5438 to inhibit cdk activity is examined using a scintillation proximity assay with recombinant cdk-cyclin complexes of cyclin-Ecdk2, cdk2-cyclin A, cdk4-cyclin D, and recombinant retinoblastoma substrate (amino acids 792-928) or cdk1-cyclin B1 with a peptide substrate derived from the in vitro p34cdc2 phosphorylation site of histone H1 (biotin-X-Pro-Lys-Thr-Pro-Lys-Lys-Ala-Lys-Lys-Leu). The activity of AZD5438 against recombinant cdk5/p25 (at 2 μM ATP) is determined in a scintillation proximity assay-based assay using peptide substrate (AKKPKTPKKAKKLOH). Inhibition of glycogen synthase kinase 3β activity is determined with scintillation proximity assay based on the use of human purified glycogen synthase kinase 3βenzyme and eukaryotic initiation factor 2B substrate (at 1 μM ATP). AZD5438 is screened against active recombinant human cdk6-cyclin D3, cdk7-cyclin H/MAT1 (cdk activating kinase complex), and cdk9-cyclin T using the kinase selectivity screening service.
Cell Research:[1]
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  • Cell lines: MCF-7, HCT-116, A549, and IM-9
  • Concentrations: 0 to 10 μM
  • Incubation Time: 48 hours or 72 hours
  • Method: AZD5438 is tested against solid tumor cell lines. Briefly, cells are incubated for 48 hours 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 hours. Cell growth is measured using AlamarBlue and GI50 values are calculated with reference to pretreatment control values.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: MCF-7, HCT-116, A549, and IM-9 cells are injected s.c. into the Swiss nude mice and nude rats.
  • Dosages: ≤100 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 74 mg/mL (199.21 mM)
Ethanol 74 mg/mL (199.21 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 371.46


CAS No. 602306-29-6
Storage powder
in solvent
Synonyms N/A
Smiles CC1=NC=C(N1C(C)C)C2=NC(=NC=C2)NC3=CC=C(C=C3)S(=O)(=O)C

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID