KRASG12C IN-21
KRASG12C IN-21 is an orally active KRAS G12C inhibitor with IC50 = 17 nM. KRASG12C IN-21 covalently modifies Cys12 of the active GTP-bound KRAS G12C, stabilizes the GTP-bound state, and disrupts KRAS-cRAF interaction, thereby inhibiting downstream ERK phosphorylation. KRASG12C IN-21 achieves durable complete tumor regression in pancreatic cancer xenograft models. KRASG12C IN-21 can be used for research on pancreatic cancer.
For research use only. We do not sell to patients.
- Formula: C36H33F5N6O3
- Molecular Weight:692.68
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
KRAS(G12C) 17 nM (IC50) |
In Vitro
KRASG12C IN-21 inhibits SOS-catalyzed KRASG12C nucleotide exchange with an IC50 of 76 nM[1].
KRASG12C IN-21 has an MDCK II apparent permeability of 11 × 10-6 cm/s[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
KRASG12C IN-21 (80 mg/kg; p.o.; once daily; 45 days) induces complete and durable tumor regression in the MIA PaCa-2 xenograft model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female; 6-7 weeks of age; were inoculated subcutaneously in the lower right flank with 5 × 106 MIA PaCa-2 cells in 0.1 mL of PBS mixed with Matrigel)[1]
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Dosage:80 mg/kg
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Administration:p.o.; once daily; 45 days
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Result:Achieved complete tumor regression within 15 days of dosing and maintained regression for an additional 30‑day period thereafter.
- Kinase activity and phosphorylation assays
- Western Blot
- Patient-Derived Xenograft (PDX)
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Protocol for Kinase activity and phosphorylation assays
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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Molecular Weight 692.68
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Formula C36H33F5N6O3
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SMILES
CC1=NC2=C(N(CC3)C)C(C4=CC=CN5C4=C3C=C5C(C6=CC(F)=C(NC(/C=C/CNC7(COC7)C)=O)C(F)=C6)=O)=C(C(F)(F)F)C=C2N1C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KRASG12C IN-21 Related Classifications
HY-190803 Related Classifications
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