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Cat. No.: HY-181965

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KRAS G12C-IN-78

KRAS G12C-IN-78 is a selective SWII-binding KRASG12C dual inhibitor targeting both inactive and active states. KRAS G12C-IN-78 rapidly inhibits ERK1/2 phosphorylation, induces covalent adduct formation with endogenous KRASG12C, suppresses MAPK pathway gene expression, and inhibits cellular proliferation in KRASG12C mutant cells. KRAS G12C-IN-78 can be used for the research of KRASG12C mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer.

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

CAS No.: 3023465-20-2
Formula: C₃₇H₃₁F₄N₇O₃S
Molecular Weight:729.75

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

KRAS G12C-IN-78 Chemical Structure

CAS No.: 3023465-20-2

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
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Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

KRas G12C

ERK1

ERK2

All Ras Isoforms :

All ERK Isoforms :

All p38 MAPK Isoforms :

In Vitro

KRAS G12C-IN-78 (Compound 6) (2 h) potently inhibits ERK1/2 phosphorylation in MIA PaCa-2 KRAS^G12C mutant cells with an IC₅₀ of 0.1 nM^[1].
KRAS G12C-IN-78 (5 days) potently inhibits proliferation of MIA PaCa-2 KRAS^G12C mutant cells with an IC₅₀ of 0.1 nM after 5 days of treatment^[1].
KRAS G12C-IN-78 shows IC₅₀ values <10 nM for G12C mutant cells and IC₅₀ values >1000 nM for non-G12C mutant cells^[1].

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

Chemical Information

CAS No. 3023465-20-2
Molecular Weight 729.75
Formula C₃₇H₃₁F₄N₇O₃S
SMILES

[H]C#CC1=C(C=CC2=CC(O)=CC(C3=C(C4=C(C(N5CCN(CC5)C(/C(F)=C/C6=NC=CS6)=O)=NC(OC[C@@]78CCCN7C[C@@H](C8)F)=N4)C=N3)F)=C21)F
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

Handling Instructions (2659 KB)

References

[1]. Condakes ML, et al. Covalent inhibitor design confers activity against both GDP- and GTP-bound forms of KRAS G12C. Nat Commun. 2026;17(1):2233. Published 2026 Jan 31. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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KRAS G12C-IN-78

All Ras Isoforms

All ERK Isoforms

All p38 MAPK Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

KRAS G12C-IN-78 Related Classifications

HY-181965 Related Classifications