2-Pyridinecarboxamide, 4-[4-[[[[2-fluoro-5-[1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl]phenyl]amino]carbonyl]amino]phenoxy]-N-methyl-

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2-Pyridinecarboxamide, 4-[4-[[[[2-fluoro-5-[1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl]phenyl]amino]carbonyl]amino]phenoxy]-N-methyl- Basic information
Product Name:2-Pyridinecarboxamide, 4-[4-[[[[2-fluoro-5-[1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl]phenyl]amino]carbonyl]amino]phenoxy]-N-methyl-
Synonyms:2-Pyridinecarboxamide, 4-[4-[[[[2-fluoro-5-[1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl]phenyl]amino]carbonyl]amino]phenoxy]-N-methyl-;APS6-45;APS6-45,calibrated,signaling,TCI,Inhibitor,APS-6-45,APS645,Carcinoma,Thyroid,Ras,antitumor,Medullary,MAPK,APS6 45,tumor,inhibit;4-(4-(3-(2-Fluoro-5-(perfluoropropan-2-yl)phenyl)ureido)phenoxy)-N-methylpicolinamide;APS6-45, 10 mM in DMSO;4-[4-[[2-fluoro-5-(1,1,1,2,3,3,3-heptafluoropropan-2-yl)phenyl]carbamoylamino]phenoxy]-N-methylpyridine-2-carboxamide;APS6-45 ，S3493;N-(2-fluoro-4-(1,1,2,2,3,3,3-heptafluoropropyl)phenyl)-N'-(4-((5-(methylcarbamoyl)pyridin-3-yl)oxy)phenyl)urea
CAS:2188236-41-9
MF:C23H16F8N4O3
MW:548.39
EINECS:
Product Categories:
Mol File:2188236-41-9.mol
2-Pyridinecarboxamide, 4-[4-[[[[2-fluoro-5-[1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl]phenyl]amino]carbonyl]amino]phenoxy]-N-methyl- Structure
2-Pyridinecarboxamide, 4-[4-[[[[2-fluoro-5-[1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl]phenyl]amino]carbonyl]amino]phenoxy]-N-methyl- Chemical Properties
solubility DMF: 5 mg/ml
DMSO: 10 mg/ml
Ethanol: 10 mg/ml
form Solid
color Off-white to light yellow
Safety Information
MSDS Information
2-Pyridinecarboxamide, 4-[4-[[[[2-fluoro-5-[1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl]phenyl]amino]carbonyl]amino]phenoxy]-N-methyl- Usage And Synthesis
UsesAPS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity[1].
in vivo

APS6-45 (10 mg/kg; p.o. daily for 30 d) inhibits growth of TT tumors in mice and does not affect body weight[1].
APS6-45 (0.1-160 mg/kg; a single p.o.) does not cause detectable toxic effects in mice[1].
APS6-45 (20 mg/kg; a single p.o.) exhibits long half-life (5.6 h), Cmax (9.7 μM) and AUC0-24 (123.7 μMh) in mice[1].

Animal Model:Female nude mice (6 weeks) are implanted with TT cells[1]
Dosage:10 mg/kg
Administration:P.o. daily for 30 days
Result:Led to partial or complete responses in 75% and was well tolerated.
Animal Model:Male ICR mice (6 weeks of age)[1]
Dosage:20 mg/kg (Pharmacokinetic Analysis)
Administration:A single p.o.
Result:T1/2=5.6 h, Cmax=9.7 μM, AUC0-24=123.7 μMh.
References[1] Sonoshita M, et, al. A whole-animal platform to advance a clinical kinase inhibitor into new disease space. Nat Chem Biol. 2018 Mar;14(3):291-298. DOI:10.1038/nchembio.2556
2-Pyridinecarboxamide, 4-[4-[[[[2-fluoro-5-[1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl]phenyl]amino]carbonyl]amino]phenoxy]-N-methyl- Preparation Products And Raw materials
Tag:2-Pyridinecarboxamide, 4-[4-[[[[2-fluoro-5-[1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl]phenyl]amino]carbonyl]amino]phenoxy]-N-methyl-(2188236-41-9) Related Product Information
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