(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.
CAS Number: 1374356-45-2
Molecular Weight: 450.34
Chemical Name: (S)-3-(1-(2,6-dichloro-3-fluorophenyl)ethoxy)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine
Appearance: Solid powder
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: 42 mg/mL (93.26 mM); EtOH: 22 mg/mL (48.85 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Powder: 4oC for 1year, -20oC for 3 years; DMSO: 4oC for 3 months.
Shelf Life: ≥36 months if stored properly.
Stock Solution Storage: 0-4oC for short term (days to weeks), or -20oC for long term (months).
Drug Formulation: This drug may be formulated in DMSO
HS Tariff Code: 2934.99.9001
How to use
(S)-Crizotinib was used at 2-10 µM final concentration in various in vitro and cellular assays.
(S)-Crizotinib was dosed to mice orally at 50?mg/kg once per day to impair tumor growth in an SW480 colon carcinoma xenograft model. Formulation is 1% DMSO, 10% ethanol, 10% Cremophor, 10% Tween 80, 69% PBS.
- Huber KV, et al. Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy. (2014) Nature. 508(7495):222-7.
Products are for research use only. Not for human use.
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