KRASG12C IN-18
KRASG12C IN-18 is an orally active covalent KRASG12C inhibitor that achieves complete covalent engagement of KRASG12C in both GDP- and GMPPNP-bound states and displays strong antiproliferative activity against KRASG12C and resistance-associated variants, including KRASG12C/R68S, with low-nanomolar IC50 values. KRASG12C IN-18 exhibits marked in vivo efficacy in KRASG12C-driven solid tumor and KRASG12C/R68S xenograft models and can be used for colorectal cancer research.
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- CAS No.: 2966924-24-1
- Formule: C37H32F4N6O2
- Masse moléculaire:668.68
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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KRAS(G12C) |
Following 72-144 h incubation, KRASG12C IN-18 (compound 20) potently inhibited KRASG12C-mutant Ba/F3 cells and multiple secondary resistance variants, including H95Q (IC50 = 7.5 nM), Y96D (IC50 = 2.8 nM), R68S (IC50 = 5.4 nM) and Q99L (IC50 = 8.2 nM), showing low-nanomolar inhibitory activity across these models[1].
KRASG12C IN-18 achieves 100% covalent modification of KRASG12C in both GDP-bound and GMPPNP-bound states within minutes, indicating rapid and efficient target engagement[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
KRASG12C IN-18 (Ba/F3 KRASG12C/R68S xenograft; oral administration, 30 mg/kg, once daily, 21 days) also shows strong antitumor activity, producing 79.2% tumor regression and exhibiting good tolerability[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; 28 days
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Result:Achieved 103% tumor growth inhibition and induced complete tumor stasis without body-weight loss.
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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; 21 days
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Result:Produced 79.2% tumor regression and demonstrated good tolerability.
Chemical Information
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CAS No. 2966924-24-1
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Masse moléculaire 668.68
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Formule C37H32F4N6O2
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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)=C(F)C=CC5=CC=C4)=C(F)C3=NC(OCC67CCCN6CCC7)=N2)C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KRASG12C IN-18 Related Classifications
HY-179404 Related Classifications
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