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Daphnetin

SKU: orb1224968

Description

Daphnetin, a natural coumarin derivative, is a protein kinase inhibitor, inhibits EGFR, PKA and PKC with IC50 of 7.67 μM, 9.33 μM and 25.01 μM, respectively, also known to exhibit anti-inflammatory and anti-oxidant activities.(In Vitro):Daphnetin (7,8-dihydroxycoumarin) (0-40 μg/mL; 24-48 hours) inhibits the proliferation of ovarian cancer cells.Daphnetin (7,8-dihydroxycoumarin) (0-40 μg/mL; 24 hours; A2780 cells) induces apoptosis and increases ROS production in a dose-dependent manner.Daphnetin (7,8-dihydroxycoumarin) (0-40 μg/mL; 24 hours; A2780 cells) induces autophagy through modulation of the AMPK/Akt/mTOR pathway.Daphnetin (7,8-dihydroxycoumarin) (1-10 μM; plasmodium falciparum) exhibits schizontocidal activity in a dose-dependent manner.\n(In Vivo):Daphnetin (7,8-dihydroxycoumarin) (30 mg/kg; i.p.; daily; for 12 days; BALB/c nude mice) has antitumour activities in a xenograft animal model.Daphnetin (7,8-dihydroxycoumarin) (2.5-10 mg/kg; i.p.; daily; for three days; C57BL/6 mice) inhibits cisplatin-induced inflammation, decreases TNF-α, IL-1β, ROS and MDA production in a dose-dependent manner in kidney tissues. Daphnetin inhibits cisplatin-induced NF-κB activation and up-regulated Nrf2 and HO-1.Daphnetin (7,8-dihydroxycoumarin) (10-100 mg/kg; i.g. and i.p.; every four days, for 30 days; male Kunming outbred strain mice) displays certain schizontocidal activity in vivo.

Images & Validation

Key Properties

CAS Number486-35-1
MW178.14
Purity>98% (HPLC)
FormulaC9H6O4
SMILESO=C1C=CC2=CC=C(O)C(O)=C2O1
TargetEGFR
SolubilityDMSO: 35 mg/mL (196.47 mM)

Bioactivity

In Vivo
Daphnetin (7, 8-dihydroxycoumarin) (30 mg/kg; i.p.; daily; for 12 days; BALB/c nude mice) has antitumour activities in a xenograft Animal model. Daphnetin (7, 8-dihydroxycoumarin) (2.5-10 mg/kg; i.p.; daily; for three days; C57BL/6 mice) inhibits cisplatin-induced inflammation, decreases TNF-α, IL-1β, ROS and MDA production in a dose-dependent manner in kidney tissues. Daphnetin inhibits cisplatin-induced NF-κB activation and up-regulated Nrf2 and HO-1.Daphnetin (7, 8-dihydroxycoumarin) (10-100 mg/kg; i. g. and i.p.; every four days, for 30 days; male Kunming outbred strain mice) displays certain schizontocidal activity In vivo. Animal model: BALB/c nude mice. Dosage: 30 mg/kg. Administration: Intraperitoneal injection; Daily; for 12 days. Result: Decreased tumor volume and weight in a xenograft Animal model. Animal model: Male Kunming outbred strain mice. Dosage: 10, 50 or 100 mg/kg. Administration: Oral gavage and intraperitoneal injection; every four days, for 30 days. Result: Reduced the number of parasites in mice.
In Vitro
Daphnetin (7, 8-dihydroxycoumarin) (0-40 μg/mL; 24-48 hours) inhibits the proliferation of ovarian cancer cells. Daphnetin (7, 8-dihydroxycoumarin) (0-40 μg/mL; 24 hours; A2780 cells) induces apoptosis and increases ROS production in a dose-dependent manner. Daphnetin (7, 8-dihydroxycoumarin) (0-40 μg/mL; 24 hours; A2780 cells) induces autophagy through modulation of the AMPK/Akt/mTOR pathway. Daphnetin (7, 8-dihydroxycoumarin) (1-10 μM; plasmodium falciparum) exhibits schizontocidal activity in a dose-dependent manner. Cell Viability Assay Cell line: IOSE8C, A2780, SKOV3 and OVCAR8 cells. Concentration: 0, 5, 10, 20 and 40 μg/mL. Incubation time: 24 h and 48 hours. Result: Inhibited growth in ovarian cancer cells but not in normal cells. Apoptosis Analysis Cell line: A2780 and SKOV3 cells. Concentration: 0, 10, 20 and 40 μg/mL. Incubation time: 24 hours. Result: Increased apoptosis in a dose-dependent manner in A2780 and SKOV3 cells. Western blot analysis. Cell line: A2780 and SKOV3 cells. Concentration: 0, 10, 20 and 40 μg/mL. Incubation time: 24 hours. Result: Increased proapoptotic protein (Caspase 3, Bax, and PARP) expression but decreased antiapoptotic protein (Bcl2) expression. Western blot analysis. Cell line: A2780 cells. Concentration: 0, 10, 20 and 40 μg/mL. Incubation time: 24 hours. Result: Increased LC3 II and p62 expression in a dose-dependent manner and reduced the expression levels of p-Akt, p-mTOR, but increased the expression level of p-AMPK.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

7,8-Dihydroxycoumarin | NSC 633563

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Daphnetin (orb1224968)

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