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Daphnetin EGFR inhibitor

Name: Daphnetin
Brand: Selleck Chemicals
SKU: S2554
Rating: 5 (4 reviews)

Cat.No.S2554

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.

Chemical Structure

Molecular Weight: 178.14

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Quality Control

Batch: Purity: 99.55%

99.55

Related Targets	VEGFR JAK PDGFR FGFR Src HIF FLT FLT3 HER2 Bcr-Abl
Other EGFR Inhibitors	Lazertinib (YH25448) Icotinib Hydrochloride Sunvozertinib AG-490 AG-1478 Canertinib (CI-1033) WZ4002 Rociletinib (CO-1686) Poziotinib (NOV120101, HM781-36B) Genistein

Chemical Information, Storage & Stability

Molecular Weight	178.14	Formula	C₉H₆O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	486-35-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	C1=CC(=C(C2=C1C=CC(=O)O2)O)O

Solubility

In vitro
Batch:

DMSO : 36 mg/mL (202.08 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	EGFR 7.67 μM PKA 9.33 μM PKC 25.01 μM
In vitro	Daphnetin strongly inhibits not only EGF receptor-catalysed tyrosine phosphorylation of exogenous substrate but also PKA and PKC activities. This compound inhibits MCF-7 oestrogen-responsive human carcinoma cell line at 24-hour exposure with IC50 of 73 μM. It reduces the level of cyclin D1 even at 50 μM. This chemical protects the cortical neurones against dexamethasone-induced reduction of cell viability in a dose-dependent manner. It inhibits the activities of endogenous or recombinant TaPRK in a specific and dose-dependent manner. This compound causes a 50% inhibition (IC50) of 3H-hypoxanthine incorporation by Plasmodium falciparum at concentrations between 25 μM and 40 μM. It inhibits the mitogenic signalling of ERK1/ERK2.
Kinase Assay	Assay of protein kinase C (PKC) and cAMP-dependent protein kinase (PKA) activities.
Kinase Assay	PKC and PKA activities are detected. Briefly, 5 mL of PKC or PKA is mixed with 5 mL of lipid preparation containing 100 mM phorbol 12-myristate 13-acetate, 2.8 mg/mL phosphatidyl serine, and Triton X-100 mixed micelles for PKC assay or 5 mL of 40 mM cAMP in 50 mM Tris-HCl, pH 7.5, for PKA assay, and 5 mL of daphnetin. The reaction is started by adding 10 mL of PKC substrate solution containing 250 mM acetylated myelin basic protein, 100 mM ATP, 5 mM CaCl₂, 10 mM MgCl₂, 20 mM Tris-HCl, pH 7.5, or 10 mL of PKA substrate solution containing 200 mM Kemptide, 400 mM ATP, 40 mM MgCl₂, 1 mg/mL BSA, 50 mM Tris-HCl, pH 7.5, and 20-25 mCi/mL [g-³²P] ATP. After incubation at 25 °C for 5 minutes, 20 mL of each mixture is spotted on a piece of phosphocellulose disc which is immediately put into 1% H₃PO₄. After free [g-³²P] ATP on the discs is removed, the peptide-incorporated ³²P on the discs is counted in a scintillation counter.
In vivo	Daphnetin at 140 mg/kg significantly decreases uterine weights by 39.5%. Two and 8 mg/kg administration of this compound could improve the performance of stress mice in Morris water maze tests and forced swimming tests. This chemical significantly prolongs survival of P. yoelli-infected mice.
References	[1] https://pubmed.ncbi.nlm.nih.gov/10403826/ [2] https://pubmed.ncbi.nlm.nih.gov/21741969/ [3] https://pubmed.ncbi.nlm.nih.gov/22715971/ [4] https://pubmed.ncbi.nlm.nih.gov/22827600/ [5] https://pubmed.ncbi.nlm.nih.gov/1311154/ [6] https://pubmed.ncbi.nlm.nih.gov/15081877/

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