SCH 51344

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Cat.No. 5280 - SCH 51344 | C16H20N4O3 | CAS No. 171927-40-5
Description: Potent MTH1 inhibitor
Chemical Name: 2-[2-[(6-Methoxy-3-methyl-1H-pyrazolo[3,4-b]quinolin-4-yl)amino]ethoxy]ethanol
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature

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

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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

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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References

References are publications that support the biological activity of the product.

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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