4-[2-Methyl-1-isopropyl-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine
4-(1-isopropyl-2-methyl-1H-imidazol-5-yl)-N-(4-(methylsulfonyl)phenyl)pyrimidin-2-amine
CAS: 602306-29-6
Molecular Formula: C18H21N5O2S
4-[2-Methyl-1-isopropyl-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine - Names and Identifiers
4-[2-Methyl-1-isopropyl-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine - Physico-chemical Properties
| Molecular Formula | C18H21N5O2S |
| Molar Mass | 371.46 |
| Density | 1.31 |
| Boling Point | 655.2±65.0 °C(Predicted) |
| pKa | 4.08±0.50(Predicted) |
| Storage Condition | Keep in dark place,Inert atmosphere,2-8°C |
| In vitro study | AZD5438 on cyclin-dependent kinases, including cyclin E-cdk2, cyclin A- cdk2, cyclin B1-cdk1, cyclin D3-cdk6, and the activity of cyclin T-cdk9 showed potent inhibition with IC50 of 6 nM,45 nM,16 nM,21 nM, and 20 nM, respectively. In addition, AZD5438 also inhibited the kinase activity of p25-cdk5 and glycogen synthase kinase 3β with IC50 of 14 nM and 17 nM, respectively. AZD5438 induces cell cycle arrest by inhibiting the phosphorylation of cdk-dependent substrates and on a range of tumor cell lines, including lung, colorectal, breast, prostate, and hematologic tumors exhibited a broad range of anti-proliferative activity with IC50 values ranging from 0.2 μm (MCF-7) to 1.7 μm (ARH-77). |
| In vivo study | In vivo, oral AZD5438 therapy produces a statistically significant inhibitory effect on the growth of human tumor xenografts derived from a variety of different types of cancer, including breast, colon, lung, prostate and ovarian cancer, the maximum TGI ranged from 38% to 153%. In the SW620 xenograft model, AZD5438 produced dose-dependent inhibition of various cyclins, such as phH3, nucleolin phosphates, PP1a, and several phospho-pRb polypeptides. |
4-[2-Methyl-1-isopropyl-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.692 ml | 13.46 ml | 26.921 ml |
| 5 mM | 0.538 ml | 2.692 ml | 5.384 ml |
| 10 mM | 0.269 ml | 1.346 ml | 2.692 ml |
| 5 mM | 0.054 ml | 0.269 ml | 0.538 ml |
Last Update：2024-01-02 23:10:35
4-[2-Methyl-1-isopropyl-1H-imidazol-5-yl]-N-[4-(methylsulfonyl)phenyl]-2-pyrimidinamine - Reference Information
| biological activity | AZD5438 is an effective CDK1/2/9 inhibitor, and IC50 is 16 nM/6 nM/20 nM in cell-free test. The effect on CDK5/6 is slightly weak, and it also has inhibitory effect on GSK3β. Phase 1. |
| target | TargetValue CDK2 (Cell-Free Assay) 6 nM CDK1 (Cell-Free Assay) 16 nM CDK9 (Cell-Free Assay) 20 nM |
| Target | Value |
| CDK2 (Cell-free assay) | 6 nM |
| CDK1 (Cell-free assay) | 16 nM |
| CDK9 (Cell-free assay) | 20 nM |
| in vitro study | AZD5438 on cyclin-dependent kinases, including cyclin E-cdk2, cyclin A- cdk2, cyclin B1-cdk1, cyclin D3-cdk6, and the activity of cyclin T-cdk9 showed effective inhibition, IC50 was 6 nM,45 nM,16 nM,21 nM, and 20 nM respectively. In addition, AZD5438 also inhibits the kinase activity of p25-cdk5 and glycogen synthesis kinase 3β with IC50 of 14 nM and 17 nM, respectively. AZD5438 induces cell cycle arrest by inhibiting phosphorylation of cdk-dependent substrates and exhibits extensive antiproliferative activity against a range of tumor cell lines, including lung, colorectal, breast, prostate, and hematological tumors, with IC50 ranging from 0.2 μM (MCF-7) to 1.7 μM (ARH-77). |
| in vivo studies | in vivo, AZD5438 oral therapy has a statistically significant inhibitory effect on the growth of human tumor xenografts derived from various types of cancer, including breast cancer, colon cancer, lung cancer, prostate cancer and ovarian cancer, with the maximum TGI ranging from 38% to 153%. In the SW620 xenograft model, AZD5438 will produce dose-dependent inhibition on various cyclin, such as phH3, phosphonucleolin, PP1a, and several phosphate-pRb polypeptides. |
Last Update：2024-04-10 22:29:15
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Product Name: 4-(1-isopropyl-2-methyl-1H-imidazol-5-yl)-N-(4-(methylsulfonyl)phenyl)pyrimidin-2-amine Visit Supplier Webpage Request for quotation
CAS: 602306-29-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 602306-29-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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