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(S)-crizotinib

CAS No. 1374356-45-2

(S)-crizotinib( (S)-Crizotinib | S-Crizotinib )

Catalog No. M17983 CAS No. 1374356-45-2

(S)-crizotinib（IC50 of 72 nM）, an effective MTH1 (NUDT1) inhibitor, is the (S)-enantiomer of crizotinib.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    (S)-crizotinib
  • Note
    Research use only, not for human use.
  • Brief Description
    (S)-crizotinib（IC50 of 72 nM）, an effective MTH1 (NUDT1) inhibitor, is the (S)-enantiomer of crizotinib.
  • Description
    (S)-Crizotinib is an MTH1 inhibitor. By inhibiting MTH1, (S)-Crizotinib disrupts nucleotide pool homeostasis, induces an increase in DNA single-strand breaks, activates DNA repair in human colon carcinoma cells, and effectively suppresses tumor growth in animal models.
  • In Vitro
    Cell Viability Assay Cell Line:NSCLC cells, NCI-H460, H1975 and A549 cells Concentration:0.625, 1.25, 2.5, 5, 10, 20, 40, 60, 80 μM Incubation Time:24 hours Result:Decreased the viability of NCI-H460, H1975 and A549 cells with IC50 values of 14.29, 16.54 and 11.25 μM, respectively.Apoptosis Analysis Cell Line:NSCLC cells, NCI-H460, H1975 and A549 cells Concentration:10, 20 or 30 μM Incubation Time:24 hours Result:Induced cells apoptosis.Western Blot Analysis Cell Line:NSCLC cells, NCI-H460, H1975 and A549 cells Concentration:10, 20 or 30 μM Incubation Time:24 hours Result:Decreased Bcl-2: Bax ratio.
  • In Vivo
    Animal Model:Five-week-old, athymic BALB/c nu/nu female mice (17-19 g) with NCI-H460 cells Dosage:7.5 or 15 mg/kg Administration:Intraperitoneal injections; once daily for 10 days Result:Resulted in significant reductions in both tumor volume and tumor weight.
  • Synonyms
    (S)-Crizotinib | S-Crizotinib
  • Pathway
    GPCR/G Protein
  • Target
    Calcium Channel
  • Recptor
    MTH1
  • Research Area
    Cancer
  • Indication
    ——

Chemical Information

  • CAS Number
    1374356-45-2
  • Formula Weight
    450.34
  • Molecular Formula
    C21H22Cl2FN5O
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 12.5 mg/mL (27.76 mM)
  • SMILES
    C[C@@H](c1c(ccc(c1Cl)F)Cl)Oc1c(ncc(c1)c1cn(nc1)C1CCNCC1)N
  • Chemical Name
    3-[(1S)-1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-2-pyridinamine

Shipping & Storage Information

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

Reference

1. Huber KV, et al. Nature. 2014 , 508(7495), 222-227.
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