Home>>APS6-45
APS6-45 Catalog No.GC60592

Size Price Stock Qty
10mM*1 mL in DMSO
$391.00
In stock
5mg
$324.00
In stock
10mg
$538.00
In stock
25mg
$1,020.00
In stock
50mg
$1,576.00
In stock
100mg
$2,318.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical Properties

Cas No. 2188236-41-9 SDF Download SDF
Synonyms N/A
Chemical Name N/A
Canonical SMILES O=C(C1=NC=CC(OC2=CC=C(C=C2)NC(NC3=CC(C(F)(C(F)(F)F)C(F)(F)F)=CC=C3F)=O)=C1)NC
Formula C23H16F8N4O3 M.Wt 548.39
Solubility DMSO: 250 mg/mL (455.88 mM) Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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Background

APS6-45 is an orally active tumor-calibrated inhibitor (TCI). APS6-45 inhibits RAS/MAPK signaling and exhibits antitumor activity[1].

APS6-45 (3-30 nM; 3 weeks) strongly suppresses TT human Medullary Thyroid Carcinoma (MTC) cells colony formation in a soft agar assay[1].APS6-45 (1 μM; 1 h) strongly inhibits RAS pathway activity signaling in human MTC cell lines TT and MZ-CRC-1[1].

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]

[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.