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TAK-901

CAS No. 934541-31-8

TAK-901( TAK901 | TAK 901 )

Catalog No. M16681 CAS No. 934541-31-8

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).

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    TAK-901
  • Note
    Research use only, not for human use.
  • Brief 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).
  • 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
  • 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.
  • 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.
  • Synonyms
    TAK901 | TAK 901
  • Pathway
    Cell Cycle/DNA Damage
  • Target
    Aurora Kinase
  • Recptor
    CLK2|c-Src|FGR|JAK3|Yes1
  • Research Area
    Cancer
  • Indication
    Blood cancer

Chemical Information

  • CAS Number
    934541-31-8
  • Formula Weight
    504.6437
  • Molecular Formula
    C28H32N4O3S
  • Purity
    >98% (HPLC)
  • Solubility
    10 mM in DMSO
  • 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
  • Chemical Name
    9H-Pyrido[2,3-b]indole-7-carboxamide, 5-[3-(ethylsulfonyl)phenyl]-3,8-dimethyl-N-(1-methyl-4-piperidinyl)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Farrell P, et al. Mol Cancer Ther. 2013 Apr;12(4):460-70. 2. Murai S, et al. Anticancer Res. 2017 Feb;37(2):437-444.
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