Name | N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea |
Synonyms | SNS314 CS-901 SNS 314 SNS-314 SNS-314 free base 1-(3-chlorophenyl)-3-(5-(2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl)thiazol-2-yl)urea 1-(3-chlorophenyl)-3-(4-(2-(thieno[3,2-d]pyriMidin-4-ylaMino)ethyl)thiazol-2-yl)urea N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea Urea, N-(3-chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]- |
CAS | 1057249-41-8 |
Molecular Formula | C18H15ClN6OS2 |
Molar Mass | 430.93 |
Density | 1.588 |
Solubility | DMSO:100 mg/mL (232.06 mM) |
pKa | 6.12±0.70(Predicted) |
Storage Condition | -20°C |
In vitro study | SNS-314 potent inhibition of tumor cell lines, the IC50 was 1.8 to 24 nM, independent of the relative Aurora-A of cells or Aurora-B protein levels. SNS-314 inhibiting the phosphorylation of histone H3 at Ser10 site, the mitosis of HCT116 cells was disturbed. Consecutive treatment with SNS-314 and Carboplatin, Gemcitabine, 5-FU, Daunomycin, and SN-38 showed a potentiated antiproliferative effect, and the combination of SNS-314 and Gemcitabine,Docetaxel, or Vincristine showed a synergistic effect. |
In vivo study | SNS-314 acts on HCT116 colon transplantation tumor and shows obvious and long-lasting anti-cancer effect. SNS-314 at 170 mg/kg for human breast cancer (MDA-MB-231), prostate cancer (PC-3), lung cancer (H1299 and Calu-6), ovarian cancer (A2780), and malignant melanoma (A375) the murine xenografts also showed significant anticancer activity, with tumor growth inhibition rates ranging from 54 to 91%. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.321 ml | 11.603 ml | 23.205 ml |
5 mM | 0.464 ml | 2.321 ml | 4.641 ml |
10 mM | 0.232 ml | 1.16 ml | 2.321 ml |
5 mM | 0.046 ml | 0.232 ml | 0.464 ml |
biological activity | SNS-314 is A potent, selective inhibitor of Aurora A, Aurora B, and Aurora C, the IC50 was 9 nM, 31 nM, and 3 nM, respectively, and the effect on Trk A/B, Flt4, Fms, Axl, c-Raf, and DDR2 was slightly weaker. Phase 1. |
Target | Value |
Aurora C | 3 nM |
Aurora A | 9 nM |
Aurora B | 31 nM |