FAK-IN-4

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FAK-IN-4 (Compound 7d) is potential FAK inhibitor with anticancer activities. FAK-IN-4 induces cell apoptosis.

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FAK-IN-4 Chemical Structure

CAS No. : 3032200-62-4

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Description

FAK-IN-4 (Compound 7d) is potential FAK inhibitor with anticancer activities. FAK-IN-4 induces cell apoptosis^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
MCF-10A	IC₅₀	40.63 μM Compound: 7d	Cytotoxicity against human MCF-10A cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Cytotoxicity against human MCF-10A cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35569251]
MDA-MB-157	IC₅₀	12.09 μM Compound: 7d	Antiproliferative activity against human MDA-MB-157 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-157 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35569251]
MDA-MB-231	IC₅₀	8.37 μM Compound: 7d	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35569251]
MDA-MB-453	IC₅₀	9.07 μM Compound: 7d	Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-453 cells assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay	[PMID: 35569251]

In Vitro

FAK-IN-4 (Compound 7d) (0-200 μM, 72 h) shows antiproliferative activity against triple-negative breast cancer (TNBC) cells^[1].
FAK-IN-4 (0-20 μM, 24 h) inhibits cell invasion and migration of MDA-MB-231 cells^[1].
FAK-IN-4 (0-20 μM, 72 h) causes dose-dependent Y925 dephosphorylation of FAK, and induces apoptosis in MDA-MB-231 cells^[1].
FAK-IN-4 inhibits the formation of focal adhesions (FAs) and stress fibers (SFs) in MDA-MB-231 cells^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	MDA-MB-231, MDA-MB-157, MDA-MB-453 and MCF10A
Concentration:	0.78, 1.56, 3.13, 5, 6.25, 100, 12.5, 25, 50, 100 and 200 μM
Incubation Time:	72 h
Result:	Inhibited the growth of TNBC cells with IC₅₀ values of 8.37, 12.09, 9.07 and 40.63 μM against MDA-MB-231, MDA-MB-157, MDA-MB-453 and MCF10A cells.

Cell Invasion Assay^[1]

Cell Line:	MDA-MB-231
Concentration:	5, 10 and 20 μM
Incubation Time:	24 h
Result:	Significantly inhibited the invasion of MDA-MB-231 cells in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:	MDA-MB-231
Concentration:	5, 10 and 20 μM
Incubation Time:	72 h
Result:	Caused an obvious dose-dependent Y925 dephosphorylation of FAK.

Apoptosis Analysis^[1]

Cell Line:	MDA-MB-231
Concentration:	5, 10 and 20 μM
Incubation Time:	72 h
Result:	Increased the percentage of apoptotic MDA-MB-231 cells ranging from 13.10% to 41.59% in a dose-dependent manner.

Molecular Weight

334.41

Formula

C₂₀H₂₂N₄O

CAS No.

3032200-62-4

SMILES

CN(CCN(C1=NC=CC=C1)C(/C=C/C2=CNC3=C2C=CC=C3)=O)C

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

Handling Instructions (2659 KB)

References

[1]. Fei Yang, et al. Discovery of novel chloropyramine-cinnamic acid hybrids as potential FAK inhibitors for intervention of metastatic triple-negative breast cancer. Bioorg Med Chem. 2022 Jul 15;66:116809. [Content Brief]

FAK-IN-4 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:

FAK-IN-43032200-62-4FAKApoptosisPTK2 protein tyrosine kinase 2PTK2Focal adhesion kinaseMDA-MB-231MDA-MB-157MDA-MB-453MCF10AanticancerInhibitorinhibitorinhibit

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