| Identification | Back Directory | [Name]
2-Pyridinecarboxamide, 4-[4-[[[[2-fluoro-5-[1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl]phenyl]amino]carbonyl]amino]phenoxy]-N-methyl- | [CAS]
2188236-41-9 | [Synonyms]
APS6-45
2-Pyridinecarboxamide, 4-[4-[[[[2-fluoro-5-[1,2,2,2-tetrafluoro-1-(trifluoromethyl)ethyl]phenyl]amino]carbonyl]amino]phenoxy]-N-methyl- | [Molecular Formula]
C23H16F8N4O3 | [MDL Number]
MFCD32874100 | [MOL File]
2188236-41-9.mol | [Molecular Weight]
548.39 |
| Hazard Information | Back Directory | [Uses]
APS6-45 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 μM?h) 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 μM?h. |
| [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 |
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