KD36
KD36 is a selective KRAS-G12C inhibitor with an IC50 value of 0.92 μM. KD36 can inhibit the phosphorylation of ERK and AKT, induce the accumulation of reactive oxygen species (ROS), reduce mitochondrial membrane potential, thereby leading to apoptosis of KRAS-G12C mutant cells. KD36 can be used in the research of non-small cell lung cancer (NSCLC).
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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: C29H32N6O3
- 分子量:512.60
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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
- プロトコル
- 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
製品説明
IC50 & Target
[1]|
KRas G12C 0.92 μM (IC50) |
体外実験
KD36 (72 h) demonstrates potent antiproliferative activity in KRAS-G12C mutant NCI-H23, NCI-H358 cells with IC50 values of 0.42 and 0.65 μM[1].
KD36 (0.5-4.0 μM; 24-48 h) induces mitochondrial-dependent apoptosis by increasing intracellular ROS levels and reducing mitochondrial membrane potential in NCI-H23 cells[1].
KD36 (0.5-8.0 μM; 8 h) significantly inhibits the phosphorylation of KRAS downstream effectors ERK and AKT (p-ERK, p-AKT) in NCI-H23 cells, with no obvious inhibitory effect on KRAS wild-type (NCI-H2228) cells[1].
KD36 (0.1-1.0 μM, 14 days) dose-dependently suppresses colony formation of NCI-H23 and NCI-H358 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–H23, NCI–H2228
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Concentration:0.5 μM, 1.0 μM, 2.0 μM, 4.0 μM, 8.0 μM
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Incubation Time:8 h
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Result:Significantly reduced the phosphorylation of ERK and AKT in NCI-H23 cells, with a 80% reduction in pERK and 70% reduction in pAKT at 4.0 μM.
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Cell Line:NCI–H23 cells
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Concentration:0.5 μM, 1.0 μM, 2.0 μM, 4.0 μM
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Incubation Time:24 h, 48 h
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Result:Increased the levels of JC-1 monmers and DCFH-DA fluorescence intensity.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NCI-H358 xenograft mice models (male, 6 weeks)[1]
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Dosage:30 mg/kg
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Administration:Intraperitoneally injection
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Result:Reduced tumor weight and volume.
Showed tumor growth inhibition (TGI) rate of 54.6%.
Caused no obvious pathological damage to major organs (heart, liver, spleen, lung, kidney), and exhibited no systemic toxicity.
- Kinase activity and phosphorylation assays
- Western Blot
- Mitochondrial membrane-potential fluorescent assay
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- ROS/oxidative-stress fluorescent staining
- Fluorescent plasma-membrane potential dye assay
- Mitochondrial membrane-potential and mitochondrial mass staining
- Apoptosis Solutions
- Protocol for Kinase activity and phosphorylation assays
化学情報
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分子量 512.60
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分子式 C29H32N6O3
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SMILES
O=C(C=C)N(CC1)CCN1C2=NC(OC[C@@H]3CCCN3C)=NC(C4=C(C=CC=C5)C5=CC(OC)=C4)=C2C#N
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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
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
KD36 関連分類
HY-179702 関連分類
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