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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- 화학식: C29H32N6O3
- 분자량:512.60
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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
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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KRas G12C 0.92 μM (IC50) |
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.
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.
Chemical Information
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분자량 512.60
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화학식 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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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)
KD36 Related Classifications
HY-179702 Related Classifications
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