KRAS-IN-64
KRAS-IN-64 is a KRAS inhibitor that inhibits KRAS translation by binding to and stabilizing the G-quadruplex in the 5'-UTR of KRAS mRNA, exhibits antiproliferative activity in KRAS-mutant cancer cells, and induces cell cycle arrest, non-apoptotic cell death, and PARP cleavage-mediated apoptosis (apoptosis). KRAS-IN-64 can be used for research on pancreatic cancer.
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- Formule: C37H45FN6O3
- Masse moléculaire:640.79
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Stockage:
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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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
K-RAS |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| PANC-1 | IC50 |
1.5 μM
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Cytotoxicity against human PANC-1 pancreatic cancer cells assessed as reduction in cell viability incubated for 72 hrs by high-content screening assay.
Cytotoxicity against human PANC-1 pancreatic cancer cells assessed as reduction in cell viability incubated for 72 hrs by high-content screening assay.
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42679165 |
| BXPC-3 | IC50 |
> 20 μM
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Antiproliferative activity against human BxPC-3 pancreatic cancer cells assessed as reduction in cell viability.
Antiproliferative activity against human BxPC-3 pancreatic cancer cells assessed as reduction in cell viability.
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42679165 |
| HIEC6 | IC50 |
> 20 μM
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Antiproliferative activity against human HIEC-6 normal intestinal epithelial cells assessed as reduction in cell viability.
Antiproliferative activity against human HIEC-6 normal intestinal epithelial cells assessed as reduction in cell viability.
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42679165 |
In Vitro
KRAS-IN-64 (compound Q29) (72 h) shows potent antiproliferative activity against PANC-1 pancreatic cancer cells with an IC50 of 1.5 μM[1].
KRAS-IN-64 (5.0 μM; 6 h) exhibits a cellular uptake rate of 38.3% in PANC-1 cells after 6 h[1].
KRAS-IN-64 inhibits KRAS protein expression in a dose-dependent manner in PANC-1 and MIA PaCa-2 cells[1].
KRAS-IN-64 does not affect KRAS mRNA levels in PANC-1 and MIA PaCa-2 cells[1].
KRAS-IN-64 (12 h) inhibits KRAS translation in PANC-1 cells in a KRAS rG4-dependent manner[1].
KRAS-IN-64 selectively inhibits the growth of KRAS-mutant cancer cell lines, with IC50 values of 1.5 to 3.8 μM[1].
KRAS-IN-64 (24 h) induces cell death in MIA PaCa-2 cells in a concentration-dependent manner[1].
KRAS-IN-64 (0.08-1.25 μM; 10 days) inhibits colony formation of MIA PaCa-2 cells[1].
KRAS-IN-64 (1.25-10.00 μM; 24-48 h) inhibits MIA PaCa-2 cell migration in a concentration- and time-dependent manner[1].
KRAS-IN-64 (1.0 μM) selectively binds to KRAS rG4 and produces a high fluorescence enhancement[1].
KRAS-IN-64 (1.0 μM) binds to both RNA and DNA G4s with Kd values of 0.7 to 2.9 μM, whereas it binds weakly to non-G4 RNAs[1].
KRAS-IN-64 (1.0-4.0 μM) exhibits high binding affinity for KRAS rG4 with a DC50 of 0.3 μM[1].
KRAS-IN-64 binds to KRAS rG4 with a docking score of −8.1 kcal/mol and forms a cation−π interaction with G11[1].
KRAS-IN-64 (24 h) induces cell cycle arrest at the S and G2/M phases in MIA PaCa-2 cells[1].
KRAS-IN-64 (1.25-5.00 μM; 24 h) induces cell death in MIA PaCa-2 cells without accompanying apoptosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MIA PaCa-2
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Concentration:1.25, 2.5, 5.0 μM
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Incubation Time:24 h
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Result:Showed no apparent activation of cleaved PARP (CL-PARP).
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Cell Line:MIA PaCa-2
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Concentration:0.08, 0.16, 0.32, 0.63, 1.25 μM
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Incubation Time:10 days
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Result:Inhibited colony formation.
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Cell Line:MIA PaCa-2
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Concentration:1.25, 2.50, 5.00, 10.00 μM
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Incubation Time:24, 48 h
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Result:Inhibited MIA PaCa-2 cell migration in a concentration- and time-dependent manner.
In Vivo
Q29 (80 mg/kg; i.p.; once daily; 7 days) has an MTD of 80 mg/kg in mice, indicating lower acute toxicity than the quaternary ammonium lead 15a[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c mice (4 weeks old)[1]
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Dosage:80 mg/kg
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Administration:i.p.; once daily; 7 days
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Result:Determined the maximum tolerated dose (MTD) to be 80 mg/kg.
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Animal Model:BALB/c-nu/nu male mice (3-4 weeks old)[1]
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Dosage:2.5-10.0 mg/kg
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Administration:i.p.; once daily; 18 days
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Result:Achieved tumor growth inhibition (TGI) rates of 31%, 61%, and 78% at 2.5, 5.0, and 10.0 mg/kg, respectively.
Reduced KRAS protein expression significantly compared with the control group.
- RNA extraction experimental
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Apoptosis Solutions
- Protocol for Cell Cycle
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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Masse moléculaire 640.79
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Formule C37H45FN6O3
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SMILES
FC1=C(C=C(C2=C1)N=C(C=C2C(NCCN3CCCC3)=O)/C=C/C4=CC5=C(OC4=O)C=C(C=C5)N(CC)CC)NCCN6CCCC6
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
KRAS-IN-64 Related Classifications
HY-189278 Related Classifications
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