(S)-Crizotinib

CAT: 0026-B3071-25Size: 25 mgDry Ice: NoHazardous: No
CAT#:0026-B3071-25Size:25 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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Description
(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 330 nM and 408 nM 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.
Shipping Conditions
RT
Storage Conditions
-20ºC
Shelf Life
36 months

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