AZD 5438
Synonym(s):4-[2-Methyl-1-(1-methylethyl)-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine;AZD 5438;AZD-5438
- CAS NO.:602306-29-6
- Empirical Formula: C18H21N5O2S
- Molecular Weight: 371.46
- MDL number: MFCD11112135
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-08 20:21:46
What is AZD 5438?
The Uses of AZD 5438
AZD 5438 is a potent oral inhibitor of cyclin-dependent kinases 1, 2, and 9, which leads to leads to pharmacodynamic changes and potent antitumor effects in human tumor xenografts.
What are the applications of Application
AZD 5438 is an antiproliferative agent and potent inhibitor of cyclin-dependent kinases Cdk1, Cdk2, and Cdk9
Definition
ChEBI: 4-(2-methyl-3-propan-2-yl-4-imidazolyl)-N-(4-methylsulfonylphenyl)-2-pyrimidinamine is a sulfonamide.
Biological Activity
azd5438 is a potent small molecule inhibitor of cyclin-dependent kinase (cdk) 1, 2 and 9 with half maximal inhibitory concentration ic50 of 16 nmol/l, 6 nmol/l and 20 nmol/l respectively. azd5438 has also been found to potently inhibit the human cyclin e/cdk2 complex, the cyclin b1/cdk1 complex and the cyclin a/cdk2 complex with ic50 of 0.006 μm, 0.016 μm and 0.045 μm respectively. in previous studies, azd5438 has exhibited significant anti-proliferative activity in a few human tumor cell lines with ic50 ranging from 0.2 μmol/l to 1.7 μmol/l, in which the phosphorylation of a few proteins, including cdk substrates prb, nucleolin, protein phosphatase 1a and rna polymerase ii cooh-terminal domain, and cell cycling at g2-m, s and g1 phases were inhibited.
storage
Desiccate at RT
References
[1]camidge dr1, smethurst d, growcott j, barrass nc, foster jr, febbraro s, swaisland h, hughes a. a first-in-man phase i tolerability and pharmacokinetic study of the cyclin-dependent kinase-inhibitor azd5438 in healthy male volunteers. cancer chemother pharmacol. 2007 aug;60(3):391-8. epub 2006 nov 18.
[2]byth kf, thomas a, hughes g, forder c, mcgregor a, geh c, oakes s, green c, walker m, newcombe n, green s, growcott j, barker a, wilkinson rw. 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. doi: 10.1158/1535-7163.mct-08-0836. epub 2009 jun 9.
Properties of AZD 5438
Boiling point: | 655.2±65.0 °C(Predicted) |
Density | 1.31 |
storage temp. | Keep in dark place,Inert atmosphere,2-8°C |
solubility | insoluble in H2O; ≥18.55 mg/mL in DMSO; ≥42.1 mg/mL in EtOH |
form | solid |
pka | 4.08±0.50(Predicted) |
color | White to light yellow |
Safety information for AZD 5438
Computed Descriptors for AZD 5438
New Products
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