1. Protein Tyrosine Kinase/RTK Apoptosis
  2. FAK Apoptosis
  3. FAK-IN-29

FAK-IN-29 is a selective FAK inhibitor with an IC50 of 0.5 nM. FAK-IN-29 can inhibit the proliferation and colony formation of MDA-MB-231 cells, and induce cell cycle arrest and apoptosis. FAK-IN-29 exhibits antitumor activity and can be used for the research of tumors such as triple-negative breast cancer.

For research use only. We do not sell to patients.

FAK-IN-29

FAK-IN-29 Chemical Structure

CAS No. : 3104566-26-6

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Description

FAK-IN-29 is a selective FAK inhibitor with an IC50 of 0.5 nM. FAK-IN-29 can inhibit the proliferation and colony formation of MDA-MB-231 cells, and induce cell cycle arrest and apoptosis. FAK-IN-29 exhibits antitumor activity and can be used for the research of tumors such as triple-negative breast cancer[1].

In Vitro

FAK-IN-29 (Compound 7h) (3 μM; 24 h) induces G2/M phase cell cycle arrest in MDA-MB-231 cells[1].
FAK-IN-29 (0.15625-50 μM, 48 h) has IC50 values of 0.18, 0.17, and 0.15 μM against MDA-MB-231, SKOV3, and HepG2 cells, respectively[1].

FAK-IN-29 (0.3-3 μM; 24 h) induces concentration-dependent apoptosis in MDA-MB-231 cells[1].

FAK-IN-29 (0.3-3 μM; 24 h) significantly inhibits colony formation in MDA-MB-231 cells[1].

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

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231
Concentration: 3 μM
Incubation Time: 24 h
Result: Caused a significant accumulation of MDA-MB-231 cells in the G2/M phase, with a corresponding decrease in the G0/G1 phase. The G2/M phase population increased from 10.4% to 35.7%, while the G0/G1 phase decreased from 68.3% to 45.2%.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231
Concentration: 0.3, 1, and 3 μM
Incubation Time: 24 h
Result: Induced apoptosis in a concentration-dependent manner. The total apoptotic rates were 5.62 %, 33.15 %, and 62.48 % at concentrations of 0.3, 1, and 3 μM, respectively.
In Vivo

FAK-IN-29 (5-10 mg/kg, i.v., 14 days) demonstrates potent antitumor activity with favorable safety profiles in a MDA-MB-231 tumor xenograft nude mice model[1].

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

Animal Model: BALB/c nude mice (MDA-MB-231 tumor xenograft model)[1]
Dosage: 5 mg/kg, 10 mg/kg
Administration: i.v.
Result: Achieved 61.8% tumor growth inhibition in MDA-MB-231 xenograft models, comparable to Paclitaxel (HY-B0015) (54.8%) at 10 mg/kg.
Significantly reduced Tumor volumes in both 5 mg/kg and 10 mg/kg groups.
Caused no observable toxicity, and body weights and organ weights remained stable.
Caused no histopathological abnormalities.
Molecular Weight

502.54

Formula

C26H27FN8O2

CAS No.
SMILES

O=C(NC)C1=CC=CC=C1NC2=C3C(NC=C3F)=NC(NC4=CC=CC(CC(N5CCNCC5)=O)=C4)=N2

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    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.

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FAK-IN-29
Cat. No.:
HY-179679
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