SNS-314

SKU: orb1226916

Description

SNS-314 is a potent, selective pan-Aurora kinase inhibitor with IC50 of 9 and 31 nM for Aurora A and Aurora B, repectively; demonstrates broad activity in vitro against multiple human cancer cell lines and exhibits significant in vivo activity against a wide range of tumor xenograft models; shows additive antiproliferative effects with carboplatin, gemcitabine, 5-FU, daunomycin, and SN-38 both in vitro and in vivo.Solid Tumors Phase 1 Discontinued(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.(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.

Key Properties

• CAS Number: 1146618-41-8
• MW: 527.04
• Purity: >98% (HPLC)
• Formula: C₁₉H₁₉ClN₆O₄S₃
• SMILES: CS(=O)(=O)O.C1=CC(=CC(=C1)Cl)NC(=O)NC2=NC=C(S2)CCNC3=NC=NC4=C3SC=C4
• Target: Aurora Kinase
• Solubility: 10 mM in DMSO

Bioactivity

• 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.
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• 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.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SNS-314 Mesylate | SNS314 | SNS 314

Quick Database Links

Gene Symbol

Aurora Kinase