research use only

PD153035 EGFR inhibitor

Cat.No.S6546

PD153035 is a specific and potent inhibitor of the epidermal growth factor (EGF) receptor tyrosine kinase (Ki = 5.2 pM).
PD153035 EGFR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 360.21

Quality Control

Batch: S654601 DMSO]6 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.33%
99.33

Chemical Information, Storage & Stability

Molecular Weight 360.21 Formula

C16H14BrN3O2

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 153436-54-5 -- Storage of Stock Solutions

Synonyms N/A Smiles COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=CC=C3)Br)OC

Solubility

In vitro
Batch:

DMSO : 6 mg/mL ( (16.65 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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 [2]
(Cell-free assay)
5.2 pM(Ki)
In vitro

PD153035 inhibits EGF-dependent EGF receptor phosphorylation and suppresses the proliferation and cbonogenicity of a wide panel of EGF receptor-overexpressing human cancer cell lines. EGF receptor autophosphorylation in response to exogenous EGF can be completely inhibited at this compound concentrations of >75 nM in cells overexpressing the EGF receptor[1].

References

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