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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)
Biological Activity for (S)-Crizotinib
(S)-Crizotinib is a 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
Compound Libraries for (S)-Crizotinib
(S)-Crizotinib is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for (S)-Crizotinib
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for (S)-Crizotinib
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 22.52 | 50 | |
| 1eq. HCl | 9.01 | 20 with gentle warming |
Preparing Stock Solutions for (S)-Crizotinib
The following data is based on the product molecular weight 450.34. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 4.44 mL | 22.21 mL | 44.41 mL |
| 2.5 mM | 0.89 mL | 4.44 mL | 8.88 mL |
| 5 mM | 0.44 mL | 2.22 mL | 4.44 mL |
| 25 mM | 0.09 mL | 0.44 mL | 0.89 mL |
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Product Datasheets for (S)-Crizotinib
References for (S)-Crizotinib
References are publications that support the biological activity of the product.
Huber et al (2014) Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy. Nature 508 222 PMID: 24695225
If you know of a relevant reference for (S)-Crizotinib, please let us know.
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1 Citation for (S)-Crizotinib
Citations are publications that use Tocris products. Selected citations for (S)-Crizotinib include:
Noemi et al (2020) The Epstein-Barr virus nuclear antigen-1 upregulates the cellular antioxidant defense to enable B-cell growth transformation and immortalization. Oncogene 39 603-616 PMID: 31511648
Do you know of a great paper that uses (S)-Crizotinib from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Cancer Metabolism Research Product Guide
This product guide reviews some of the main areas in cancer metabolism research and lists around 150 products that can be used to investigate metabolic pathways in cancer including:
- Glycolysis
- Tricarboxylic Acid Cycle
- Lipidogenesis
- 1C Metabolism and Nucleic Acid Synthesis
- Drivers of Metabolic Reprogramming
- pH and Redox Balance
Cancer Metabolism Poster
This poster summarizes the main metabolic pathways in cancer cells and highlights potential targets for cancer therapeutics. Genetic changes and epigenetic modifications in cancer cells alter the regulation of cellular metabolic pathways providing potential cancer therapeutic targets.
Epigenetics in Cancer Poster
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.