c-Met-HGFR-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/c-Met_HGFR.html c-Met/HGFRc-Met (hepatocyte growth factor receptor, HGFR) is a protein possesses tyrosine kinase activity. The primary single chain precursorprotein is post-translationally cleaved to produce the alpha and beta subunits, which are disulfide link

2、ed to form the maturereceptor. c-Met is a membrane receptor that is essential for embryonic development and wound healing. Hepatocyte growth factor(HGF) is the only known ligand of the c-Met receptor. c-Met is normally expressed by cells of epithelial origin, while expression ofHGF is restricted to

3、cells of mesenchymalorigin. Upon HGF stimulation, c-Met induces several biological responses that collectivelygive rise to a program known as invasive growth.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/c-Met/HGFR.html c-Met/HGFR HYPERLINK https:/www.MedChemE/Targets/c-Met/HGFR.html HYPERLIN

4、K https:/www.MedChemE/Targets/c-Met/HGFR.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/c-Met/HGFR.html HYPERLINK https:/www.MedChemE/Targets/c-Met/HGFR.html Agonists HYPERLINK https:/www.MedChemE/Targets/c-Met/HGFR.html HYPERLINK https:/www.MedChemE/Targets/c-Met/HGFR.html & HYPERLINK https

5、:/www.MedChemE/Targets/c-Met/HGFR.html HYPERLINK https:/www.MedChemE/Targets/c-Met/HGFR.html Activators HYPERLINK https:/www.MedChemE/ac-386.html AC-386Cat. No.: HY-143463 HYPERLINK https:/www.MedChemE/Altiratinib.html Altiratinib(DCC-2701) Cat. No.: HY-B0791AC-386 is a highly potent c-Met inhibitor

6、 withIC value of 7.42 nM. AC-386 has50antiproliferative activities against certaincancer cell lines. AC-386 can be used forresearching anti-cancer resistance.Altiratinib (DCC-2701) is a multi-targeted kinaseinhibitor with IC s of 2.7, 8, 9.2, 9.3, 0.85,504.6, 0.83 nM for MET, TIE2, VEGFR2, FLT3,Trk1

7、, Trk2, and Trk3 respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.06%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/AMG-208.html AMG-208 HYPERLINK https:/www.MedChemE/AMG-208.html HYPERLINK https:/www.MedChemE/

8、AMG-337.html AMG-337Cat. No.: HY-12035 Cat. No.: HY-18696AMG-208 is an orally active c-Met/RON dualselective inhibitor with an IC of 9 nM for50c-Met. AMG-208 is a CYP3A4 inhibitor with an IC50of 32 M. AMG-208 has anti-cancer activity.AMG-337 is a potent and highly selective smallmolecule ATP-competi

9、tive MET kinase inhibitor. AMG337 inhibits MET kinase activity with an IC50 of98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.07%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Amuvatinib_hydrochloride.html A

10、muvatinib HYPERLINK https:/www.MedChemE/Amuvatinib_hydrochloride.html HYPERLINK https:/www.MedChemE/Amuvatinib_hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/Amuvatinib_hydrochloride.html HYPERLINK https:/www.MedChemE/antitumor-agent-45.html Antitumor HYPERLINK https:/www.MedChemE/an

11、titumor-agent-45.html HYPERLINK https:/www.MedChemE/antitumor-agent-45.html agent-45(MP470 hydrochloride; HPK 56 hydrochloride) Cat. No.: HY-10206ACat. No.: HY-144394Amuvatinib hydrochloride (MP470 hydrochloride) isan orally bioavailable multi-targeted tyrosinekinase inhibitor with potent activity a

12、gainstmutant c-Kit, PDGFR, Flt3, c-Met and c-Ret.Antitumor agent-45 (Compound 21) could induce andstimulate A549 cells apoptosis in G0/G1 and G2/Mphase. Antitumor agent-45 (Compound 21) inhibitsc-Met expression to regulate the growth of tumorcells.Purity: 98%Clinical Data: Phase 2Size: 1 mg, 5 mgPur

13、ity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/bay-474.html BAY-474 HYPERLINK https:/www.MedChemE/bay-474.html HYPERLINK https:/www.MedChemE/BMS-777607.html BMS HYPERLINK https:/www.MedChemE/BMS-777607.html HYPERLINK https:/www.MedChemE/BMS-777607.html 7

14、77607Cat. No.: HY-133083(BMS 817378) Cat. No.: HY-12076BAY-474 is a tyrosine-protein kinase c-Metinhibitor. BAY-474 acts as an epigenetics probe.BMS 777607 (BMS 817378) is a Met-relatedinhibitor for c-Met, Axl, Ron and Tyro3 withIC s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM,50respectively, and 40-fold m

15、ore selective forMet-related targets than Lck, VEGFR-2, and TrkA/B,with more than 500-fold greater selectivityPurity: 99.86%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.04%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg2 Tel:

16、609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/BMS-794833.html BMS-794833Cat. No.: HY-10497 HYPERLINK https:/www.MedChemE/bozitinib.html Bozitinib(PLB-1001; CBT-101; Vebreltinib) Cat. No.: HY-125017BMS-794833 is a VEGFR2 and Met inhibitorextracted from patent WO200

17、9094417, compoundexample 1; has IC s of 15 and 1.7 nM,50respectively.Bozitinib (PLB-1001) is a highly selectivec-MET kinase inhibitor with blood-brain barrierpermeability. Bozitinib (PLB-1001) is aATP-competitive small-molecule inhibitor, binds tothe conventional ATP-binding pocket of thetyrosine ki

18、nase superfamily.Purity: 99.78%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.66%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/bpi-9016m.html BPI-9016M HYPERLINK https:/www.MedChemE/bpi-9016m.html

19、 HYPERLINK https:/www.MedChemE/c-Kit-IN-1.html c-Kit-IN-1Cat. No.: HY-114356 Cat. No.: HY-15240BPI-9016M is a potent, orally active,and selective dual c-Met and AXL tyrosinekinases inhibitor. BPI-9016M suppresses tumor cellgrowth, migration and invasion of lungadenocarcinoma.c-Kit-IN-1 is a potent i

20、nhibitor of c-Kit andc-Met with IC s of 98%Clinical Data: Phase 1Size: 1 mg, 5 mgPurity: 98.72%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/c-Met-inhibitor-1.html c-Met HYPERLINK https:/www.MedChemE/c-Met-inhibitor-1.html HYPERLINK https:/ww

21、w.MedChemE/c-Met-inhibitor-1.html inhibitor HYPERLINK https:/www.MedChemE/c-Met-inhibitor-1.html HYPERLINK https:/www.MedChemE/c-Met-inhibitor-1.html 1 HYPERLINK https:/www.MedChemE/c-Met-inhibitor-1.html HYPERLINK https:/www.MedChemE/c-met-in-1.html c-Met-IN-1Cat. No.: HY-15735 Cat. No.: HY-101031c

22、-Met inhibitor 1 is an inhibitor of the c-Metreceptor signaling pathway useful for thetreatment of cancer including gastric,glioblastoma, and pancreatic cancer.c-met-IN-1 (compound 16) is a potent and selectivec-Met inhibitor, with IC of 1.1 nM, with50antitumor activity.Purity: 98.01%Clinical Data:

23、No Development ReportedSize: 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/c-Met-IN-2.html c-Met-IN-2 HYPERLINK https:/www.MedChemE/c-Met-IN-2.html HYPERLINK https:/www.MedChemE/c-met-in-9.html c-Met-IN-9Cat. No.

24、: HY-101773 Cat. No.: HY-115937c-Met-IN-2 is a potent, selective and orallyavailable c-Met inhibitor, with an IC of 0.650nM, with antitumor activity.c-Met-IN-9, a 4-phenoxypyridine derivative, is ac-Met kinas inhibitor with an IC of 12 nM.50c-Met-IN-9 induces cells apoptosis, and hasantitumor activi

25、ties.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/c-met-hdac-in-2.html c-Met/HDAC-IN-2 HYPERLINK https:/www.MedChemE/c-met-hdac-in-2.html HYPERLINK https:/www.MedChemE/Cabozantinib.htm

26、l CabozantinibCat. No.: HY-143462(XL184; BMS-907351) Cat. No.: HY-13016c-Met/HDAC-IN-2 is a highly potent c-Met andHDAC dual inhibitor with IC s of 18.49 nM and505.40 nM for HDAC1 and c-Met, respectively.c-Met/HDAC-IN-2 has antiproliferative activitiesagainst certain cancer cell lines.Cabozantinib i

27、s a potent multiple receptortyrosine kinases (RTKs) inhibitor that inhibitsVEGFR2, c-Met, Kit, Axl and Flt3 with IC s of500.035, 1.3, 4.6, 7 and 11.3 nM, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.96%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg,

28、50 mg, 100 mg, 200 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/cabozantinib-d4.html Cabozantinib-d4(XL184-d4; BMS-907351-d4) Cat. No.: HY-13016S1 HYPERLINK https:/www.MedChemE/cabozantinib-d6.html Cabozantinib-d6Cat. No.: HY-13016SCabozantinib-d4 is deuterium labeled Cabozantinib.Cabozantinib is

29、a potent multiple receptortyrosine kinases (RTKs) inhibitor that inhibitsVEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.Cabozantinib-d6 (XL184-d6) is the deuteriumlabeled Cabozantinib. Cabozantinib is a potentmultiple receptor tyrosine kinases (RTKs)inhibi

30、tor that inhibits VEGFR2, c-Met, Kit, Axland Flt3 with IC s of 0.035, 1.3, 4.6, 7 and 11.350nM, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.14%Clinical Data: No Development ReportedSize: 2.5 mg, 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/INCB28060.ht

31、ml Capmatinib(INC280; INCB28060) Cat. No.: HY-13404 HYPERLINK https:/www.MedChemE/CEP-40783.html CEP-40783(RXDX-106) Cat. No.: HY-100946Capmatinib (INC280; INCB28060) is a potent, orallyactive, selective, and ATP competitive c-Metkinase inhibitor (IC =0.13 nM).50CEP-40783 is a potent, selective and

32、orallyavailable inhibitor of AXL and c-Met with ICvalues of 7 nM and 12 nM, respectively.50Purity: 99.92%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mgPurity: 99.22%Clinical Data: Phase 1Size: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 200 mg, 500 mg, 1 g HYPERLINK https:/www.Me

33、dChemE/Crizotinib.html Crizotinib(PF-02341066) Cat. No.: HY-50878 HYPERLINK https:/www.MedChemE/Crizotinib-hydrochloride.html Crizotinib HYPERLINK https:/www.MedChemE/Crizotinib-hydrochloride.html HYPERLINK https:/www.MedChemE/Crizotinib-hydrochloride.html hydrochloride(PF-02341066 hydrochloride) Ca

34、t. No.: HY-50878ACrizotinib (PF-02341066) is an orallybioavailable, ATP-competitive ALK and c-Metinhibitor with IC s of 20 and 8 nM, respectively.50Crizotinib hydrochloride (PF-02341066hydrochloride) is an orally bioavailable,selective, and ATP-competitive dual ALK andc-Met inhibitor with IC s of 20

35、 and 8 nM,50respectively.Purity: 99.97%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mg, 500 mgPurity: 99.86%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg HYPERLINK https:/www.MedChemE/crizotinib-d5.html Crizotinib-d5 HYPERLINK https:/www.MedChemE

36、/crizotinib-d5.html HYPERLINK https:/www.MedChemE/TPX-022.html CSF1R-IN-2(PF-02341066-d5) Cat. No.: HY-50878SCat. No.: HY-111787Crizotinib-d5 (PF-02341066-d5) is the deuteriumlabeled Crizotinib. Crizotinib (PF-02341066) is anorally bioavailable, ATP-competitive ALK andc-Met inhibitor with IC s of 20

37、 and 8 nM,50respectively.CSF1R-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%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.97%Clinical Data: No Development ReportedS

38、ize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/ds-1205b-free-base.html DS-1205b HYPERLINK https:/www.MedChemE/ds-1205b-free-base.html HYPERLINK https:/www.MedChemE/ds-1205b-free-base.html free HYPERLINK https:/www.MedChemE/ds-1205b-free-base.html HYPERLINK https:/ww

39、w.MedChemE/ds-1205b-free-base.html base HYPERLINK https:/www.MedChemE/ds-1205b-free-base.html HYPERLINK https:/www.MedChemE/egfr-in-8.html EGFR-IN-8Cat. No.: HY-114357A Cat. No.: HY-126320DS-1205b free base is a potent and selectiveinhibitor of AXL kinase, with an IC of 1.3 nM.50DS-1205b free base a

40、lso inhibits MER, MET,and TRKA, with IC s of 63, 104, and 407 nM,50respectively. DS-1205b free base can inhibit cellmigration in vitro and tumor growth in vivo.Purity: 99.92%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mgEGFR-IN-8 is a dual EGFR and c-Met inhibitor,compound 48.

41、 EGFR-IN-8 can be a promisingcandidate for further development to target EGFRTKI-resistant NSCLC.Purity: 98.31%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/X-396.html Ensarti

42、nib(X-396) Cat. No.: HY-103714 HYPERLINK https:/www.MedChemE/X-396_hydrochloride.html Ensartinib HYPERLINK https:/www.MedChemE/X-396_hydrochloride.html HYPERLINK https:/www.MedChemE/X-396_hydrochloride.html dihydrochloride(X-396 dihydrochloride) Cat. No.: HY-103714AEnsartinib (X-396) is a potent and

43、 dualALK/MET inhibitor with IC s of 0.4 nM and500.74 nM, respectively.Ensartinib dihydrochloride (X-396 dihydrochloride)is a potent and dual ALK/MET inhibitor withIC s of 98%Clinical Data: LaunchedSize: 1 mg, 5 mgPurity: 99.46%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 m

44、g HYPERLINK https:/www.MedChemE/Foretinib.html Foretinib(XL880; GSK1363089; GSK089; EXEL-2880) Cat. No.: HY-10338 HYPERLINK https:/www.MedChemE/fosgonimeton.html Fosgonimeton(ATH-1017) Cat. No.: HY-132814Foretinib is a multi-target tyrosine kinaseinhibitor with IC s of 0.4 nM and 0.9 nM for50Met and

45、 KDR.Fosgonimeton (ATH-1017) is a hepatocyte growthfactor receptor agonist (WO2017210489).Purity: 99.77%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/gemnelatinib.html GemnelatinibCat.

46、 No.: HY-132816 HYPERLINK https:/www.MedChemE/glesatinib.html Glesatinib(MGCD265) Cat. No.: HY-19642Gemnelatinib is a tyrosine kinase inhibitor(WO2018077227, implementation example 1).Gemnelatinib can be used for the research ofcancer.Glesatinib (MGCD265) is an orally active, potentMET/SMO dual inhi

47、bitor. Glesatinib, a tyrosinekinase inhibitor, antagonizes P-glycoprotein(P-gp) mediated multidrug resistance (MDR) innon-small cell lung cancer (NSCLC).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:

48、/www.MedChemE/Glesatinib-hydrochloride.html Glesatinib HYPERLINK https:/www.MedChemE/Glesatinib-hydrochloride.html HYPERLINK https:/www.MedChemE/Glesatinib-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/Glesatinib-hydrochloride.html HYPERLINK https:/www.MedChemE/glumetinib.html Glume

49、tinib(MGCD265 hydrochloride) Cat. No.: HY-19642A (SCC244) Cat. No.: HY-116000Glesatinib hydrochloride (MGCD265 hydrochloride)is an orally active, potent MET/SMO dualinhibitor. Glesatinib hydrochloride, a tyrosinekinase inhibitor, antagonizes P-glycoprotein(P-gp) mediated multidrug resistance (MDR) i

50、nnon-small cell lung cancer (NSCLC).Glumetinib (SCC244) is a highly selective, orallybioavailable, ATP-competitive c-Met inhibitorwith an IC of 0.42 nM.50Purity: 98.25%Clinical Data: Phase 2Size: 10 mM 1 mL, 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.15%Clinical Data: Phase 2Size: 10 mM 1 mL,

51、 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/e-7050.html Golvatinib HYPERLINK https:/www.MedChemE/e-7050.html HYPERLINK https:/www.MedChemE/JNJ-38877605.html JNJ-38877605(E-7050) Cat. No.: HY-13068Cat. No.: HY-50683Golvatinib (E-7050) is a potent dual inhibitor ofboth c-Met and VEGFR2 k

52、inases with IC s of 1450and 16 nM, respectively.JNJ-38877605 is an ATP-competitive inhibitor ofc-Met with IC50 of 4 nM, 600-fold selective forc-Met than 200 other tyrosine and serine-threoninekinases.Purity: 99.89%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.95%Clinic

53、al Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgwww.MedChemE 5 HYPERLINK https:/www.MedChemE/JNJ-38877618.html JNJ-38877618 HYPERLINK https:/www.MedChemE/JNJ-38877618.html HYPERLINK https:/www.MedChemE/meleagrin.html MeleagrinCat. No.: HY-111050 Cat. No.: HY-N6797JNJ-38877618 is a potent

54、, highly selective, orallybioavailable Met kinase inhibitor with IC s of502 and 3 nM for wild type and mutant Met,respectively.Meleagrin is a roquefortine C-derived alkaloidproduced by fungi of the genus Penicillium andhas antimicrobial and anti-proliferativeactivities. Meleagrin is a class of FabI

55、inhibitor.Purity: 98.26%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/LY2801653.html Merestinib(LY2801653) Cat. No.: HY-15514 HYPERLINK https:/www.MedChe

56、mE/LY2801653-dihydrochloride.html Merestinib HYPERLINK https:/www.MedChemE/LY2801653-dihydrochloride.html HYPERLINK https:/www.MedChemE/LY2801653-dihydrochloride.html dihydrochloride(LY2801653 dihydrochloride) Cat. No.: HY-15514AMerestinib (LY2801653) is a potent, orallybioavailable c-Met inhibitor

57、(K=2 nM) withianti-tumor activities.Merestinib dihydrochloride (LY2801653dihydrochloride) is a potent, orally bioavailablec-Met inhibitor (K=2 nM) with anti-tumoriactivities.Purity: 99.99%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.36%Clinical Data: Phase 2Size: 10 m

58、M 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/met-kinase-in-2.html MET HYPERLINK https:/www.MedChemE/met-kinase-in-2.html HYPERLINK https:/www.MedChemE/met-kinase-in-2.html kinase-IN-2 HYPERLINK https:/www.MedChemE/met-kinase-in-2.html HYPERLINK https:/www.MedChemE/MGCD-265-analog

59、.html MGCD-265 HYPERLINK https:/www.MedChemE/MGCD-265-analog.html HYPERLINK https:/www.MedChemE/MGCD-265-analog.html analogCat. No.: HY-131065 Cat. No.: HY-10991MET kinase-IN-2 is a potent, selective, orallybioavailable MET kinase inhibitor with an IC50of 7.4 nM. MET kinase-IN-2 has antitumor activi

60、ty.MGCD-265 analog is a potent and oral activeinhibitor of c-Met and VEGFR2 tyrosinekinases, with IC s of 29 nM and 10 nM,50respectively. MGCD-265 analog has significantantitumor activity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.57%Clinical Data: Phase 2Size: 10 mM