(S)-Crizotinib

Cat. No. 6025

(S)-Crizotinib C21H22Cl2FN5O [1374356-45-2]

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Chemical Name: 3-[(1S)-1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-2-pyridinamine

Biological Activity

Potent MTH1 inhibitor (IC50 = 72 nM). Induces DNA damage and disrupts nucleotide pool homeostasis in cancer cells. Also attenuates colony formation of KRAS-mutated PANC1 cells in vitro. Suppresses tumor growth ~50% in a colon cancer carcinoma xenograft model.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc

Technical Data

M.Wt:
450.34
Formula:
C21H22Cl2FN5O
Solubility:
Soluble to 50 mM in DMSO and to 20 mM in 1eq. HCl with gentle warming
Purity:
>98 %
Storage:
Store at RT
CAS No:
1374356-45-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

Huber et al (2014) Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy. Nature 508 222. PMID: 24695225.

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Keywords: (S)-Crizotinib, supplier, potent, MTH1, inhibitors, inhibits, ras, transformation, anticancer, hydrolases, g, proteins, mutT, homologue, NUDT1, nucleotide, pool, homeostasis, DNA, damage, Tocris Bioscience, MTH1 Inhibitor products

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