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Cat. No.: HY-181913

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KRAS G12C-IN-76

KRAS G12C-IN-76 (Compound 39) is an orally active KRAS^G12C inhibitor. KRAS G12C-IN-76 inhibits the phosphorylation of ERK. KRAS G12C-IN-76 exhibits anticancer activity against pancreatic cancer.

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

CAS No.: 3023465-61-1
Formula: C₃₈H₃₃F₄N₇O₂S
Molecular Weight:727.77

Storage:

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

KRAS G12C-IN-76 Chemical Structure

CAS No.: 3023465-61-1

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Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

KRas G12C

All Ras Isoforms :

All ERK Isoforms :

In Vitro

KRAS G12C-IN-76 (2 h) potently inhibits ERK phosphorylation in MIA PaCa-2 KRAS^G12C mutant cells, with a pIC₅₀ of 9.64^[1].
KRAS G12C-IN-76 (5 days) potently inhibits the proliferation of MIA PaCa-2 KRAS^G12C mutant cells, with a pIC₅₀ of 8.96^[1].

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

Parmacokinetics

Species	Dose	Route	CL	V_ss	T_1/2	AUC_0-24	F
Mice^[1]	0.5 mg/kg	i.v.	2.0 mL/min/kg	0.2 L/kg	1.2 h	5600 nM·h	/
Mice^[1]	30 mg/kg	p.o.	/	/	/	38500 nM·h	/
Dog^[1]	1 mg/kg	i.v.	2.2 mL/min/kg	0.6 L/kg	4.4 h	11000 nM·h	/
Dog^[1]	2 mg/kg	p.o.	/	/	/	6000 nM·h	27 %

In Vivo

KRAS G12C-IN-76 (50-150 mg/kg; p.o.; once daily; for 17 consecutive days) exhibits antitumor activity in athymic nude mice bearing MIA PaCa-2 KRAS^G12C xenografts^[1].

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

Animal Model:

Crl:NU(NCr)-Foxn1nu-homozygous nude (female, MIA PaCa-2 KRASG12C pancreatic cancer xenograft model)^[1]
Dosage:

50 mg/kg; 150 mg/kg
Administration:

p.o.; daily; 17 days
Result:

Induced 21% tumor growth regression at 50 mg/kg.
Induced 89% tumor growth regression, with complete tumor responses observed in 3 of 8 treated mice at 150 mg/kg.

Chemical Information

CAS No. 3023465-61-1
Molecular Weight 727.77
Formula C₃₈H₃₃F₄N₇O₂S
SMILES

F[C@@H]1C[C@@](CCC2)(COC3=NC4=C(C(N5[C@H](CN(CC5)C(/C(F)=C/C6=NC=CS6)=O)C)=N3)C=NC(C7=C8C(C#C[H])=C(C=CC8=CC=C7)F)=C4F)N2C1
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. Optimization of α-Fluoro, β-Heteroaryl Acrylamide Warheads for KRAS^G12C Active-State Inhibition. J Med Chem. 2026;69(5):5935-5943. [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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100 mg

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

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KRAS G12C-IN-76

All Ras Isoforms

All ERK Isoforms