Chemical Name: 2-[2-[(6-Methoxy-3-methyl-1H-pyrazolo[3,4-b]quinolin-4-yl)amino]ethoxy]ethanol
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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
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
Certificate of Analysis / Product Datasheet
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References
References are publications that support the products' biological activity.
Walshet 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
Kumaret al (1999) SCH 51344, an inhibitor of RAS/RAC-mediated cell morphology pathway. Ann.N.Y.Acad.Sci. 886 122 PMID: 10667210
Huberet al (2014) Stereospecific targeting of MTH1 by (S)-crizotinib as an anticancer strategy. Nature 508 222 PMID: 24695225