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Supinoxin

Catalog No. T16961 CAS 888478-45-3

Synonyms: RX-5902

Supinoxin is an orally active inhibitor of phosphorylated-p68 RNA helicase and a potent first-in-class anti-cancer agent. Supinoxin induces cell apoptosis and inhibits the growth of TNBC cancer cell lines (IC50s:10 nM - 20 nM).

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Supinoxin, CAS 888478-45-3

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Purity: 98%

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Chemical Properties

Storage & Solubility Information

Description	Supinoxin is an orally active inhibitor of phosphorylated-p68 RNA helicase and a potent first-in-class anti-cancer agent. Supinoxin induces cell apoptosis and inhibits the growth of TNBC cancer cell lines (IC50s:10 nM - 20 nM).
In vitro	Supinoxin inhibits cell growth, MDA-MB-231, Caki-1, UMRC2, PANC-1, A549, MKN-45, HepG2, HCT116, HT29, PC-3, U251, HeLa, SK-MEL-28 and OVCAR-3 (IC50: range from 0.01 μM to 0.021 μM in the growth inhibition of cancer cells). Supinoxin (0-10 μM; 72 hours) is active against cell lines of all TNBC molecular subtypes and is active against cell lines with mutations in p53, RB1, CDKN2A, and loss of PTEN. Supinoxin (20-100 nM; 24 hours) treatment causes a dose-dependent increase in tetraploid cells, consistent with induction of G2–M cell-cycle arrest. Supinoxin (0-100 nM; 24 or 48 hours) reduces MCL-1 expression in a dose-dependent manner in TNBC cell lines sensitive to Supinoxin. Supinoxin (0-100 nM; 72 hours) exhibits no significant induction of apoptosis in cell lines resistant to the antiproliferative effects of Supinoxin. But in sensitive cells, the observed activation of apoptosis begins at 24–48 hours and reaches a peak at 72 hours. The induced apoptosis is treated with a dose of 100 nM [1][2].
In vivo	Supinoxin (p.o.; 160/320/600 mg/kg; once weekly for 3 weeks) obviously dose-dependent tumor growth inhibition in the MDA-MB-231 model, exhibits TGI of 55.7%, 80.29% and 94.58% at 160 mg/kg, 320 mg/kg and 600 mg/kg, respectively [1].

Synonyms	RX-5902
Molecular Weight	441.46
Formula	C22H24FN5O4
CAS No.	888478-45-3

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 100 mg/mL (226.52 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Kost GC, et al. A Novel Anti-Cancer Agent, 1-(3,5-Dimethoxyphenyl)-4-[(6-Fluoro-2-Methoxyquinoxalin-3-yl)Aminocarbonyl] Piperazine (RX-5902), Interferes With β-Catenin Function Through Y593 Phospho-p68 RNA Helicase.J Cell Biochem. 2015 Aug;116(8):1595-601. 2. Capasso A, et al. First-in-Class Phosphorylated-p68 Inhibitor RX-5902 Inhibits β-Catenin Signaling and Demonstrates Antitumor Activity in Triple-Negative Breast Cancer.Nov;18(11):1916-1925.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Supinoxin 888478-45-3 DNA损伤和修复凋亡细胞周期 Apoptosis DNA/RNA Synthesis breast inhibit PANC-1 Inhibitor HCT116 UMRC2 PC-3 MKN-45 TNBC HepG2 RNA helicase HT29 RX-5902 cancer A549 Caki-1 RX5902 RX 5902 inhibitor

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