Shanghai Nianxing Industrial Co., Ltd
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Product Name: K-80003
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1292821-90-9

1292821-90-9 structure

1292821-90-9 structure

Name: K-80003
Chemical Name: K-80003
CAS Number: 1292821-90-9
Molecular Formula: C₂₂H₂₁FO₂
Molecular Weight: 336.399
Catalog: Research Areas Cancer
Create Date: 2018-01-02 16:22:03
Modify Date: 2025-08-26 07:41:13
K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.

Name	K-80003
Synonyms	4S7931G4PP [(1Z)-5-Fluoro-1-(4-isopropylbenzylidene)-2-methyl-1H-inden-3-yl]acetic acid 1H-Indene-3-acetic acid, 5-fluoro-2-methyl-1-[[4-(1-methylethyl)phenyl]methylene]-, (1Z)- [5-fluoro-1-(4-isopropylbenzylidene)-2-methylinden-3-yl]acetic acid

Description	K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.
Related Catalog	Research Areas >> Cancer
Target	Akt
In Vitro	When MCF-7 cells are cotreated with K-80003, TNFα-induced colocalization of tRXRα with p85α in the cytoplasm is inhibited, resulting in tRXRα nuclear localization. Western blotting shows that K-80003-stabilized tetrameric form of tRXRα is found exclusively in the nuclear fraction, while tRXRα monomer is distributed both in the nuclear and cytoplasmic fractions[2].
In Vivo	K-80003 is a potent inhibitor of AKT activation by all-trans-retinoic acid. K-80003 displays enhanced efficacy in inhibiting tRXRα-dependent AKT activation and tRXRα tumor growth in animals. K-80003 has high affinity to RXRα but lacks COX inhibitory activity[1].
Cell Assay	MCF-7 cells cotransfected with Myc-RXRα, Myc-tRXRα, tRXRα/L433D and p85α are pretreated with or without K-80003 (5 μM) for 3 h before exposed to TNFα (10 ng/mL) for 30 min. Cells are immunostained with anti-Myc and anti-p85α antibody, and their subcellular localization revealed by confocal microscopy. HEK293T cells cotransfected with Myc-tRXRα are treated with or without K-80003 (5 μM) for 6 h. Nuclear (N) and cytoplasmic (C) fractions are prepared, subjected to BS3 crosslinking, and analysed by western blotting using anti-Myc antibody. The purity of fractions is examined by analysing the expression of nuclear PARP and cytoplasmic α-tubulin in non-crosslinked fractions. One of three similar experiments is shown[2].
Animal Admin	Mice[1] Nude mice (BALB/c, 4-5-week old) are injected subcutaneously with 100 μL of cells (2×106). For drug treatment, mice (n=6) are treated intraperitoneally after 7 days of transplantation with Corn oil, Sulindac (60 mg/kg), or K-80003 (60 mg/kg) once every other day (six injections). Body weight and tumor sizes are measured every 4 days.
References	[1]. Zhou H, et al. NSAID sulindac and its analog bind RXRalpha and inhibit RXRalpha-dependent AKT signaling. Cancer Cell. 2010 Jun 15;17(6):560-73. [2]. Chen L, et al. Modulation of nongenomic activation of PI3K signalling by tetramerization of N-terminally-cleaved RXRα. Nat Commun. 2017 Jul 17;8:16066.

Density	1.2±0.1 g/cm3
Boiling Point	491.6±40.0 °C at 760 mmHg
Molecular Formula	C₂₂H₂₁FO₂
Molecular Weight	336.399
Flash Point	251.1±27.3 °C
Exact Mass	336.152557
LogP	6.60
Vapour Pressure	0.0±1.3 mmHg at 25°C
Index of Refraction	1.615
Storage condition	2-8℃

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