ASP6918
ASP6918 is a potent and orally active KRAS G12C inhibitor with an IC50 value of 0.028 µM. ASP6918 inhibits cell growth. ASP6918 shows antitumor activity.
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- Formule: C36H43N7O3
- Masse moléculaire:621.77
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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 0.028 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| NCI-H1373 | IC50 |
0.006 μM
Compound: 29a; ASP6918
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Cytotoxicity against KRAS G12C mutant positive human NCI-H1373 cells assessed as inhibition of cell growth incubated for 6 days by Celltiter-Glo 2.0 assay
Cytotoxicity against KRAS G12C mutant positive human NCI-H1373 cells assessed as inhibition of cell growth incubated for 6 days by Celltiter-Glo 2.0 assay
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[PMID: 38176113] |
| NCI-H1373 | IC50 |
0.008 μM
Compound: 28b
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Cytotoxicity against KRAS G12C mutant positive human NCI-H1373 cells assessed as inhibition of cell growth incubated for 6 days by Celltiter-Glo 2.0 assay
Cytotoxicity against KRAS G12C mutant positive human NCI-H1373 cells assessed as inhibition of cell growth incubated for 6 days by Celltiter-Glo 2.0 assay
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[PMID: 38176113] |
ASP6918 (compound 29a) (6 days) inhibits cell growth with an IC50 value of 0.0061 µM for NCI-H1373 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H1373 cells
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Concentration:
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Incubation Time:6 days
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Result:Inhibited cell growth with an IC50 value of 0.0061 µM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Four-week-old male nude mice (NCI-H1373 xenograft mouse model)[1]
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Dosage:10, 20, 40, 60 mg/kg
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Administration:Oral, daily for 13 days
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Result:Inhibited of tumor growth with tumor growth inhibition (TGI) rate of 27%, 68%, 49%, 73% at 10, 20, 40, 60 mg/kg.
Chemical Information
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Masse moléculaire 621.77
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Formule C36H43N7O3
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SMILES
C=CC1=CC2=C(N=C(OC3CCN(C)CC3)N=C2N4CCC5(CN(C(C=C)=O)C5)CC4)C(OCC)=[C@]1[C@]6=C(C)C=CC7=C6C=NN7
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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
[1]. Imaizumi T, et al. Discovery of ASP6918, a KRAS G12C inhibitor: Synthesis and structure-activity relationships of 1-{2,7-diazaspiro[3.5]non-2-yl}prop-2-en-1-one derivatives as covalent inhibitors with good potency and oral activity for the treatment of solid tumors. Bioorg Med Chem. 2024 Jan 15;98:117581. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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