c-Fms-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/c-Fms.html c-FmsCSF-1 receptor; colony stimulating factor 1 receptor; CSF-1R; CSF1Rc-FMS (CSF1R, CSF-1R) is a receptor protein-tyrosine kinase of the platelet-derived growth factor receptor (PDGFR) family. c-FMS isthe cell surface receptor for IL-34 and CSF1. c

2、-FMS has important roles in haematopoiesis, regulation of proliferation, cell survivaland maturation of microglia and monocytes, as well as in controlling the overall immune response.c-FMS is specifically expressed in osteoclasts and myelomonocytic-lineage cells, such as monocytes and macrophages, a

3、nd theactivation of c-FMS signaling promotes the proliferation or differentiation of these cells. It also promotes the production ofinflammatory mediators, such as tumor necrosis factor-alpha (TNF-) and interleukin 6 (IL6).www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/c-Fms.html c-Fms HYPERLI

4、NK https:/www.MedChemE/Targets/c-Fms.html HYPERLINK https:/www.MedChemE/Targets/c-Fms.html Inhibitors HYPERLINK https:/www.MedChemE/AZD7507.html AZD7507 HYPERLINK https:/www.MedChemE/AZD7507.html HYPERLINK https:/www.MedChemE/bpr1r024.html BPR1R024Cat. No.: HY-117244 Cat. No.: HY-132935AZD7507 is a

5、potent and orally active CSF-1Rinhibitor, with antitumor activity.BPR1R024 is an orally active and selective CSF1Rinhibitor (IC = 0.53 nM).50Purity: 99.45%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5

6、mg HYPERLINK https:/www.MedChemE/c-fms-in-1.html c-Fms-IN-1 HYPERLINK https:/www.MedChemE/c-fms-in-1.html HYPERLINK https:/www.MedChemE/c-fms-in-10.html c-Fms-IN-10Cat. No.: HY-18791 Cat. No.: HY-126297c-Fms-IN-1 is a FMS kinase inhibitor with anIC of 0.0008 M.50c-Fms-IN-10 is the derivative of thie

7、no 3,2-dpyrimidine, an kinase inhibitor of FMS (Colonystimulating factor-1 receptor, CSF-1R) with IC50of 2 nM. c-Fms-IN-10 has anti-tumor activity.Purity: 99.85%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.04%Clinical Data: No Development ReportedSize:

8、 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/cFMS-IN-2.html c-Fms-IN-2 HYPERLINK https:/www.MedChemE/cFMS-IN-2.html HYPERLINK https:/www.MedChemE/c-FMS-inhibitor.html c-Fms-IN-3Cat. No.: HY-18787 Cat. No.: HY-13075c-Fms-IN-2 is a FMS kinase inhibitor with anIC of 0.02

9、4 M.50c-Fms-IN-3 is a novel c-Fms kinase inhibitor witha potential as anti-inflammatory agent andantirheumatic agent.Purity: 99.05%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.39%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg

10、 HYPERLINK https:/www.MedChemE/c-fms-in-6.html c-Fms-IN-6 HYPERLINK https:/www.MedChemE/c-fms-in-6.html HYPERLINK https:/www.MedChemE/c-fms-in-7.html c-Fms-IN-7Cat. No.: HY-111947 Cat. No.: HY-111948c-Fms-IN-6 is a potent inhibitor of c-FMS, withan IC of 10 nM for unphosphorylated c-FMS, also50weakl

11、y inhibits unphosphorylated c-KIT and PDGFR(IC , 1 M). Used in the research of50autoimmune diseases.c-Fms-IN-7 is a cFMS inhibitor extracted frompatent WO2011079076A1, example159, has an IC of5018.5 nM.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Deve

12、lopment ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/c-fms-in-8.html c-Fms-IN-8 HYPERLINK https:/www.MedChemE/c-fms-in-8.html HYPERLINK https:/www.MedChemE/c-fms-in-9.html c-Fms-IN-9Cat. No.: HY-119942 Cat. No.: HY-128680c-Fms-IN-8 (compound 4a) is a colony stimulatingfactor-1 receptor (CS

13、F-1R, c-FMS) Type IIinhibitor, with an IC of 9.1 nM.50c-Fms-IN-9 is a c-FMS inhibitor extracted frompatent WO2014145023A1, Compound Example 7.c-Fms-IN-9 inhibits unphosphorylated c-FMS kinase(uFMS) and uKIT with IC s of 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mgPurity:

14、 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/cfms-receptor-inhibitor-ii.html cFMS HYPERLINK https:/www.MedChemE/cfms-receptor-inhibitor-ii.html HYPERLINK https:/www.MedChemE/cfms-receptor-inhibitor-

15、ii.html Receptor HYPERLINK https:/www.MedChemE/cfms-receptor-inhibitor-ii.html HYPERLINK https:/www.MedChemE/cfms-receptor-inhibitor-ii.html Inhibitor HYPERLINK https:/www.MedChemE/cfms-receptor-inhibitor-ii.html HYPERLINK https:/www.MedChemE/cfms-receptor-inhibitor-ii.html IICat. No.: HY-112451 HYP

16、ERLINK https:/www.MedChemE/chiauranib.html Chiauranib(CS2164) Cat. No.: HY-124526cFMS Receptor Inhibitor II is a CSF1R kinaseinhibitor. CSF-1 is a cytokine.Chiauranib (CS2164) is an orally activemulti-target inhibitor against tumor angiogenesis.Purity: 99.80%Clinical Data: No Development ReportedSiz

17、e: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.28%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/CSF1R-IN-1.html CSF1R-IN-1 HYPERLINK https:/www.MedChemE/CSF1R-IN-1.html HYPERLINK https:/www.MedChemE/TPX-022.html CSF1R-IN-

18、2Cat. No.: HY-101774 Cat. No.: HY-111787CSF1R-IN-1 is a CSF1R inhibitor with an with anIC of 0.5 nM.50CSF1R-IN-2 (compound 5) is an oral-activeinhibitor of SRC, MET and c-FMS, with IC50values of 0.12 nM, 0.14 nM and 0.76 nM for SRC,MET and c-FMS respectively.Purity: 98.75%Clinical Data: No Developme

19、nt ReportedSize: 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.97%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/csf1r-in-3.html CSF1R-IN-3 HYPERLINK https:/www.MedChemE/csf1r-in-3.html HYPERLINK https:/www.MedChemE/csf1r-i

20、n-4.html CSF1R-IN-4Cat. No.: HY-139990 Cat. No.: HY-144040CSF1R-IN-3 (compound 21) is a potent and orallyactive CSF-1R inhibitor (IC =2.1 nM). CSF1R-IN-350is a potent antiproliferative activity againstcolorectal cancer cells.CSF1R-IN-4 is a potent inhibitor of CSF1R. CSF-1Ris expressed in macrophage

21、s, and the survival anddifferentiation of macrophages depends on theCSF-1/CSF-1R signaling pathway. CSF1R-IN-4 affectsthe exchange of inflammatory factors between TAMsand glioma cells.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSi

22、ze: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/csf1r-in-5.html CSF1R-IN-5 HYPERLINK https:/www.MedChemE/csf1r-in-5.html HYPERLINK https:/www.MedChemE/Dovitinib.html DovitinibCat. No.: HY-144041(CHIR-258; TKI258) Cat. No.: HY-50905CSF1R-IN-5 is a potent inhibitor of CSF1R. CSF-1Ris expressed in macroph

23、ages, and the survival anddifferentiation of macrophages depends on theCSF-1/CSF-1R signaling pathway. CSF1R-IN-5 affectsthe exchange of inflammatory factors between TAMsand glioma cells.Dovitinib (CHIR-258) is an orally active, potentmulti-targeted tyrosine kinase (RTK) inhibitorwith IC s of 1, 2,

24、36, 8/9, 10/13/8, 27/210 nM50for FLT3, c-Kit, CSF-1R, FGFR1/FGFR3,VEGFR1/VEGFR2/VEGFR3 and PDGFR/PDGFR,respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.94%Clinical Data: Phase 3Size: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg HYPERLINK https:/www.MedChem

25、E/Edicotinib.html Edicotinib HYPERLINK https:/www.MedChemE/Edicotinib.html HYPERLINK https:/www.MedChemE/GENZ-882706.html GENZ-882706(JNJ-40346527; JNJ-527) Cat. No.: HY-109086 (RA03546849) Cat. No.: HY-101526Edicotinib (JNJ-40346527) is a potent, selective,brain penetrant and orallyactive colony-st

26、imulating factor-1receptor (CSF-1R) inhibitor with an IC of503.2 nM.GENZ-882706 is a potent colony stimulatingfactor-1 receptor (CSF-1R) Inhibitor extractedfrom patent WO 2017015267A1.Purity: 99.56%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No

27、Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/GENZ-882706_Raceme_.html GENZ-882706(Raceme)(GENZ-882706 racemate) Cat. No.: HY-101526R HYPERLINK https:/www.MedChemE/GW2580.html GW2580Cat. No.: HY-10917GENZ-882706(Raceme) is the racemate ofGENZ-882706.GW2580 is an or

28、ally bioavailable and selectiveinhibitor of c-Fms kinase which completelyinhibits human cFMS kinase in vitro at 0.06 M.GW2580 acts as a competitive inhibitor of ATPbinding to the cFMS kinase and inhibitscolony-stimulating-factor-1 signaling.Purity: 98.79%Clinical Data: No Development ReportedSize: 1

29、 mg, 5 mgPurity: 99.83%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g HYPERLINK https:/www.MedChemE/gw2580-d6.html GW2580-d6 HYPERLINK https:/www.MedChemE/gw2580-d6.html HYPERLINK https:/www.MedChemE/ihmt-trk-284.html IHMT-TRK-284Cat. No.: HY-10917S

30、 Cat. No.: HY-146697GW2580-d6 is the deuterium labeled GW2580. GW2580is an orally bioavailable and selective inhibitorof c-Fms kinase which completely inhibits humancFMS kinase in vitro at 0.06 M.IHMT-TRK-284 (Compound 34) is a potent, orallyactive type II TRK kinase inhibitor with IC50values of 10.

31、5, 0.7, and 2.6 nM to TRKA, B, andC respectively. IHMT-TRK-284 displays greatselectivity profile in the kinome and good in vivoantitumor efficacies.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.

32、MedChemE/JTE-952.html JTE-952 HYPERLINK https:/www.MedChemE/JTE-952.html HYPERLINK https:/www.MedChemE/Ki20227.html Ki20227Cat. No.: HY-122906 Cat. No.: HY-10408JTE-952 is a potent, oral active and selectiveType II inhibitor of colony stimulating factor-1receptor (CSF-1R or cFMS, type III receptorty

33、rosine kinase), with IC values of 13 nM and50261 nM for CSF1R and TrkA , respectively.Ki20227 is an orally active and highly selectivec-Fms tyrosine kinase (CSF1R) inhibitor withIC s of 2 nM, 12 nM, 451 and 217 nM for CSF1R,50VEGFR2 (vascular endothelial growth factorreceptor-2), c-Kit (stem cell fa

34、ctor receptor) andPDGFR (platelet-derived growth factorPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.17%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/linifanib.html Linifanib HYPERLINK http

35、s:/www.MedChemE/linifanib.html HYPERLINK https:/www.MedChemE/OSI-930.html OSI-930(ABT-869; AL-39324) Cat. No.: HY-50751Cat. No.: HY-10204Linifanib (ABT-869) is a potent and orally activemulti-target inhibitor of VEGFR and PDGFR familywith IC s of 4, 3, 66, and 4 nM for KDR, FLT1,50PDGFR, and FLT3, r

36、espectively. Linifanib showsprominent antitumor activity.OSI-930 is an orally selective inhibitor of Kit,KDR and CSF-1R (c-Fms) with IC s of 80 nM, 950nM and 15 nM, respectively. OSI-930 alsomoderately inhibits Flt-1, c-Raf, Lck and lowactivity against PDGFR/, Flt-3 and Abl. OSI-930has antitumor act

37、ivity.Purity: 99.72%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mgPurity: 98.13%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/Pazopanib-Hydrochloride.html Pazopanib HYPERLINK https:/www.MedChemE/Pazopanib-Hydrochloride.html HYPER

38、LINK https:/www.MedChemE/Pazopanib-Hydrochloride.html Hydrochloride HYPERLINK https:/www.MedChemE/Pazopanib-Hydrochloride.html HYPERLINK https:/www.MedChemE/Pexidartinib.html Pexidartinib(GW786034 (Hydrochloride) Cat. No.: HY-12009 (PLX-3397) Cat. No.: HY-16749Pazopanib Hydrochloride (GW786034 Hydro

39、chloride)is a novel multi-target inhibitor of VEGFR1,VEGFR2, VEGFR3, PDGFR, c-Kit, FGFR1, andc-Fms with an IC of 10, 30, 47, 84, 74, 14050and 146 nM, respectively.Pexidartinib (PLX-3397) is a potent, orallyactive, selective, and ATP-competitive colonystimulating factor 1 receptor (CSF1R or M-CSFR)an

40、d c-Kit inhibitor, with IC s of 20 and 10 nM,50respectively.Purity: 99.84%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mg, 500 mgPurity: 99.64%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE H

41、YPERLINK https:/www.MedChemE/pexidartinib-hydrochloride.html Pexidartinib HYPERLINK https:/www.MedChemE/pexidartinib-hydrochloride.html HYPERLINK https:/www.MedChemE/pexidartinib-hydrochloride.html hydrochloride(PLX-3397 hydrochloride) Cat. No.: HY-16749A HYPERLINK https:/www.MedChemE/PF-477736.html

42、 PF HYPERLINK https:/www.MedChemE/PF-477736.html HYPERLINK https:/www.MedChemE/PF-477736.html 477736(PF 00477736) Cat. No.: HY-10032Pexidartinib hydrochloride (PLX-3397hydrochloride) is a potent, orally active,selective, and ATP-competitive colony stimulatingfactor 1 receptor (CSF1R or M-CSFR) and c

43、-Kitinhibitor, with IC s of 20 and 10 nM,50respectively.PF 477736 (PF 00477736) is a potent, selective andATP-competitive inhibitor of Chk1, with a K ofi0.49 nM, it is also a Chk2 inhibitor, with a Kiof 47 nM.Purity: 99.89%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 200 mg, 500 mg,

44、1 gPurity: 99.21%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/plx5622.html PLX5622 HYPERLINK https:/www.MedChemE/plx5622.html HYPERLINK https:/www.MedChemE/plx5622-hemifumarate.html PLX5622 HYPERLINK https:/www.MedChemE/plx5622-hemifumarate

45、.html HYPERLINK https:/www.MedChemE/plx5622-hemifumarate.html hemifumarateCat. No.: HY-114153 Cat. No.: HY-114153APLX5622 is a highly selective brain penetrant andorally active CSF1R inhibitor (IC =0.016 M;50K=5.9 nM). PLX5622 allows for extended andispecific microglial elimination, preceding anddur

46、ing pathology development. PLX5622 demonstratesdesirable PK properties in varies animals.PLX5622 hemifumarate is a highly selective brainpenetrant and orally active CSF1R inhibitor(IC50=0.016 M; Ki=5.9 nM). PLX5622 hemifumarateallows for extended and specific microglialelimination, preceding and dur

47、ing pathologydevelopment.Purity: 99.95%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.64%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/PLX647.html PLX647 HYPERLINK https:/www.MedChemE/PLX647.html HYPERLINK https:/www.MedChemE/plx647-dihydrochloride.html PLX647 HYPERLINK https:/www.MedChemE/plx647-dihydrochloride.html HYPERLINK https:/www.MedChemE/plx647-dihydrochloride.html dihydrochlorideCat. No.: HY-13838 Cat. No.: HY-13838APLX647 is an orally active, highly specific dualFMS and KI