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Table 1 Summary of FAK inhibitors in preclinical trials

From: Focal adhesion kinase: from biological functions to therapeutic strategies

Name

Alternative names

Target(s)

Cancer types

In vitro

In vivo

References

VS-6062

PF-562, 271

FAK, Pyk2

Glioma

+

+

[175]

Colon cancer

+

+

[175]

Breast cancer

+

+

[175]

Pancreatic cancer

+

+

[112, 175]

Prostate cancer

+

+

[175,176,177]

Lung cancer

+

+

[175, 178]

Hepatocellular cancer

+

+

[179]

Thyroid tumor

+

+

[180]

B16

−

+

[181]

Ovarian cancer

+

+

[182]

Ewing sarcoma

+

+

[183]

VS-6063

Defactinib, PF-04554878

FAK, Pyk2

Pancreatic cancer

+

+

[156, 184]

Lung cancer

+

+

[5, 164, 165]

Prostate cancer

+

+

[188]

Ovarian cancer

+

+

[189, 190]

Esophageal cancer

+

+

[191]

Endometrial cancer

+

+

[192]

BI-853520

IN10018, ifebemtinib

FAK

Breast cancer

+

+

[193]

KRAS G12C mutant cancer

+

+

[145]

Pancreatic cancer

+

+

[162]

Ovarian cancer

+

+

[145, 194]

Prostate cancer

+

+

[195]

PF-573228

PF-228

FAK

Pancreatic cancer

+

+

[196]

Glioma

+

−

[56]

Lung cancer

+

−

[197]

TAE226

NVP-226

FAK, IGF-IR

Breast cancer

+

+

[198, 199]

Glioma

+

+

[200, 201]

Esophageal cancer

+

+

[202, 203]

GSK2256098

–

FAK

Pancreatic cancer

+

−

[204]

Ovarian cancer

+

−

[205]

PF-431396

–

FAK, Pyk2

Pancreatic cancer

 + 

 + 

[196]

Malignant pleural mesothelioma

+

+

[196]

VS-4718

PND-1186

FAK, Pyk2

Breast cancer/ovarian cancer

+

+

[206]

Pancreatic cancer

−

+

[123]

Y15

–

FAK

Breast cancer

+

+

[207]

Lung cancer

+

+

[208]

Y11

–

FAK

Colon cancer/breast cancer

+

+

[176, 204]

C4

–

FAK-VEGFR3 interaction

Breast cancer

+

+

[209]

R2

–

FAK-p53 interaction

CRC

+

+

[210]