2. Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage
  3. FAK CDK DNA/RNA Synthesis
  4. 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.

FAK1/2 ligand-1

FAK1/2 ligand-1 Chemical Structure

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FAK1/2 ligand-1 Related Antibodies

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Description

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[1].

IC50 & Target[1]

FAK1

2.9 μM (Kd)

FAK2

2.5 μM (Kd)

In Vitro

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.

FAK1/2 ligand-1 Related Antibodies

Cell Cycle Analysis[1]

Cell Line: MDA-MB-468 cells
Concentration: 0.4 and 2.0 μM
Incubation Time: 24 h
Result: Induces G2/M-phase arrest at 2.0 μM.

Western Blot Analysis[1]

Cell Line: MDA-MB-468 cells
Concentration: 0.4 and 2.0 μM
Incubation Time: 24 h
Result: Decreased p-CDK1, and increased γ-H2AX and p-DNA-PKcs(S2056).
In Vivo

FAK1/2 Ligand-1 (Compound 8a) (10-20 mg/kg; i.p.; every 2 days; ~3 weeks) inhibits triple-negative breast cancer tumor growth in a dose-dependent manner in mice[1].

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

Animal Model: BALB/c (female, 4-6 weeks old, 15-20 g, subcutaneous implantation of 4T1 murine breast cancer cells)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.p.; every 2 days; ~3 weeks
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.
Molecular Weight

473.52

Formula

C26H27N5O4
SMILES

COC1=CC(CC(N(N=C2N)C3=C2C=C(C4=CC=C(N5CCOCC5)C=C4)C=N3)=O)=CC=C1OC
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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FAK1/2 ligand-1 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:

FAK1/2 ligand-1FAKCDKDNA/RNA SynthesisPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseCyclin dependent kinaseHUVEC normal endothelial cellsFAK2triple-negative breast cancer cellsFAK1MDA-MB-468 TNBC cellskinase domainsDNA damage-related signalingG2/M-phase arrest4T1 tumorCDK1Inhibitorinhibitorinhibit

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