TAK-901

SKU: orb1223605

Description

A multikinase inhibitor with IC50 of 21 nM and 15 nM for Aurora A/TPX2 and Aurora B/INCENP respectively; inhibits 56 kinases(IC50< 100 nM); inhibits kinds of cancer cell lines with EC50s of 40-500 nM; suppresses cellular histone H3 phosphorylation and induced polyploidy.Blood Cancer Phase 1. Discontinued

Key Properties

• CAS Number: 934541-31-8
• MW: 504.6437
• Purity: >98% (HPLC)
• Formula: C₂₈H₃₂N₄O₃S
• SMILES: O=C(C1=C(C)C2=C(C(C3=CC=CC(S(=O)(CC)=O)=C3)=C1)C4=CC(C)=CN=C4N2)NC5CCN(C)CC5
• Target: Aurora Kinase
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  In rodent xenografts, TAK-901 exhibits potent activity against multiple human solid tumor types, and complete regression is observed in the ovarian cancer A2780 model. TAK-901 also displayed potent activity against several leukemia models. TAK-901 induces pharmacodynamic responses consistent with Aurora B inhibition and correlating with retention of TAK-901 in tumor tissue.
• In Vitro:
  TAK-901 exhibits time-dependent, tight-binding inhibition of Aurora B, but not Aurora A. Consistent with Aurora B inhibition, TAK-901 suppresses cellular histone H3 phosphorylation and induces polyploidy. In various human cancer cell lines, TAK-901inhibits cell proliferation with effective concentration values from 40 to 500 nM. Examination of a broad panel of kinases in biochemical assays reveals inhibition of multiple kinases. However, TAK-901 potently inhibits only a few kinases other than Aurora B in intact cells, including FLT3 and FGFR2.

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

TAK901 | TAK 901

Quick Database Links

Gene Symbol

Aurora Kinase