Crizotinib, (S)-

Based on 16 reference(s) in Google Scholar 9 10 16

Axon 2296

CAS [1374356-45-2]

MF C21H22Cl2FN5O
MW 450.34

  • Purity: 99%
  • Optical purity: 98.5 % e.e.
  • Soluble in DMSO

Crizotinib, (S)-

Description

(S)-Crizotinib is a selective inhibitor of the human mutT homologue MTH1 (also known as NUDT1; IC50 value 72 nM; Kd value 48 nM). MTH1 inhibition by (S)-Crizotinib induced an increase in DNA single-strand breaks, activated DNA repair in human colon carcinoma cells, and effectively suppressed tumor growth in animal models.
It is the opposite (S)-enantiomer of (R)-Crizotinib (PF-02341066, Axon 1660), which is a ALK/MET inhibitor. MTH1 (human mutT homologue, or NUDT1) has been implicated in aiding RAS-transformed cells to overcome oncogene-induced senescence by preventing reactive oxygen species (ROS)-induced DNA damage.

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The purity of Axon Ligands™ is confirmed by HPLC-MS, 1H-NMR and/or microanalysis. Analytical data are available upon request.

Caution: Axon Ligands™ are not fully tested. They are for research purposes only! Not for human consumption!

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