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Art. -Nr.: HY-189278

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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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Formel: C₃₇H₄₅FN₆O₃
Molecular Weight:640.79

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

KRAS-IN-64 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

K-RAS

Alle Ras Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
PANC-1	IC50	1.5 μM	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.	42679165
BXPC-3	IC50	> 20 μM	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.	42679165
HIEC6	IC50	> 20 μM	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.	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 K_d 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.

Western Blot Analysis^[1]

Cell Line:

MIA PaCa-2
Concentration:

1.25, 2.5, 5.0 μM
Incubation Time:

24 h
Result:

Showed no apparent activation of cleaved PARP (CL-PARP).

Cell Viability Assay^[1]

Cell Line:

MIA PaCa-2
Concentration:

0.08, 0.16, 0.32, 0.63, 1.25 μM
Incubation Time:

10 days
Result:

Inhibited colony formation.

Cell Migration Assay ^[1]

Cell Line:

MIA PaCa-2
Concentration:

1.25, 2.50, 5.00, 10.00 μM
Incubation Time:

24, 48 h
Result:

Inhibited MIA PaCa-2 cell migration in a concentration- and time-dependent manner.

In Vivo

Q29 (2.5-10.0 mg/kg; i.p.; once daily; 18 days) effectively suppresses tumor growth in mice bearing MIA PaCa-2 xenografts, with TGI rates of 31%, 61%, and 78% at 2.5, 5.0, and 10.0 mg/kg, respectively, and is well tolerated^[1].
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.

Animal Model:

BALB/c mice (4 weeks old)^[1]
Dosage:

80 mg/kg
Administration:

i.p.; once daily; 7 days
Result:

Determined the maximum tolerated dose (MTD) to be 80 mg/kg.

Animal Model:

BALB/c-nu/nu male mice (3-4 weeks old)^[1]
Dosage:

2.5-10.0 mg/kg
Administration:

i.p.; once daily; 18 days
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.

Related Protocols :

Chemical Information

Molecular Weight 640.79
Formel C₃₇H₄₅FN₆O₃
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Handling Instructions (2659 KB)

Verweise

[1]. Li ML, et al. Lead Optimization of Quinoline-Coumarin KRAS mRNA G-Quadruplex Ligands: Discovery of Non-Quaternary Ammonium Analogs as Translation Inhibitors. Journal of medicinal chemistry. 2026 Aug 27;69(16):19951-19970.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

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100 mg

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