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Lidocaine hydrochloride EGFR inhibitor

Cat.No.S4667

Lidocaine hydrochloride (Lidothesin, Lignocaine, Xyloneural) is an inhibitor of epidermal growth factor receptor (EGFR) and has antiproliferative effect on human tongue cancer cells. This compound is a local anesthetic and cardiac depressant used as an antiarrhythmia agent.
Lidocaine hydrochloride EGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 270.8

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Quality Control

Batch: S466701 DMSO]54 mg/mL]false]Water]54 mg/mL]false]Ethanol]54 mg/mL]false Purity: 99.86%
99.86

Solubility

In vitro
Batch:

DMSO : 54 mg/mL (199.4 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 54 mg/mL

Ethanol : 54 mg/mL

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In vivo
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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.

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Chemical Information, Storage & Stability

Molecular Weight 270.8 Formula

C14H22N2O.HCl

 Storage (From the date of receipt)
CAS No. 73-78-9 Download SDF Storage of Stock Solutions

Synonyms Lidocaine HCL, Lidothesin, Lignocaine hydrochloride, Xyloneural Smiles CCN(CC)CC(=O)NC1=C(C=CC=C1C)C.Cl

Mechanism of Action

Targets/IC50/Ki
EGFR
In vitro
Lidocaine hydrochloride above 1.25 g/l reduces cellular viability and triggers apoptosis in HCE cells in a time- and dose-dependent manner. This compound-induced apoptosis is caspase dependent and may be related to mitochondrial pathway. This chemical, at the level of tissue concentration under topical or local administration, also has a direct inhibitory effect on the activity of epidermal growth factor receptor (EGFR), which is a potential target for antiproliferation in cancer cells.
In vivo
Intravenous administration of the local anaesthetic lidocaine has been used to treat neuropathic pain for several decades and significantly improves postoperative pain associated with complex spine surgery and cholecystectomy. It is well established that this compound blocks impulses in peripheral nerves by inhibiting voltage-gated sodium (Na+) channels. Intravenous lidocaine has an analgesic effect on mechanical noxious response, decreases the spinal noxious response induced by peripheral pinch stimuli and the frequency of spontaneous excitatory postsynaptic currents(EPSCs) without changing their amplitude. It has no effect on spontaneous inhibitory postsynaptic currents and produces an outward current in SG neurons.
References

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