FAK-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/FAK.html FAKPTK2 protein tyrosine kinase 2; PTK2; Focal adhesion kinaseFAK (Focal Adhesion Kinase or PTK2) is a non-receptor and non-membrane associated protein tyrosine kinase that is activated atthe sites of cell-matrix adhesions and integrin clustering by au

2、to-phosphorylation (at Tyr397), Src, and other tyrosine kinases. FAKmediates integrin-based cell signaling by transferring signals regulating cell migration, adhesion, and survival from the extracellularmatrix to the cytoplasm.FAK is overexpressed in many tumors, including those derived from the hea

3、d and neck, colon, breast, prostate, liver, and thyroid.Furthermore, FAK overexpression is highly correlated with an invasive phenotype in these tumors. Inhibition of FAK signaling byoverexpression of dominant-negative fragments of FAK reduces invasion of glioblastomas and ovarian cancer cells. FAK

4、thereforerepresents an important target for the development of anti-neoplastic and anti-metastatic drugs.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/FAK.html FAK HYPERLINK https:/www.MedChemE/Targets/FAK.html HYPERLINK https:/www.MedChemE/Targets/FAK.html Inhibitors HYPERLINK https:/www.Med

5、ChemE/ALK-inhibitor-1.html ALK HYPERLINK https:/www.MedChemE/ALK-inhibitor-1.html HYPERLINK https:/www.MedChemE/ALK-inhibitor-1.html inhibitor HYPERLINK https:/www.MedChemE/ALK-inhibitor-1.html HYPERLINK https:/www.MedChemE/ALK-inhibitor-1.html 1 HYPERLINK https:/www.MedChemE/ALK-inhibitor-1.html HY

6、PERLINK https:/www.MedChemE/ALK-inhibitor-2.html ALK HYPERLINK https:/www.MedChemE/ALK-inhibitor-2.html HYPERLINK https:/www.MedChemE/ALK-inhibitor-2.html inhibitor HYPERLINK https:/www.MedChemE/ALK-inhibitor-2.html HYPERLINK https:/www.MedChemE/ALK-inhibitor-2.html 2Cat. No.: HY-15357 Cat. No.: HY-

7、15358ALK inhibitor 1 (compound 17) is a potentpyrimidin ALK inhibitor. ALK inhibitor 1 is apotent inhibitor of testis-specificserine/threonine kinase 2 (TSSK2; IC =31 nM)50and focal adhesion kinase (FAK; IC =2 nM).50ALK inhibitor 2 (compound 18) is a potentpyrimidin ALK inhibitor. ALK inhibitor 2 is

8、 apotent inhibitor of testis-specificserine/threonine kinase 2 (TSSK2; IC =37 nM)50and focal adhesion kinase (FAK; IC =5 nM).50Purity: 99.71%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mgPurity: 99.77%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10

9、 mg HYPERLINK https:/www.MedChemE/amp-945.html AMP-945 HYPERLINK https:/www.MedChemE/amp-945.html HYPERLINK https:/www.MedChemE/batatasin-iii.html Batatasin HYPERLINK https:/www.MedChemE/batatasin-iii.html HYPERLINK https:/www.MedChemE/batatasin-iii.html IIICat. No.: HY-145652 Cat. No.: HY-122965AMP

10、-945 is an inhibitor of the enzyme focaladhesion kinase (FAK).Batatasin III, a stilbenoid, inhibits cancermigration and invasion by suppressing epithelialto mesenchymal transition (EMT) and FAK-AKTsignals. Batatasin III has anti-cancer activities.Purity: 98.96%Clinical Data: No Development ReportedS

11、ize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.70%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/BI-3663.html BI-3663 HYPERLINK https:/www.MedChemE/BI-3663.html HYPERLINK https:/www.MedChemE/bi-4464.html BI-4464Cat. No.: HY-111546 Cat. No.: HY-124625BI-3663 i

12、s a highly selective PTK2/FAK PROTAC(DC =30 nM), with ligands to hijack E350 Cereblonligases for PTK2 degradation. BI-3663 inhibitsPTK2 with an IC of 18 nM. BI-3663 is a PROTAC50that composes of BI-4464 (HY-124625) linked toPomalidomide (HY-10984) with a linker.BI-4464 is a highly selective ATP comp

13、etitiveinhibitor of PTK2/FAK, with an IC of 17 nM. A50PTK2 ligand for PROTAC.Purity: 98.14%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 99.27%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/CEP-37440.html CEP-37440 HYPERLIN

14、K https:/www.MedChemE/CEP-37440.html HYPERLINK https:/www.MedChemE/Chloropyramine_hydrochloride.html Chloropyramine HYPERLINK https:/www.MedChemE/Chloropyramine_hydrochloride.html HYPERLINK https:/www.MedChemE/Chloropyramine_hydrochloride.html hydrochlorideCat. No.: HY-15841 Cat. No.: HY-B1305CEP-37

15、440 is a novel potent and selective DualFAK/ALK inhibitor with IC50 s of 2.3 nM (FAK) and120 nM(ALK cellular IC50 in 75% human plasma).Chloropyramine hydrochloride is a histaminereceptor H1 antagonist which can also inhibit thebiochemical function of VEGFR-3 and FAK.Purity: 99.97%Clinical Data: Phas

16、e 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.73%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 50 mg HYPERLINK https:/www.MedChemE/conteltinib.html Conteltinib HYPERLINK https:/www.MedChemE/conteltinib.html HYPERLINK https:/www.MedChemE/Defactinib.html Defactinib(CT-707) Cat. N

17、o.: HY-109084 (VS-6063; PF-04554878) Cat. No.: HY-12289Conteltinib (CT-707) is a multi-kinase inhibitortargeting FAK, ALK, and Pyk2. Conteltinib exertssignificant inhibitory effect on FAK with an IC50of 1.6 nM.Defactinib (VS-6063; PF-04554878) is a novel FAKinhibitor with potential antiangiogenic an

18、dantineoplastic activities.Purity: 99.47%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 99.87%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/defactinib-hydrochloride

19、.html Defactinib HYPERLINK https:/www.MedChemE/defactinib-hydrochloride.html HYPERLINK https:/www.MedChemE/defactinib-hydrochloride.html hydrochloride(VS-6063 hydrochloride; PF 04554878 hydrochloride) Cat. No.: HY-12289A HYPERLINK https:/www.MedChemE/egfr-in-46.html EGFR-IN-46Cat. No.: HY-144794Defa

20、ctinib hydrochloride (VS-6063 hydrochloride;PF 04554878 hydrochloride) is a novel FAKinhibitor, which inhibits FAK phosphorylation atthe Tyr397 site in a time- and dose-dependentmanner.EGFR-IN-46 is a potent EGFR and FAK dualinhibitor with IC s of 20.17 nM, 14.25 nM,50respectively. EGFR-IN-46 signif

21、icantly inhibitsthe growth of cancer cells. EGFR-IN-46 inducescell apoptosis.Purity: 98.95%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/fak-inhibitor-2.html FAK HYPERLINK https:/www.M

22、edChemE/fak-inhibitor-2.html HYPERLINK https:/www.MedChemE/fak-inhibitor-2.html inhibitor HYPERLINK https:/www.MedChemE/fak-inhibitor-2.html HYPERLINK https:/www.MedChemE/fak-inhibitor-2.html 2 HYPERLINK https:/www.MedChemE/fak-inhibitor-2.html HYPERLINK https:/www.MedChemE/fak-inhibitor-5.html FAK

23、HYPERLINK https:/www.MedChemE/fak-inhibitor-5.html HYPERLINK https:/www.MedChemE/fak-inhibitor-5.html inhibitor HYPERLINK https:/www.MedChemE/fak-inhibitor-5.html HYPERLINK https:/www.MedChemE/fak-inhibitor-5.html 5Cat. No.: HY-128580 Cat. No.: HY-18928FAK inhibitor 2 is a potent focal adhesion kina

24、se(FAK) inhibitor with an IC of 0.07nM, with50antitumor and anti-angiogenesis activities.FAK inhibitor 5 (compound 2) is a novel allostericFAK inhibitor, with IC values in the low50micromolar range.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Developm

25、ent ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/fak-protac-b5.html FAK HYPERLINK https:/www.MedChemE/fak-protac-b5.html HYPERLINK https:/www.MedChemE/fak-protac-b5.html PROTAC HYPERLINK https:/www.MedChemE/fak-protac-b5.html HYPERLINK https:/www.MedChemE/fak-protac-b5.html B5 HYPERLINK ht

26、tps:/www.MedChemE/fak-protac-b5.html HYPERLINK https:/www.MedChemE/fak-in-1.html FAK-IN-1Cat. No.: HY-143458 Cat. No.: HY-145108FAK PROTAC B5 (Compound B5) is a FAK PROTACdegrader with an IC value of 14.9 nM. FAK PROTAC50B5 presents strong FAK degradation activity,antiproliferative activity, outstan

27、ding plasmastability and moderate membrane permeability. FAKPROTAC B5 inhibits cell migration and invasion.FAK-IN-1 is a FAK inhibitor with anticanceractivities (WO2020231726 (Example 27).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development Report

28、edSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/fak-in-2.html FAK-IN-2 HYPERLINK https:/www.MedChemE/fak-in-2.html HYPERLINK https:/www.MedChemE/fak-in-3.html FAK-IN-3Cat. No.: HY-144448 Cat. No.: HY-143407FAK-IN-2 is a potent and orally active focaladhesion kinase (FAK) inhibitor, with anticancera

29、ctivity (FAK IC = 35 nM).50FAK-IN-3 (Compound 36) is a potent inhibitor offocal adhesion kinase (FAK). FAK-IN-3 not onlydecreases migration and invasion of PA-1 cells,but also reduces expression of MMP-2 and MMP-9.FAK-IN-3 inhibits tumor growth and metastasis, andno obvious adverse effects.Purity: 9

30、8%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/fak-in-4.html FAK-IN-4 HYPERLINK https:/www.MedChemE/fak-in-4.html HYPERLINK https:/www.MedChemE/fak-in-5.html FAK-IN-5Cat. No.: HY-146065 Cat. No.:

31、 HY-147520FAK-IN-4 (Compound 7d) is potential FAK inhibitorwith anticancer activities. FAK-IN-4 induces cellapoptosis.FAK-IN-5 (Compound 8l) is a FAK signalinginhibitor. FAK-IN-5 induces cell apoptosis andautophagy.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical

32、Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/fangchinoline.html Fangchinoline HYPERLINK https:/www.MedChemE/fangchinoline.html HYPERLINK https:/www.MedChemE/gsk215.html GSK215Cat. No.: HY-N1372A Cat. No.: HY-132296Fangchinoline is isolated from Stephania

33、tetrandrawith extensive biological activities, such asenhancing immunity, anti-inflammatorysterilization and anti-atherosclerosis.GSK215 is a potent and selective PROTAC focaladhesion kinase (FAK) degrader. GSK215 isdesigned by a binder for the VHL E3 ligase and theFAK inhibitor VS-4718.Purity: 99.9

34、2%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/GSK2256098.html GSK2256098 HYPERLINK https:/www.MedChemE/GSK2256098.html HYPERLINK https:/www.MedChemE/harringtonolide.

35、html HarringtonolideCat. No.: HY-100498 Cat. No.: HY-N10335GSK2256098 is a selective FAK kinase inhibitor,which inhibits growth and survival of pancreaticductal adenocarcinoma cells.Harringtonolide is a potent RACK1 inhibitor(IC =39.66 M in A375 cells). Harringtonolide50inhibits the epithelial-mesen

36、chymal transition(EMT) process and cell proliferation by affectingthe interaction between FAK and RACK1.Purity: 99.74%Clinical Data: Phase 2Size: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Masitin

37、ib.html Masitinib(AB1010) Cat. No.: HY-10209 HYPERLINK https:/www.MedChemE/NAMI-A.html NAMI-ACat. No.: HY-19376Masitinib (AB1010) is a potent, orallybioavailable, and selective inhibitor of c-Kit(IC =200 nM for human recombinant c-Kit). It also50inhibits PDGFR/ (IC50s=540/800 nM), Lyn (IC50=510 nM f

38、or LynB), Lck, and, to a lesser extent,FGFR3 and FAK.NAMI-A is a ruthenium-based drug characterised bythe selective activity against tumour metastases,inhibits the adhesion and migration. In vitro:NAMI-A can significantly affect tumor cells withmetastatic ability.Purity: 99.98%Clinical Data: Phase 3

39、Size: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/nitidine-chloride.html Nitidine HYPERLINK https:/www.MedChemE/nitidine-chloride.html HYPERLINK https:/www.MedChemE/nitidin

40、e-chloride.html chloride HYPERLINK https:/www.MedChemE/nitidine-chloride.html HYPERLINK https:/www.MedChemE/NVP-TAE-226.html NVP-TAE HYPERLINK https:/www.MedChemE/NVP-TAE-226.html HYPERLINK https:/www.MedChemE/NVP-TAE-226.html 226Cat. No.: HY-N0498(TAE226) Cat. No.: HY-13203Nitidine chloride, a pote

41、ntial anti-malariallead compound derived from Zanthoxylum nitidum(Roxb) DC, exerts potent anticancer activitythrough diverse pathways, including inducingapoptosis, inhibiting STAT3 signaling cascade,DNA topoisomerase 1 and 2A, ERK andNVP-TAE 226 (TAE226) is a potent andATP-competitive dual FAK and I

42、GF-1R inhibitor withIC s of 5.5 nM and 140 nM, respectively. NVP-TAE50226 (TAE226) also effectively inhibits Pyk2 andinsulin receptor (InsR) with IC s of 3.5 nM and 4450nM, respectively.Purity: 99.61%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 20 mgPurity: 99.92%Clinical Data: No Develo

43、pment ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/pdz1i.html PDZ1i HYPERLINK https:/www.MedChemE/pdz1i.html HYPERLINK https:/www.MedChemE/petunidin-chloride.html Petunidin HYPERLINK https:/www.MedChemE/petunidin-chloride.html HYPERLINK https:/www.MedChemE/petun

44、idin-chloride.html chloride(113B7) Cat. No.: HY-124813Cat. No.: HY-126410PDZ1i is a potent, BBB-penetrated and specificMDA-9/Syntenin inhibitor. PDZ1i inhibitscrucial GBM (glioblastoma multiforme) signalinginvolving FAK and EGFRvIII. PDZ1i reduces MMPsecretion. PDZ1i can improve survival of braintum

45、or-bearing mice and reduce tumor invasion.Petunidin chloride is an O-methylatedanthocyanidin derived from delphinidin.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChe

46、mE HYPERLINK https:/www.MedChemE/PF-431396.html PF-431396Cat. No.: HY-10460 HYPERLINK https:/www.MedChemE/PF-562271.html PF-562271(VS-6062) Cat. No.: HY-10459PF-431396 is an orally active dual focal adhesionkinase (FAK) and proline-rich tyrosine kinase 2(PYK2) inhibitor, with IC values of 2 nM and 1

47、150nM, respectively.PF-562271 (VS-6062) is a potent, ATP-competitiveand reversible FAK and Pyk2 kinase inhibitorwith IC s of 1.5 nM and 13 nM, respectively.50Purity: 98.86%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mgPurity: 99.68%Clinical Data: No Development

48、ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/PF-562271-besylate.html PF-562271 HYPERLINK https:/www.MedChemE/PF-562271-besylate.html HYPERLINK https:/www.MedChemE/PF-562271-besylate.html besylate(VS-6062 besylate) Cat. No.: HY-10458 HYPERLINK https:/www.MedChemE/pf-5622

49、71-hydrochloride.html PF-562271 HYPERLINK https:/www.MedChemE/pf-562271-hydrochloride.html HYPERLINK https:/www.MedChemE/pf-562271-hydrochloride.html hydrochloride(VS-6062(hydrochloride) Cat. No.: HY-20403PF-562271 (VS-6062) besylate is a potentATP-competitive, reversible inhibitor of FAK andPyk2 ki

50、nase, with an IC of 1.5 nM and 13 nM,50respectively.PF-562271 (VS-6062) hydrochloride is a potent,ATP-competitive and reversible FAK and Pyk2kinase inhibitor with IC s of 1.5 nM and 13 nM,50respectively.Purity: 99.17%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 9

51、8%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/PF-573228.html PF-573228Cat. No.: HY-10461 HYPERLINK https:/www.MedChemE/PND-1186.html PND-1186(VS-4718; SR-2516) Cat. No.: HY-13917PF-573228 is a potent and selective FAK inhibitorwith IC of 4 nM for purified rec

52、ombinant50catalytic fragment of FAK.PND-1186 (VS-4718) is a potent, highly-specificand reversible inhibitor of FAK with an IC of501.5 nM. PND-1186 selectively promotes tumor cellapoptosis.Purity: 99.66%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 500 mgPurity: 99.80%

53、Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/pnd-1186-hydrochloride.html PND-1186 HYPERLINK https:/www.MedChemE/pnd-1186-hydrochloride.html HYPERLINK https:/www.MedChemE/pnd-1186-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/pnd-11

54、86-hydrochloride.html HYPERLINK https:/www.MedChemE/protac-fak-degrader-1.html PROTAC HYPERLINK https:/www.MedChemE/protac-fak-degrader-1.html HYPERLINK https:/www.MedChemE/protac-fak-degrader-1.html FAK HYPERLINK https:/www.MedChemE/protac-fak-degrader-1.html HYPERLINK https:/www.MedChemE/protac-fa

55、k-degrader-1.html degrader HYPERLINK https:/www.MedChemE/protac-fak-degrader-1.html HYPERLINK https:/www.MedChemE/protac-fak-degrader-1.html 1(VS-4718 hydrochloride; SR-2516 hydrochloride) Cat. No.: HY-13917ACat. No.: HY-119932PND-1186 hydrochloride (VS-4718 hydrochloride) isa potent, highly-specific and reversible inhibitorof FAK with an IC of 1.5 nM. PND-118650hydrochloride selectively promotes tumor cellapoptosis.PROTAC FAK degrader 1 is a selective and potentvon Hippel-Lindau-based focal adhesion kinase (