(S)-crizotinib --- MTH1 Inhibitor, CAS [[1374356-45-2]], Unconjugated
Biozol Catalog Number:
BSS-BS-60208C
Supplier Catalog Number:
bs-60208C
Alternative Catalog Number:
BSS-BS-60208C-10,BSS-BS-60208C-2
Manufacturer:
Bioss
Category:
Biochemikalien
Conjugation:
Unconjugated
(S)-Crizotinib is a novel potent, selective and cell permeable MTH1 inhibitor with an IC50 of ~72 nM. MTH1 is a nucleotide pool sanitizing enzyme. (S)-Crizotinib disrupts nucleotide pool homeostasis via MTH1 inhibition and induces an increase in DNA single-strand breaks in cancer cells. In vivo it can effectively suppress tumor growth in colon carcinoma xenograft model by once per day oral dosing. (R)-Crizotinib, which is (R)-enantiomer of the drug, is inactive against MTH1 in vitro. Loss-of-function of MTH1 impaired growth of KRAS tumor cells. (S)-Crizotinib is a useful chemical probe to further validate MTH1 as a promising novel class of anticancer target.
Buffer:
Powder
CAS Number:
[1374356-45-2]
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