2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Stem Cell/Wnt MAPK/ERK Pathway
  3. EGFR ERK
  4. STX-721

STX-721 is an orally active, irreversible, covalent EGFR exon 20 insertion (ex20ins) inhibitor that selectively targets ex20ins-mutant dynamic protein states. STX-721 potently inhibits the kinase activity of EGFR ex20ins mutants (NPG, ASV, SVD). STX-721 inhibits phosphorylation of EGFR (pEGFR Y1068) and downstream ERK (pERK Thr202/Tyr204), and suppresses proliferation of ex20ins-mutant Ba/F3 cells and human NSCLC cell lines (NCI-H2073 ASV KI, CUTO-14 ASV). STX-721 induces tumor regression in EGFR ex20ins-mutant PDX/CDX models. STX-721 can be used for the study of non-small cell lung cancer (NSCLC) harboring EGFR or HER2 ex20ins mutations.

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

STX-721

STX-721 Chemical Structure

CAS No. : 2765525-82-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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

Customer Review

Based on 1 publication(s) in Google Scholar

STX-721 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE STX-721

View All EGFR Isoform Specific Products:

View All Isoforms
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

View All ERK Isoform Specific Products:

View All Isoforms
ERK ERK1 ERK2 ERK5 ERK8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

STX-721 is an orally active, irreversible, covalent EGFR exon 20 insertion (ex20ins) inhibitor that selectively targets ex20ins-mutant dynamic protein states. STX-721 potently inhibits the kinase activity of EGFR ex20ins mutants (NPG, ASV, SVD). STX-721 inhibits phosphorylation of EGFR (pEGFR Y1068) and downstream ERK (pERK Thr202/Tyr204), and suppresses proliferation of ex20ins-mutant Ba/F3 cells and human NSCLC cell lines (NCI-H2073 ASV KI, CUTO-14 ASV). STX-721 induces tumor regression in EGFR ex20ins-mutant PDX/CDX models. STX-721 can be used for the study of non-small cell lung cancer (NSCLC) harboring EGFR or HER2 ex20ins mutations[1][2].

In Vitro

STX-721 (10-1000 nM, 2 h) inhibits phosphorylation of EGFR (pEGFR Y1068) and ERK (pERK Thr202/Tyr204) in patient-derived EGFR exon 20 insertion-mutant cell lines (MGH10080-1 SVD, MGH10022-1.19 GF) with higher potency than in EGFR WT NCI-H2073 cells[1].
STX-721 (72 h) shows antiproliferative activity in CRISPR/Cas9-edited NCI-H2073 human cancer cell lines, with IC50 values of 10.1 nM for NCI-H2073 EGFR V769_D770 insASV knock-in (KI) cells and 6.1 nM for NCI-H2073 EGFR D770_N771 insSVD KI cells[2].

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

STX-721 Related Antibodies
In Vivo

STX-721 (12.5-100 mg/kg, p.o., once daily, 20-42 days) demonstrates excellent anti-tumor efficacy in EGFR ex20ins-mutant PDX/CDX models.[1].

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

Animal Model: Tumor tissues with NSCLC harboring EGFR NPH mutation, EGFR ASV mutation, EGFR SVD mutation, HER2 YVMA mutation and NCI-H2073 EGFR_exon20_SVD_ins cells (1×107 cells/mouse in appropriate medium) were subcutaneously implanted into the flanks of 6-8-week-old female BALB/c nude mice[1]
Dosage: 12.5, 25, 50, 100 mg/kg
Administration: p.o. once daily for 20, 26, 38 or 42 days
Result: Achieved tumor growth inhibition.
Reduced phosphorylation of EGFR (pEGFR) and ERK (pERK).
Clinical Trial
Molecular Weight

587.11

Formula

C32H35ClN6O3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N1CCC[C@]1(C)C#CC2=C(C=CN=C2)C3=C(C4=C(N3)CCNC4=O)NC5=CC=CC(Cl)=C5OC)/C=C/CN(C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (170.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7033 mL 8.5163 mL 17.0326 mL
5 mM 0.3407 mL 1.7033 mL 3.4065 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.25%

SDS (251 KB)

COA (265 KB) HNMR (169 KB) RP-HPLC (255 KB) MS (74 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7033 mL 8.5163 mL 17.0326 mL 42.5815 mL
5 mM 0.3407 mL 1.7033 mL 3.4065 mL 8.5163 mL
10 mM 0.1703 mL 0.8516 mL 1.7033 mL 4.2581 mL
15 mM 0.1136 mL 0.5678 mL 1.1355 mL 2.8388 mL
20 mM 0.0852 mL 0.4258 mL 0.8516 mL 2.1291 mL
25 mM 0.0681 mL 0.3407 mL 0.6813 mL 1.7033 mL
30 mM 0.0568 mL 0.2839 mL 0.5678 mL 1.4194 mL
40 mM 0.0426 mL 0.2129 mL 0.4258 mL 1.0645 mL
50 mM 0.0341 mL 0.1703 mL 0.3407 mL 0.8516 mL
60 mM 0.0284 mL 0.1419 mL 0.2839 mL 0.7097 mL
80 mM 0.0213 mL 0.1065 mL 0.2129 mL 0.5323 mL
100 mM 0.0170 mL 0.0852 mL 0.1703 mL 0.4258 mL
  • 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.

STX-721 Related Classifications

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:

STX-7212765525-82-2STX721STX 721EGFRERKEpidermal growth factor receptorErbB-1HER1Extracellular signal regulated kinasesnon-small cell lung cancerexon 20NCI-H2073 ASV KICUTO-14 ASVInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
STX-721
Cat. No.:
HY-157229
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

SAFETY DATA SHEET (SDS)

English - EN (251 KB) Français - FR (251 KB) Deutsch - DE (251 KB) Norwegian - NO (251 KB) Español - ES (251 KB) Swedish - SV (251 KB) Italian - IT (251 KB) Portuguese - PT (251 KB)

Request for HNMR Report

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