KRASG12C IN-17
KRASG12C IN-17 is an orally active covalent KRASG12C inhibitor, showing strong inhibitory activity in KRASG12C-mutant cancer cells (NCI-H23 IC50 = 0.7 nM; NCI-H358 IC50 = 0.5 nM). KRASG12C IN-17 covalently and irreversibly binds to KRASG12C with > 96% modification efficiency in both GDP-bound and GMPPNP-bound conformations. KRASG12C IN-17 can be used for studies of KRAS-driven cancers, including colorectal cancer.
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- CAS No.: 2966924-23-0
- 화학식: C37H33F3N6O2
- 분자량:650.69
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보관:
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
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
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KRas G12C |
In Vitro
KRASG12C IN-17 (compound 19) potently inhibits KRASG12C-mutant NCI-H23 and NCI-H358 cells with IC50 values of 0.7 nM and 0.5 nM, respectively , following 72-144 hours of incubation[1].
KRASG12C IN-17 covalently modifies KRASG12C in both GDP- and GMPPNP-bound states with >96% conjugation efficiency within 15 minutes[1].
KRASG12C IN-17 inhibits multiple resistance-associated KRASG12C variants, including R68S, H95Q, Y96C and Q99L, in Ba/F3 cells[1].
KRASG12C IN-17 exhibits antiproliferative activity against selected KRASG12C secondary-mutation cancer cell lines, retaining strong potency particularly against Y96C and Q99L variants[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H23 (KRASG12C), NCI-H358 (KRASG12C)
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Concentration:0.7 nM (NCI-H23), 0.5 nM (NCI-H358)
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Incubation Time:72 h
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Result:Significantly inhibited proliferation of KRASG12C-mutant NCI-H23 and NCI-H358 cells.
In Vivo
KRASG12C IN-17 (30 mg/kg, oral gavage, QD for 21 days) significantly reduces tumor volume in Ba/F3 KRASG12C/R68S xenograft models, achieving 65.9% tumor reduction[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SW837 human rectal cancer xenograft (KRASG12C) female NOD SCID mice (6–7 weeks old, 20.5–23.7 g)
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Dosage:30 mg/kg
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Administration:Oral gavage (p.o.); once daily (QD); 28 days
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Result:Achieved 103% tumor growth inhibition and induced near-complete tumor stasis without significant body-weight loss in SW837 KRASG12C xenograft models.
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Animal Model:Ba/F3 KRASG12C/R68S xenograft model female NOD SCID mice (6-8 weeks old, 18.6-23.3 g)
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Dosage:30 mg/kg
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Administration:Oral gavage (p.o.); once daily (QD); 21 days
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Result:Reduced tumor volume by 65.9% and demonstrated good tolerability in Ba/F3 KRASG12C/R68S xenograft models.
Chemical Information
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CAS No. 2966924-23-0
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분자량 650.69
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화학식 C37H33F3N6O2
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SMILES
N#CC[C@@H]1N(C(C(F)=C)=O)CCN(C2=C3C=C(F)C(C4=C5C(C#C)=CC=CC5=CC=C4)=C(F)C3=NC(OCC67CCCN6CCC7)=N2)C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KRASG12C IN-17 Related Classifications
HY-179403 Related Classifications
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