2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. EGFR-IN-82

EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFRL858R/T790M/C797S and EGFRDel19/T790M/C797S, respectively. EGFR-IN-82 has no significant effect on EGFRWT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research .

For research use only. We do not sell to patients.

EGFR-IN-82 Chemical Structure

EGFR-IN-82 Chemical Structure

CAS No. : 2568086-81-5

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

EGFR-IN-82 Related Antibodies

Top Publications Citing Use of Products

View All EGFR Isoform Specific Products:

View All Isoforms

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

EGFR-IN-82 (Cmpound 8a) is a potent and orally active EGFR inhibitor with IC50 values of 0.09 and 0.06 nM for EGFRL858R/T790M/C797S and EGFRDel19/T790M/C797S, respectively. EGFR-IN-82 has no significant effect on EGFRWT. EGFR-IN-82 has anti-proliferative activity and inhibits tumor formation in nude mice. EGFR-IN-82 can be used in non-small cell lung cancer research [1].

IC50 & Target

0.09 , 0.06 nM (EGFRL858R/T790M/C797S, EGFRDel19/T790M/C797S)
In Vitro

EGFR-IN-82 (compound 8a) (72 h) significantly inhibits the growth of Ba/F3-EGFRDel19/T790M/C797S cells with the IC50 value of 12.7 nM, but has no significant effect on the growth of A431 cells [1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

EGFR-IN-82 Related Antibodies
In Vivo

EGFR-IN-82 (Cmpound 8a) has better pharmacokinetic performance than Brigatinib (HY-12857) in vivo[1].
EGFR-IN-82 (15 - 30 mg/kg；Oral gavage (p.o.)；14 - 21 days) exhibits moderate inhibition on PC9-EGFR Del19/T790M/C797S xenograft mice model, while presents a very strong tumor growth inhibition effect on tumor with high expression of EGFRDel19/T790M/C797S[1].

Pharmacokinetic Analysis in Male Balb/C mice Model[1]

Route Dose (mg/kg) Cmax (ng/mL) AUC0-t (ng/mL*h) AUC0-∞(ng/mL*h) t1/2 (h) MRT (h)
p.0. 5 1574 15375 15632 3.5 6

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: PC9-EGFRDel19/T790M/C797S xenograft mice model
Ba/F3-EGFR Del19/T790M/C797S xenograft mice model [1]
Dosage: 15 or 30 mg/kg/day, 14-21 days
Administration: Oral gavage (p.o.)
Result: Exhibited moderate inhibition on tumor growth, with a tumor growth inhibition rate (TGI) of 21.60% at 15 mg/kg and 46.79% at 30 mg/kg in PC9-EGFR Del19/T790M/C797S xenograft mice model. Presented a very strong tumor growth inhibition effect with the TGI of 48.43% at low dose(15 mg/kg) and 82.60% at high dose(30 mg/kg) in xenograft mice model of Ba/F3-EGFR Del19/T790M/C797S.
Molecular Weight

694.60

Formula

C32H41BrN9O2P
CAS No.
SMILES

COC1=C(NC2=NC=C(Br)C(NC3=C(P(C)(C)=O)C(N=CC=N4)=C4C=C3)=N2)C=C(C)C(N5CCC(N6CC(N(C)C)C6)CC5)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

EGFR-IN-82 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

EGFR-IN-822568086-81-5EGFREpidermal growth factor receptorErbB-1HER1Ba/F3-EGFR（Del19/T790M/C797S）cellsA431 cellsPC9-EGFR（Del19/T790M/C797S）xenograft mice modelxenograft mice model of Ba/F3-EGFR（Del19/T790M/C797S）Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
EGFR-IN-82
Cat. No.:
HY-149401
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.