2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. KRAS G12C inhibitor 65

KRAS G12C inhibitor 65 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.

KRAS G12C inhibitor 65 Chemical Structure

KRAS G12C inhibitor 65 Chemical Structure

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KRAS G12C inhibitor 65 Related Antibodies

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Description

KRAS G12C inhibitor 65 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

KRAS G12C inhibitor 65 (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].
KRAS G12C inhibitor 65 (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.

KRAS G12C inhibitor 65 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

KRAS G12C inhibitor 65 (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
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KRAS G12C inhibitor 65 Related Classifications

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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:

KRAS G12C inhibitor 65RasGDPantitumorKRAS-mutantnon-small cell lung cancerInhibitorinhibitorinhibit

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