Product Description
AZD5438 is an orally-bioavailable imidazole-pyrimidine inhibitor of cyclin dependent kinase (CDK) 1, 2, and 9 at IC50s of 16, 6, and 20 nM, respectively. In vitro AZD5438 showed significant antiproliferative activity in human tumor cell lines with IC50s in the range of 0.2-1.7 uM, inhibiting phosphorylation of CDK substrates pRb, nucleolin, protein phosphatase 1a, and RNA polymerase II carboxylate-terminus. AZD5438 blocks cell cycling at the G2-M, S, and G1 phases and maintains suppression of biomarkers such as phospho-pRbSer249/Thr252 for up to 16h following a single oral dose in SW620 cells. [1]
Technical information:
| Chemical Formula: | C18H21N5O2S | |
| CAS #: | 602306-29-6 | |
| Molecular Weight: | 371.46 | |
| Purity: | >98% | |
| Appearance: | Pale Orange | |
| Chemical Name: | 4-(1-isopropyl-2-methyl-1H-imidazol-5-yl)-N-(4-(methylsulfonyl)phenyl)pyrimidin-2-amine | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | AZD-5438, AZD 5438, AZD5438 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature. Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | 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, 1856-1866. Pubmed ID: 19509270 |
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