research use only

EGFR Inhibitor EGFR inhibitor

Name: EGFR Inhibitor
Brand: Selleck Chemicals
SKU: S0360
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S0360

EGFR inhibitor, a cell permeable, 4,6-disubstituted pyrimidine compound, is a highly selevtive inhibitor of EGFR kinase with IC50 of 21 nM. EGFR inhibitor directly depolymerizes microtubules and is used as a chemical probe to investigate both the EGFR pathway and microtubule dynamics.

Chemical Structure

Molecular Weight: 413.40

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S036001 DMSO]83 mg/mL]false]Ethanol]2 mg/mL]false]Water]˂1 mg/mL]false Purity: 99.56%

99.56

Related Targets	VEGFR PDGFR FGFR c-Met Src FLT3 HER2 c-Kit Bcr-Abl MEK BTK IGF-1R ALK Trk receptor Syk Axl CSF-1R c-RET FAK Mertk Tie-2 DYRK Tyro3 Ephrin receptor ROS1 Pyk2 RON DDR ACK Fer kinase
Related Products	AG-490 AG-1478 Canertinib (CI-1033) Rociletinib (CO-1686) WZ4002 Genistein Poziotinib (HM781-36B) PD153035 PD153035 HCl Allitinib tosylate AEE788 (NVP-AEE788) Pelitinib (EKB-569) Canertinib dihydrochloride Varlitinib Icotinib (BPI-2009H) Nazartinib (EGF816) NSC228155 PD168393 Olmutinib (BI 1482694) Zorifertinib (AZD3759) AZ5104 Lazertinib CL-387785 (EKI-785) TAK-285 Daphnetin Pyrotinib dimaleate Alflutinib (Furmonertinib) mesylate Chrysophanic Acid Norcantharidin WZ8040

Chemical Information, Storage & Stability

Molecular Weight	413.40	Formula	C₂₁H₁₈F₃N₅O	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	879127-07-8	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	EGFR-IN-12			Smiles	C1CC1C(=O)NC2=CC=CC(=C2)NC3=NC=NC(=C3)NC4=CC=CC(=C4)C(F)(F)F

Solubility

In vitro
Batch:

DMSO : 83 mg/mL (200.77 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 2 mg/mL

Water : ˂1 mg/mL

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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.15mg/ml (10.04mM)	Taking the 1 mL working solution as an example, add 50 μL of 83 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.59mg/ml (1.43mM)	Taking the 1 mL working solution as an example, add 50 μL of 11.8 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

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	Microtubules ^[1] EGFR ^[1] (Cell-free assay) 21 nM
References	[1] https://pubmed.ncbi.nlm.nih.gov/16478150/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06118047	Recruiting	Metastatic Colorectal Cancer\|Cetuximab\|Skin Toxicity	Sun Yat-sen University	August 1 2023	Phase 2
NCT03051880	Unknown status	Drug-Related Side Effects and Adverse Reactions\|Epidermal Growth Factor	The Catholic University of Korea	November 2016	Not Applicable
NCT03047863	Unknown status	Drug-Related Side Effects and Adverse Reactions\|Epidermal Growth Factor	The Catholic University of Korea	November 2016	Not Applicable
NCT02588261	Terminated	Non-small Cell Lung Cancer (NSCLC)	Astellas Pharma Global Development Inc.\|Astellas Pharma Inc	February 11 2016	Phase 3

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):