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Art. -Nr.: 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.

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CAS. Nr.: 3023465-61-1
Formel: C₃₈H₃₃F₄N₇O₂S
Molecular Weight:727.77

Speicherung:

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

KRAS G12C-IN-76 Chemical Structure

CAS. Nr.: 3023465-61-1

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Use of MCE Products

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

KRas G12C

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Alle ERK Isoform-spezifische Produkte anzeigen :

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. Nr. 3023465-61-1
Molecular Weight 727.77
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[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]

Calculators

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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.

Bioz

Keywords

MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise

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KRAS G12C-IN-76

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