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AZD5438
- Soluble in DMSO
- MF: C18H21N5O2S
- MW: 371.46
Description
AZD5438 is a potent, orally bioavailable CDK1, CDK2 and CDK9 inhibitor with reported IC50 values of 16 nM, 6 nM and 20 nM, respectively. It suppresses both cell-cycle and transcription-associated CDK signaling.
CDK1 and CDK2 regulate cell-cycle progression, while CDK9 controls transcriptional elongation through P-TEFb signaling. AZD5438 is useful for studying coordinated inhibition of proliferative and transcriptional CDK pathways in cancer models.
Key Features
- Potent CDK1/CDK2/CDK9 inhibitor
- Reported IC50: 16 nM (CDK1), 6 nM (CDK2), 20 nM (CDK9)
- Orally bioavailable pharmacological profile
- Antiproliferative activity in tumor cell models
Applications
- Cell-cycle kinase studies
- Transcriptional CDK pathway research
- Cancer cell proliferation assays
- CDK inhibitor profiling
More Information
| Parent CAS No. | 602306-29-6 |
|---|---|
| Chemical Name | 4-(1-isopropyl-2-methyl-1H-imidazol-5-yl)-N-(4-(methylsulfonyl)phenyl)pyrimidin-2-amine |
| SMILES | C1(NC2=CC=C(S(C)(=O)=O)C=C2)=NC=CC(C2N(C(C)C)C(C)=NC=2)=N1 |
| MFCD | MFCD11112135 |
| InChi | InChI=1S/C18H21N5O2S/c1-12(2)23-13(3)20-11-17(23)16-9-10-19-18(22-16)21-14-5-7-15(8-6-14)26(4,24)25/h5-12H,1-4H3,(H,19,21,22) |
| InChiKey | WJRRGYBTGDJBFX-UHFFFAOYSA-N |
| CID | 16747683 |
| Short Description | CDK(1/2/9) inhibitor |
References
- KF Byth 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, 8(7), 1856-1866.
- DS Boss et al. Safety, tolerability, pharmacokinetics and pharmacodynamics of the oral cyclin-dependent kinase inhibitor AZD5438 when administered at intermittent and continuous dosing schedules in patients (...). Ann. Oncol. 2010, 21(4), 884-894.
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