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产品名称 Crizotinib, (S)-
产品货号 Axon 2296 CAS [1374356-45-2] MF C21H22Cl2FN5OMW 450.34 Purity: 99% Optical purity: 98.5 % e.e. Soluble in DMSO 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. References Certificates Categories Extra info K.V.M. Huber et al. Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy. Nature. 2014, 508, 222-227. Certificate of Analysis Material Safety Data Sheet Cell Signaling & Oncology DNA-damage Response MTH1 EC 3.6.1.56 MTH1 inhibitor Chemical name (S)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine Parent CAS No. [1374356-45-2] Order Size Unit Price Stock 5 mg €85.00 In Stock
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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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