FAK1/2 ligand-1
FAK1/2 Ligand-1 is a FAK1/FAK2 ligand with KD values of 2.9 μM and 2.5 μM for binding to FAK1 and FAK2, respectively. FAK1/2 Ligand-1 induces G2/M phase arrest, activates DNA damage-related signaling pathways, and reduces the phosphorylation level of CDK1. Antitumor agent-220 is applicable to the research of triple-negative breast cancer.
For research use only. We do not sell to patients.
- Formula: C26H27N5O4
- Molecular Weight:473.52
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
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FAK1 2.9 μM (Kd) |
FAK2 2.5 μM (Kd) |
FAK1/2 Ligand-1 (Compound 8a) (0-50 μM; 48 h) potently inhibits the proliferation of MDA-MB-468 triple-negative breast cancer (TNBC) cells with an IC50 of 1.9 μM. This compound shows high selectivity (SI=12.7) compared to normal human umbilical vein endothelial cells (HUVEC), but exhibits low activity against other cancer cell lines[1].
FAK1/2 Ligand-1 (0.4-2.0 μM; 24 h) induces G2/M phase arrest in MDA-MB-468 cells, accompanied by decreased levels of pCDK1, and activates DNA damage-related signaling pathways by upregulating the levels of pDNA-PKcs and γ-H2AX[1].
FAK1/2 Ligand-1 (1.25 μM; 48 h) significantly enhances the antiproliferative activity of Doxorubicin (HY-15142A) in MDA-MB-468 cells, but antagonizes the cytotoxic effect of Cisplatin (HY-17394), indicating that it exerts context-dependent synergistic effects[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-468 cells
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Concentration:0.4 and 2.0 μM
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Incubation Time:24 h
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Result:Induces G2/M-phase arrest at 2.0 μM.
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Cell Line:MDA-MB-468 cells
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Concentration:0.4 and 2.0 μM
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Incubation Time:24 h
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Result:Decreased p-CDK1, and increased γ-H2AX and p-DNA-PKcs(S2056).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 4-6 weeks old, 15-20 g, subcutaneous implantation of 4T1 murine breast cancer cells)[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:i.p.; every 2 days; ~3 weeks
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Result:Achieved a relative tumor volume inhibition rate (RTVI) of 52.0% and relative tumor growth inhibition rate (RTGI) of 40.0% at 10 mg/kg.
Achieved a relative tumor volume inhibition rate (RTVI) of 84.2% and relative tumor growth inhibition rate (RTGI) of 76.6% at 20 mg/kg.
Caused no significant body weight loss in either treatment group.
Chemical Information
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Molecular Weight 473.52
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Formula C26H27N5O4
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SMILES
COC1=CC(CC(N(N=C2N)C3=C2C=C(C4=CC=C(N5CCOCC5)C=C4)C=N3)=O)=CC=C1OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
FAK1/2 ligand-1 Related Classifications
HY-184307 Related Classifications
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