(S)-Crizotinib

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Cat.No. 6025 - (S)-Crizotinib | C21H22Cl2FN5O | CAS No. 1374356-45-2
Description: MTH1 inhibitor
Chemical Name: 3-[(1S)-1-(2,6-Dichloro-3-fluorophenyl)ethoxy]-5-[1-(4-piperidinyl)-1H-pyrazol-4-yl]-2-pyridinamine
Purity: ≥98% (HPLC)
Datasheet
Citations
Literature

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
Storage Store at RT
Purity ≥98% (HPLC)
CAS Number 1374356-45-2
PubChem ID 56671814
InChI Key KTEIFNKAUNYNJU-LBPRGKRZSA-N
Smiles C[C@@H](C1=C(C(F)=CC=C1Cl)Cl)OC2=CC(C3=CN(C4CCNCC4)N=C3)=CN=C2N

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
1eq. HCl 9.01 20mM with gentle warming
DMSO 22.52 50
ethanol 9.01 20

Preparing Stock Solutions

The following data is based on the product molecular weight 450.34. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.22 mL 11.1 mL 22.21 mL
5 mM 0.44 mL 2.22 mL 4.44 mL
10 mM 0.22 mL 1.11 mL 2.22 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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Product Datasheets

Safety Datasheet

References

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: potent MTH1 inhibitors inhibits ras transformation anticancer hydrolases g proteins mutT homologue NUDT1 nucleotide pool homeostasis DNA damage MutT homolog-1 (MTH1)

Citations for (S)-Crizotinib

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Literature in this Area

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Cancer Metabolism

Cancer Metabolism Poster

Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the main targets for cancer metabolism researchers. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways. These distinct metabolic circuits could provide viable cancer therapeutic targets.

Epigenetics in Cancer

Epigenetics in Cancer Poster

Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

Pathways for (S)-Crizotinib

Protocols

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