Description
APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity.
Product information
CAS Number: 2188236-41-9
Molecular Weight: 548.39
Formula: C23H16F8N4O3
Chemical Name: 4-[4-({[2-fluoro-5-(1,1,1,2,3,3,3-heptafluoropropan-2-yl)phenyl]carbamoyl}amino)phenoxy]-N-methylpyridine-2-carboxamide
Smiles: CNC(=O)C1=CC(=CC=N1)OC1C=CC(=CC=1)NC(=O)NC1=CC(=CC=C1F)C(F)(C(F)(F)F)C(F)(F)F
InChiKey: MVUPJRHPAMCBQJ-UHFFFAOYSA-N
InChi: InChI=1S/C23H16F8N4O3/c1-32-19(36)18-11-15(8-9-33-18)38-14-5-3-13(4-6-14)34-20(37)35-17-10-12(2-7-16(17)24)21(25,22(26,27)28)23(29,30)31/h2-11H,1H3,(H,32,36)(H2,34,35,37)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 250 mg/mL (455.88 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
APS6-45 (3-30 nM; 3 weeks) strongly suppresses TT human Medullary Thyroid Carcinoma (MTC) cells colony formation in a soft agar assay. APS6-45 (1 μM; 1 h) strongly inhibits RAS pathway activity signaling in human MTC cell lines TT and MZ-CRC-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. APS6-45 (0.1-160 mg/kg; a single p.o.) does not cause detectable toxic effects in mice. 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.
Products are for research use only. Not for human use.
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