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AZD-5438

Catalog No. T2506   CAS 602306-29-6
Synonyms: AZD5438

AZD-5438 is an effective inhibitor of CDK, for CDK1(IC50=16 nM), CDK2(IC50=6 nM), CDK9(IC50=20 nM).

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AZD-5438 Chemical Structure
AZD-5438, CAS 602306-29-6
Pack Size Availability Price/USD Quantity
5 mg In stock $ 44.00
10 mg In stock $ 63.00
25 mg In stock $ 113.00
50 mg In stock $ 189.00
100 mg In stock $ 342.00
1 mL * 10 mM (in DMSO) In stock $ 62.00
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Purity: 99.87%
Purity: 99.23%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description AZD-5438 is an effective inhibitor of CDK, for CDK1(IC50=16 nM), CDK2(IC50=6 nM), CDK9(IC50=20 nM).
Targets&IC50 CDK1:16 nM, CDK9:20 nM, CDK2:6 nM
In vitro In the SW620 xenograft model, AZD5438 exhibits dose-dependent inhibition on various cell cycle proteins, such as phospho-histone H3 (phH3), phospho-nucleophosmin, and PP1a. AZD5438, administered orally, demonstrates tumor-suppressive effects across various cancer types including breast, colon, lung, prostate, and ovarian cancers.
In vivo AZD5438 effectively inhibits the kinase activity of p25-cdk5 and glycogen synthase kinase 3β, with IC50 values of 14 nM and 17 nM, respectively. In various tumor cell lines (lung, colorectal, breast, prostate, and blood tumors), AZD5438 (IC50=0.2-1.7 μM) induces cell cycle arrest and inhibits cell proliferation by hindering the phosphorylation of cdk-dependent substrates. Furthermore, AZD5438 demonstrates potent inhibition of cyclin-dependent kinases (cdks) including E-cdk2 (IC50=6 nM), A-cdk2 (IC50=45 nM), B1-cdk1 (IC50=16 nM), D3-cdk6 (IC50=21 nM), and T-cdk9 (IC50=20 nM), showcasing its broad efficacy in targeting various components of the cell cycle mechanism.
Kinase Assay 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 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)
Synonyms AZD5438
Molecular Weight 371.46
Formula C18H21N5O2S
CAS No. 602306-29-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 63 mg/mL(169.6 mM)

DMSO: 74 mg/mL (199.21 mM)

TargetMolReferences and Literature

1. Byth KF, et al. Mol Cancer Ther. 2009, 8(7), 1856-1866.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Cardiovascular Disease Compound Library Drug Repurposing Compound Library Anti-Pancreatic Cancer Compound Library ReFRAME Related Library Target-Focused Phenotypic Screening Library Anti-Aging Compound Library Cell Cycle Compound Library

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Keywords

AZD-5438 602306-29-6 Cell Cycle/Checkpoint CDK Cyclin dependent kinase AZD5438 inhibit AZD 5438 Inhibitor inhibitor

 

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