FAK

Inhibitory Selectivity

Catalog No.	Inhibitor Name	FAK	Other
A12580	PF-00562271	****	CDK2/CyclinE,CDK3/CyclinE,CDK1/CyclinB
A11192	PF-562271	****	CDK2/CyclinE,CDK3/CyclinE,CDK1/CyclinB
A11235	PF-573228	*
A11507	TAE226	**	Insulin Receptor,IGF-1R,c-Met
A11171	PF-03814735	*	Aurora A,Aurora B,FLT1
A11142	PF-431396	**
A13140	PND-1186	****
A11929	Defactinib
A15543	CEP-37440	**	ALK
A15765	GSK2256098	****

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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PF 431396

Catalog No. A11142
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FAK/PYK2 抑制剂

PF 431396是一种双粘着斑激酶（FAK）和富含脯氨酸的酪氨酸激酶2（PYK2）抑制剂（IC50值分别为2和11 nM）。了解更多

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PF-03814735

Catalog No. A11171
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Aurora A/B Kinase 抑制剂

PF-03814735是一种新颖，有效且可逆的Aurora A/B抑制剂，IC50为0.8 nM/5 nM，对Flt3，FAK，TrkA的效力较低，对Met和FGFR1的活性最低。了解更多

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PF-00562271

Catalog No. A12580
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FAK 抑制剂

PF-00562271是PF-562271的苯磺酸盐，是一种有效的，ATP竞争性，可逆的FAK和Pyk2抑制剂，IC50分别为1.5 nM和14 nM。了解更多

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PND-1186

Catalog No. A13140
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FAK 抑制剂

PND-1186是一种强效fak抑制剂，ic50为1.5 nm。了解更多

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PF-4618433

Catalog No. A13461
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PYK2/FAK 抑制剂

PF-4618433与原型BIRB796相比，PF-4618433显示出PYK2效价提高、p38活性降低和总体选择性优越。了解更多

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CEP-37440

Catalog No. A15543
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FAK/ALK 抑制剂

CEP-37440是一种新型的高效选择性FAK/ALK双重抑制剂，IC50为2.3 nM（FAK）和120 nM（ALK细胞在50％人血浆中的IC50。了解更多

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PF-562271

Catalog No. A11192
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FAK 抑制剂

PF-562271是一种有效的，ATP竞争性的，可逆的FAK抑制剂，作用于FAK比作用于Pyk2选择性高10倍左右，比作用于其他蛋白激酶（除了一些CDKs）选择性高100倍以上。了解更多

Product Citations (1)

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- Jiping Yue, .et al. In vivo epidermal migration requires focal adhesion targeting of ACF7, Nat Commun, 2016, 7: 11692 PMID: 27216888
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PF 573228

Catalog No. A11235
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FAK 抑制剂

PF 573228是一种有效和选择性的粘着斑激酶（FAK）抑制剂（IC50 = 4 nM）。了解更多

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- Izumi D, .et al. CXCL12/CXCR4 activation by cancer-associated fibroblasts promotes integrin β1 clustering and invasiveness in gastric cancer, Int J Cancer, 2016, Mar 1;138(5):1207-19 PMID: 26414794
- Aya Yokota-Nakatsuma, .et al. Beta 1-integrin ligation and TLR ligation enhance GM-CSF-induced ALDH1A2 expression in dendritic cells, but differentially regulate their anti-inflammatory properties, Sci Rep, 2016, 6: 37914 PMID: 27897208
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PF-04554878 (Defactinib)

Catalog No. A11929
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FAK 抑制剂

PF-04554878 (Defactinib)是一种新型FAK激酶抑制剂，可降低胰腺神经内分泌肿瘤细胞的生长并诱导其凋亡。了解更多

Product Citations (1)

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- Shalana O'Brien, .et al. FAK inhibition with small molecule inhibitor Y15 decreases viability, clonogenicity, and cell attachment in thyroid cancer cell lines and synergizes with targeted therapeutics, Oncotarget., 2014, Sep; 5(17): 7945-7959. PMID: 25277206
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NVP-TAE 226

Catalog No. A11507
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FAK 抑制剂

NVP-TAE 226是一种强效FAK抑制剂，IC50为5.5 nM，对pyk2(IC50=3.5 nM)有适度的强效作用；对InsR, IGF-1R, ALK和c-Met的效力降低10-100倍。了解更多

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GSK2256098

Catalog No. A15765
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FAK 抑制剂

GSK2256098是一种粘着斑激酶1（FAK）抑制剂，具有潜在的抗血管生成和抗肿瘤活性。了解更多

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BI-4464

Catalog No. A18894
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PTK2/FAK inhibitor

BI-4464 is a highly selective ATP competitive inhibitor of PTK2/FAK, with an IC50 of 17 nM. A PTK2 ligand for PROTAC. 了解更多

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Y15

Catalog No. A21472
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FAK inhibitor

Y15 is a potent and specific inhibitor of focal adhesion kinase (FAK) that inhibits its autophosphorylation activity, decreases the viability of cancer cells, and blocks tumor growth. 了解更多

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Defactinib

Catalog No. A21958
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FAK inhibitor

Defactinib (VS-6063; PF-04554878) is a novel FAK inhibitor with potential antiangiogenic and antineoplastic activities. 了解更多

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Defactinib hydrochloride

Catalog No. A22003
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FAK inhibitor

Defactinib hydrochloride (VS-6063 hydrochloride; PF 04554878 hydrochloride) is a novel FAK inhibitor, which inhibits FAK phosphorylation at the Tyr397 site in a time- and dose-dependent manner. 了解更多

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