(S)-Crizotinib

(S)-crizotinib is a low nanomolar inhibitor of 7, 8-dihydro-8-oxoguanine triphosphatase (MTH1 or NUDT1) whereas the (R)-enantiomer shows IC50 values in the micromolar range. MTH1 aids in RAS-transformed cells to overcome oncogene-induced senescence by preventing reactive oxygen species (ROS)-induced DNA damage. The average IC50 values for (S)-crizotinib and the MTH1 substrates 8-oxo-dGTP and 2-OH-dATP is 330nM and 408nM respectively. In vitro Kd measurements indicate that (S)-crizotinib is considerably less potent than the (R)-enantiomer against the targets ALK, MET and ROS1. (S)-crizotinib reduces tumor volume by more than 50% in mouse xenograft studies using SW480 cells.

https://pubchem.ncbi.nlm.nih.gov/compound/56671814

Small volumes of (S)-Crizotinib biochemical vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS8400511 is a biochemical targeting (S)-Crizotinib.