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9、ction, NJ 08852, USAPage 6 of 6 www.MedChemETAS-120Cat. No.: HY-100818CAS No.: 1448169-71-8Molecular Formula: CHNOMolecular Weight: 418.45Target: FGFRPathway: Protein Tyrosine Kinase/RTKStorage: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 monthSolvent & SolubilityIn Vitro DMSO : 29 m
10、g/mL (69.30 mM)* “ means soluble, but saturation unknown.ConcentrationSolvent Mass 1 mg 5 mg 10 mg1 mM 2.3898 mL 11.9489 mL 23.8977 mL5 mM 0.4780 mL 2.3898 mL 4.7795 mLPreparing Stock Solutions10 mM 0.2390 mL 1.1949 mL 2.3898 mLPlease refer to the solubility information to select the appropriate sol
11、vent.BIOLOGICAL ACTIVITYDescription TAS-120 is a novel, potent and highly selective FGFR inhibitor, used for antitumor treatment.IC & Target FGFRIn Vivo TAS-120 (3, 30, 100 mg/kg/day, p.o.) exerts an anti-tumor effect in mice. TAS-120 shows anti-tumor effect by administering at moderate intervals, s
12、uch as intermittent administration of every other day dosing and 2 times/week, and reducing the sustained elevation and weight suppression blood phosphorus level, and take a antitumor effective as daily administration1.PROTOCOLProduct Data Sheet InhibitorsAgonistsScreening Librarieswww.MedChemE1Kina
13、se Assay 1 In the inhibitory activity measurement of compounds it is first serially diluted as with test compound dimethyl sulfoxide (DMSO) to 20 times the concentration of the final concentration. Then, reaction buffer (15 mM Tris-HCl pH7.5,0.01% Tween-20, 2 mM DTT) purified human FGFR2 protein in,
14、 FL-Peptide 22 (final concentration 1.5 M), magnesium chloride (final concentration 5 mM), ATP (final concentration is final concentration and incubated with the kinase reaction for 120 minutes at 25C by adding 5%) of 75 M) and test compound in DMSO (DMSO. EDTA diluted in (final concentration 30 mM)
15、 are the kinase reaction is stopped by adding. Finally, LabChip (TM) 3000 system (an excitation wavelength of 488 nm, detection wavelength 530 nm) separating the phosphorylated peptide and a non-phosphorylated peptide by measuring the amount of each, and phosphorus from the ratio to determine the oxidation reaction amount is defined the compound concentration able to inhibit the phosphorylation reac
