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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C36H43N7O3
- 分子量:621.77
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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KRas G12C 0.028 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 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.
化学情報
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分子量 621.77
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
ASP6918 関連分類
HY-162249 関連分類
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