An MTH1 inhibitor
Related Products
Enantiomer(s)
12087(R)-Crizotinib
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(S)-Crizotinib

Item No. 31114

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3-[(1S)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-2-pyridinamine
CAS Number
1374356-45-2
Molecular Formula
C21H22Cl2FN5O
Formula Weight
450.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 0.5 mg/mlEthanol: 0.5 mg/ml
λmax
270 nm
SMILES
FC1=CC=C(Cl)C([C@H](C)OC2=CC(C3=CN(C4CCNCC4)N=C3)=CN=C2N)=C1Cl
InChi Code
InChI=1S/C21H22Cl2FN5O/c1-12(19-16(22)2-3-17(24)20(19)23)30-18-8-13(9-27-21(18)25)14-10-28-29(11-14)15-4-6-26-7-5-15/h2-3,8-12,15,26H,4-7H2,1H3,(H2,25,27)/t12-/m0/s1
InChi Key
KTEIFNKAUNYNJU-LBPRGKRZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    (S)-Crizotinib is an inhibitor of muT homolog 1 (MTH1; IC50 = 72 nM).1 It is selective for MTH1 over a panel of 456 kinases at 1 µM. (S)-Crizotinib (30 µM) induces oxidative DNA damage and apoptosis in SGC-7901 and BGC-823 human gastric cancer cells.2 It inhibits proliferation in a panel of 14 cancer cell lines expressing wild-type or various mutant forms of K-Ras and p53 (IC50s = 0.52-7.4 µM).1 (S)-Crizotinib (25 mg/kg, s.c.) reduces tumor growth in an SW480 mouse xenograft model.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Huber, K.V.M., Salah, E., Radic, B., et al. Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy. Nature 508(7495), 222-227 (2014).

    2. Ji, J., Chen, W., Lian, W., et al. (S)-crizotinib reduces gastric cancer growth through oxidative DNA damage and triggers pro-survival akt signal. Cell Death Dis. 9(6), 660 (2018).