Biological Activity
Potent MTH1 inhibitor (Kd = 49 nM). Inhibits Ras-induced malignant transformation and increases α-actin promoter-driven CAT activity in Ras-transformed cells. Has no effect on Ras-induced ERK and JNK activation. Inhibits Ras-induced membrane ruffling in REF-52 fibroblasts and blocks anchorage-independent growth of Ras-transformed tumor cell lines. Also induces DNA damage in SW480 colon cancer cells.
Compound Libraries
SCH 51344 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 316.35 |
| Formula | C16H20N4O3 |
| Storage | Store at -20°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 171927-40-5 |
| PubChem ID | 9995890 |
| InChI Key | YWEGXZZAORIRQR-UHFFFAOYSA-N |
| Smiles | CC1=NN=C(N3)C1=C(NCCOCCO)C2=C3C=CC(OC)=C2 |
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 | |||
| DMSO | 31.64 | 100 | |
| ethanol | 3.16 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 316.35. 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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.16 mL | 15.81 mL | 31.61 mL |
| 5 mM | 0.63 mL | 3.16 mL | 6.32 mL |
| 10 mM | 0.32 mL | 1.58 mL | 3.16 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.63 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Walsh et al (1997) SCH 51344-induced reversal of RAS-transformation is accompanied by the specific inhibition of the RAS and RAC-dependent cell morphology pathway. Oncogene 15 2553 PMID: 9399643
Kumar et al (1999) SCH 51344, an inhibitor of RAS/RAC-mediated cell morphology pathway. Ann.N.Y.Acad.Sci. 886 122 PMID: 10667210
Huber et al (2014) Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy. Nature 508 222 PMID: 24695225
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