2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. KRASG12C IN-1

KRASG12C IN-1 is a potent and covalent KRASG12C inhibitor that traps KRASG12C in the GDP-bound state. KRASG12C IN-1 exhibits potent antitumor activity against KRAS-mutant non-small cell lung cancer.

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

KRASG12C IN-1 Chemical Structure

KRASG12C IN-1 Chemical Structure

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.

KRASG12C IN-1 Related Antibodies

Top Publications Citing Use of Products

View All Ras Isoform Specific Products:

View All Isoforms
K-Ras H-Ras Ras

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

KRASG12C IN-1 is a potent and covalent KRASG12C inhibitor that traps KRASG12C in the GDP-bound state. KRASG12C IN-1 exhibits potent antitumor activity against KRAS-mutant non-small cell lung cancer[1].

In Vitro

KRASG12C IN-1 (compound 20a) (72 h) shows potent and selective antiproliferative activities against KRASG12C NSCLC cells, with IC50s of 0.5 μM against NCI-H358 cells and 1.30 μM against NCI-H23 cells, with 7- to 21-fold selectivity over KRASG12S and KRASWT cells[1].
KRASG12C IN-1 (0.5-8.0 μM; 6 h) decreases the phosphorylation of ERK and AKT in KRASG12C-mutant NCIH358 cells[1].

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

KRASG12C IN-1 Related Antibodies

Western Blot Analysis[1]

Cell Line: NCI-H358 and NCI-H2228 cells
Concentration: 0.5, 1.0, 2.0, 4.0, 8.0 μM
Incubation Time: 6 hours
Result: Showed no impact on KRAS signaling in KRASWT NCI-H2228 cells.
The pERK level decreased 40%-90%, and the pAKT level was down-regulated by 30%-90% in NCI-H358 cells.
In Vivo

KRASG12C IN-1 (compound 20a) (10-15 mg/kg; i.p. every 2 d for 21 d) inhibited tumor growth in H358 xenografts by suppressing KRASG12C signalling[1].

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

Animal Model: Female BALB/c Nude mice were injected subcutaneously with NCI-H358 cells[1]
Dosage: 10, 15 mg/kg
Administration: I.p. every two days for 21 days
Result: Significantly inhibited tumor growth while the body weight of mice was not influenced.
Molecular Weight

410.27

Formula

C19H18Cl2FN3O2
SMILES

O=C(N1CCN(CC1)C(NC2=CC(C3=C(C=CC=C3)F)=C(C=C2)Cl)=O)CCl
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.

KRASG12C IN-1 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:

KRASG12C IN-1RasGDPantitumorKRAS-mutantnon-small cell lung cancerInhibitorinhibitorinhibit

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:
KRASG12C IN-1
Cat. No.:
HY-151999
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.