2. GPCR/G Protein MAPK/ERK Pathway Cell Cycle/DNA Damage PI3K/Akt/mTOR NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Apoptosis
  3. Ras PERK Akt Reactive Oxygen Species (ROS) Apoptosis Mitochondrial Metabolism
  4. 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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KD36

KD36 Chemical Structure

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KD36 Related Antibodies

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Description

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)[1].

IC50 & Target[1]

KRas G12C

0.92 μM (IC50)

In Vitro

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.

KD36 Related Antibodies

Western Blot Analysis[1]

Cell Line: NCI–H23, NCI–H2228
Concentration: 0.5 μM, 1.0 μM, 2.0 μM, 4.0 μM, 8.0 μM
Incubation Time: 8 h
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.

Immunofluorescence[1]

Cell Line: NCI–H23 cells
Concentration: 0.5 μM, 1.0 μM, 2.0 μM, 4.0 μM
Incubation Time: 24 h, 48 h
Result: Increased the levels of JC-1 monmers and DCFH-DA fluorescence intensity.
In Vivo

KD36 (30 mg/kg, i.p., once daily for 11 days) significantly inhibits tumor growth in the NCI-H358 xenograft mice models with a tumor growth inhibition (TGI) rate of 54.6%[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NCI-H358 xenograft mice models (male, 6 weeks)[1]
Dosage: 30 mg/kg
Administration: Intraperitoneally injection
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.
Molecular Weight

512.60

Formula

C29H32N6O3
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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KD36 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KD36KD 36KD-36RasPERKAktReactive Oxygen Species (ROS)ApoptosisMitochondrial MetabolismProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinasePKBProtein kinase BPyrimidineKRAS-G12CStructure-activity relationshipNSCLCInhibitorinhibitorinhibit

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