1146618-41-8
1146618-41-8 structure
- Name: SNS-314 Mesylate
- Chemical Name: 1-(3-chlorophenyl)-3-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-1,3-thiazol-2-yl]urea,methanesulfonic acid
- CAS Number: 1146618-41-8
- Molecular Formula: C19H19ClN6O4S3
- Molecular Weight: 527.04000
- Catalog: Organic raw materials Amino compound Sulfonic acid amino compound
- Create Date: 2018-12-28 15:13:46
- Modify Date: 2024-01-13 15:08:47
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SNS-314 is a potent and selective aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively.
| Name | 1-(3-chlorophenyl)-3-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-1,3-thiazol-2-yl]urea,methanesulfonic acid |
|---|---|
| Synonyms |
SNS-314
SNS-314 Mesylate SNS314,SNS-314 Mesylate cc-347 SNS-314 Mesylate salt S1154_Selleck UNII-KGW32FDY3U |
| Description | SNS-314 is a potent and selective aurora kinase inhibitor with IC50s of 9, 31, and 6 nM for aurora A, B and C, respectively. |
|---|---|
| Related Catalog | |
| Target |
Aurora A:9 nM (IC50) Aurora B:31 nM (IC50) Aurora C:6 nM (IC50) |
| In Vitro | SNS-314 blocks proliferation in a broad panel of tumor cell lines (HCT116, A2780, PC-3, HeLa, MDA-MB-231, H-1299, and HT29) with IC50 values ranging from 1.8 nM in A2780 ovarian cancer cells to 24 nM in HT29 colon cancer cells[2]. |
| In Vivo | In the HCT116 human colon cancer xenograft model, administration of 50 and 100 mg/kg SNS-314 leads to dose-dependent inhibition of histone H3 phosphorylation for at least 10 h. SNS-314 shows significant tumor growth inhibition in a dose dependent manner under a variety of dosing schedules including weekly, bi-weekly, and 5 days on/9 days off[2]. |
| Kinase Assay | A homogeneous time-resolved fluorescence (HTRF)-based biochemical IC50 assay is used to test for the kinase activity of the three isoforms of Aurora (A, B, and C) in the presence of SNS-314. A biotin-conjugated histone H3 peptide is used as substrate. Aurora-A kinase (7.5 nM) is assayed in 10 mM Tris–HCl pH 7.2, 10 mM MgCl2, 0.1% BSA, 0.05% Tween 20, 1 mM DTT, 120 nM biotinylated peptide ARTKQTARKSTGGKAPRKQLA-GGK-biotin, 6 μM ATP (2×the Km for the enzyme) for 1 h at 25°C. The reaction is stopped with 200 mM EDTA. Aurora-B and Aurora-C are assayed at 5 nM enzyme concentration, 120 nM biotinylated peptide, and 300 lM ATP (29 the Km for the enzymes) for 1 h at 25°C[2]. |
| Cell Assay | HCT116 cells are treated with various concentrations of SNS-314 for 96 hours. cells are incubated with BrdU for 2 h at 37°C. Cell proliferation activity is evaluated by chemiluminescence detection of BrdU incorporated in DNA[2]. |
| Animal Admin | Mice: Tumor mice are treated with vehicle or SNS-314. Animals are weighed, monitored for signs or symptoms of toxic effects, and measured for tumor volumes twice weekly until an end point is met[2]. |
| References |
| Molecular Formula | C19H19ClN6O4S3 |
|---|---|
| Molecular Weight | 527.04000 |
| Exact Mass | 526.03200 |
| PSA | 217.78000 |
| LogP | 5.19310 |
| Storage condition | -20℃ |