Trk-Receptor-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Trk Receptor.html Trk HYPERLINK https:/www.MedChemE/Targets/Trk Receptor.html HYPERLINK https:/www.MedChemE/Targets/Trk Receptor.html ReceptorTropomyosin related kinase receptorTrk receptors are a family of three receptor tyrosine kinases (TrkA, TrkB, and TrkC)

2、, each of which can be activated by one or more of four neurotrophins-nerve growth factor (NGF), brain-derived neurotrophic factor (BDNF), and neurotrophins 3 and 4 (NT3 andNT4).TrkA, TrkB, and TrkC are transmembrane proteins that comprise the TRK receptor family. These receptor tyrosine kinases are

3、expressed in human neuronal tissue, and play an essential role in both the physiology of development and function of the nervoussystem through activation by neurotrophins (NTs). The latter are specific ligands known as NGF for TrkA, BDGF, and NT-4/5 for TrkBand NT3 for TrkC, respectively.The binding

4、 of the ligand to the receptor triggers the oligomerisation of the receptors and phosphorylation of specific tyrosineresidues in the intracytoplasmic kinase domain. This event results into the activation of signal transduction pathways leading toproliferation, differentiation and survival in normal

5、and neoplastic neuronal cells.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Trk Receptor.html Trk HYPERLINK https:/www.MedChemE/Targets/Trk Receptor.html HYPERLINK https:/www.MedChemE/Targets/Trk Receptor.html Receptor HYPERLINK https:/www.MedChemE/Targets/Trk Receptor.html HYPERLINK https:/w

6、ww.MedChemE/Targets/Trk Receptor.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/Trk Receptor.html HYPERLINK https:/www.MedChemE/Targets/Trk Receptor.html Agonists, HYPERLINK https:/www.MedChemE/Targets/Trk Receptor.html HYPERLINK https:/www.MedChemE/Targets/Trk Receptor.html Activators HYPER

7、LINK https:/www.MedChemE/Targets/Trk Receptor.html HYPERLINK https:/www.MedChemE/Targets/Trk Receptor.html & HYPERLINK https:/www.MedChemE/Targets/Trk Receptor.html HYPERLINK https:/www.MedChemE/Targets/Trk Receptor.html Antagonists HYPERLINK https:/www.MedChemE/r-larotrectinib.html (R)-Larotrectini

8、b(R)-LOXO-101; (R)-ARRY-470) Cat. No.: HY-12866B HYPERLINK https:/www.MedChemE/7,8-Dihydroxyflavone.html 7,8-DihydroxyflavoneCat. No.: HY-W013372(R)-Larotrectinib is a potent TRK inhibitor withan IC value of 28.5 nM for TrkA.50(R)-Larotrectinib can be used for researchingcancer, inflammatory and cer

9、tain infectiousdiseases.7,8-Dihydroxyflavone is a potent and selectiveTrkB agonist that mimics the physiologicalactions of Brain-derived neurotrophic factor(BDNF). Displays therapeutic efficacy towardvarious neurological diseases.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurit

10、y: 99.90%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 50 mg HYPERLINK https:/www.MedChemE/Altiratinib.html Altiratinib(DCC-2701) Cat. No.: HY-B0791 HYPERLINK https:/www.MedChemE/amitriptyline-hydrochloride.html Amitriptyline HYPERLINK https:/www.MedChemE/amitriptyline-hydrochloride.html H

11、YPERLINK https:/www.MedChemE/amitriptyline-hydrochloride.html hydrochlorideCat. No.: HY-B0527AAltiratinib (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, Trk2, and Trk3 respectively.Amitriptyline hydrochloride is an

12、inhibitor ofserotonin reuptake transporter (SERT) andnoradrenaline reuptake transporter (NET), with Ksiof 3.45 nM and 13.3 nM for human SERT and NET,respectively.Purity: 98.06%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.56%Clinical Data: LaunchedSize: 10 mM 1 mL, 500

13、 mg, 1 g, 5 g HYPERLINK https:/www.MedChemE/amitriptyline-d3-hydrochloride.html Amitriptyline-d3 HYPERLINK https:/www.MedChemE/amitriptyline-d3-hydrochloride.html HYPERLINK https:/www.MedChemE/amitriptyline-d3-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/amitriptyline-d3-hydrochlor

14、ide.html HYPERLINK https:/www.MedChemE/amitriptyline-d6-hydrochloride.html Amitriptyline-d6 HYPERLINK https:/www.MedChemE/amitriptyline-d6-hydrochloride.html HYPERLINK https:/www.MedChemE/amitriptyline-d6-hydrochloride.html hydrochlorideCat. No.: HY-135096 Cat. No.: HY-B0527ASAmitriptyline-d3 hydroc

15、hloride is the deuteriumlabeled Amitriptyline (hydrochloride).Amitriptyline-d6 hydrochloride is the deuteriumlabeled Amitriptyline hydrochloride.Purity: 98%Clinical Data: No Development ReportedSize: 2.5 mg, 1 mg, 5 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 2.5 mg, 1 mg, 5 mg,

16、25 mg HYPERLINK https:/www.MedChemE/ANA-12.html ANA-12 HYPERLINK https:/www.MedChemE/ANA-12.html HYPERLINK https:/www.MedChemE/AZ-23.html AZ-23Cat. No.: HY-12497(AZ23; AZ 23) Cat. No.: HY-15590ANA-12 is a potent and selective TrkB antagonistwith IC s of 45.6 nM and 41.1 M for the high and50low affin

17、ity sites, respectively.AZ-23 is an ATP-competitive and orallybioavailable Trk kinase A/B/C inhibitor withIC s of 2 nM (TrkA), 8 nM (TrkB), 24 nM (FGFR1),5052 nM (Flt3), 55 nM (Ret), 84 nM (MuSk), 99 nM(Lck), respectively.Purity: 99.91%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 5

18、0 mgPurity: 98.57%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Belizatinib.html Belizatinib HYPERLINK https:/www.MedChemE/Belizatinib.html HYPERLINK https:/www.MedChemE/CE-245677.html CE-245677(TSR-011) Cat. No.: HY-17603Cat.

19、 No.: HY-112423Belizatinib is an oral, dual, potent inhibitor ofALK and TRKA, TRKB, and TRKC, with IC of 0.7nM50for wild-type recombinant ALK kinase.CE-245677 is a potent reversible inhibitor of Tie2and TrkA/B kinases with a cellular IC s of 4.750and 1 nM.Purity: 99.66%Clinical Data: Phase 2Size: 10

20、 mM 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.72%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/CH7057288.html CH7057288 HYPERLINK https:/www.MedChemE/CH7057288.h

21、tml HYPERLINK https:/www.MedChemE/cyclotraxin-b.html Cyclotraxin HYPERLINK https:/www.MedChemE/cyclotraxin-b.html HYPERLINK https:/www.MedChemE/cyclotraxin-b.html BCat. No.: HY-107362 Cat. No.: HY-P1178CH7057288 is a potent and selective TRKinhibitor.Cyclotraxin B, a cyclic peptide, is a highlypoten

22、t and selective TrkB inhibitor withoutaltering the binding of BDNF. Cyclotraxin Bnon-competitively inhibits BDNF-induced TrkBactivity with an IC of 0.30 nM.50Purity: 98.68%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.87%Clinical Data: No Develop

23、ment ReportedSize: 1 mg, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/cyclotraxin-b-tfa.html Cyclotraxin HYPERLINK https:/www.MedChemE/cyclotraxin-b-tfa.html HYPERLINK https:/www.MedChemE/cyclotraxin-b-tfa.html B HYPERLINK https:/www.MedChemE/cyclotraxin-b-tfa.html HYPERLINK https:/www.MedChemE/cyclotr

24、axin-b-tfa.html TFA HYPERLINK https:/www.MedChemE/cyclotraxin-b-tfa.html HYPERLINK https:/www.MedChemE/d5261.html D5261Cat. No.: HY-P1178A Cat. No.: HY-144690Cyclotraxin B TFA, a cyclic peptide, is a highlypotent and selective TrkB inhibitor withoutaltering the binding of BDNF. Cyclotraxin B TFAnon-

25、competitively inhibits BDNF-induced TrkBactivity with an IC of 0.30 nM.50D5261 is a potent, type III allosterictropomyosin-related kinase A (TrkA) inhibitor.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK ht

26、tps:/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:/www.MedChemE/ds-1205b-free-base.html baseCat. No.: HY-114357A HYP

27、ERLINK https:/www.MedChemE/Entrectinib.html Entrectinib(NMS-E628; RXDX-101) Cat. No.: HY-12678DS-1205b free base is a potent and selectiveinhibitor of AXL kinase, with an IC of 1.3 nM.50DS-1205b free base also inhibits MER, MET,and TRKA, with IC s of 63, 104, and 407 nM,50respectively. DS-1205b free

28、 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 mgEntrectinib (NMS-E628) is a potent, orallyavailable, and CNS-active pan-Trk, ROS1, andALK inhibitor. Entrectinib inhibits TrkA, TrkB,TrkC, ROS1 and ALK

29、 with IC values of 1, 3, 5, 1250and 7 nM, respectively. Antitumor activity.Purity: 99.32%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/flt3-trka-in-1.html FLT3/TrKA-IN-1 HYPERLINK https:/www.MedChemE/flt3-trka-in-1.html HYPERLINK https:/www.MedChem

30、E/GNF-5837.html GNF-5837Cat. No.: HY-146749 Cat. No.: HY-13491FLT3/TrKA-IN-1 is a potent FLT3/TrKA dual kinaseinhibitor with the IC s of 43.8 nM, 97.2 nM, 92.550nM and 23.6 nM for FLT3, FLT3-ITD, FLT3-TKD andTrKA, respectively.GNF-5837 is a potent, selective, and orallybioavailable pan-tropomyosin r

31、eceptor kinase(TRK) inhibitor which display antiproliferativeeffects in cellular Ba/F3 assays ( IC values of507 nM, 9 nM and 11 nM for cells containing thefusion proteins Tel-TrkC, Tel-TrkB andPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.45%Clinical Data: No Developmen

32、t ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/gnf-8625-monopyridin-n-piperazine-hydrochloride.html GNF-8625 HYPERLINK https:/www.MedChemE/gnf-8625-monopyridin-n-piperazine-hydrochloride.html HYPERLINK https:/www.MedChemE/gnf-8625-monopyridin-n-piperazine

33、-hydrochloride.html monopyridin-N-piperazine HYPERLINK https:/www.MedChemE/gnf-8625-monopyridin-n-piperazine-hydrochloride.html HYPERLINK https:/www.MedChemE/gnf-8625-monopyridin-n-piperazine-hydrochloride.html hydrochloride HYPERLINK https:/www.MedChemE/gnf-8625-monopyridin-n-piperazine-hydrochlori

34、de.html HYPERLINK https:/www.MedChemE/GW-441756.html GW HYPERLINK https:/www.MedChemE/GW-441756.html HYPERLINK https:/www.MedChemE/GW-441756.html 441756Cat. No.: HY-131706A Cat. No.: HY-18314GNF-8625 monopyridin-N-piperazine hydrochloride(TRKi-2), a TRK inhibitor, which is from thepatent WO 20200384

35、15 A1.GW 441756 is a potent and specific nerve growthfactor (NGF) receptor tyrosine kinases A (TrkA)inhibitor (IC =2 nM), which eliminates the BmK50NSPK-induced neurite outgrowth.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.65%Clinical Data: No Development ReportedSize

36、: 10 mM 1 mL, 10 mg, 50 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/htrka-in-1.html hTrkA-IN-1 HYPERLINK https:/www.MedChemE/htrka-in-1.html HYPERLINK https:/www.MedChemE/ihmt-trk-284.html IHMT-TRK-284Cat. No.: HY-136535 Cat. No.: HY-146697hTrkA-IN-1 is a potent and orally active inhibitorof TrkA

37、 kinase with an IC of 1.3 nM, compound 2.50extracted from patent WO2015175788. hTrkA-IN-1 canbe used for the study of inflammatory disease,such as prostatitis, pelvic, et al.IHMT-TRK-284 (Compound 34) is a potent, orallyactive type II TRK kinase inhibitor with IC50values of 10.5, 0.7, and 2.6 nM to

38、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.MedChemE/k-252a.html K

39、-252a(SF2370; Antibiotic K 252a; Antibiotic SF 2370) Cat. No.: HY-N6732 HYPERLINK https:/www.MedChemE/LOXO-101.html Larotrectinib(LOXO-101; ARRY-470) Cat. No.: HY-12866K-252a, a staurosporine analog, inhibits proteinkinase, with IC values of 470 nM, 140 nM, 270 nM,50and 1.7 nM for PKC, PKA,Ca2+/calm

40、odulin-dependent kinase type II, andphosphorylase kinase, respectively.Larotrectinib (LOXO-101) is an ATP-competitiveoral, selective inhibitor of thetropomyosin-related kinase (TRK) familyreceptors, with low nanomolar 50% inhibitoryconcentrations against all three isoforms (TRKA,B, and C).Purity: 99

41、.45%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg, 5 mgPurity: 99.93%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/LOXO-101-sulfate.html Larotrectinib HYPERLINK https:/www.MedChemE/LOXO-101-sulfate.html HYPERLINK https:/www.MedChemE/

42、LOXO-101-sulfate.html sulfate(LOXO-101 sulfate; ARRY-470 sulfate) Cat. No.: HY-12866A HYPERLINK https:/www.MedChemE/larotrectinib-d7.html Larotrectinib-d7(LOXO-101-d7; ARRY-470-d7) Cat. No.: HY-12866SLarotrectinib sulfate (LOXO-101 sulfate; ARRY-470sulfate) is an ATP-competitive oral, selectiveinhib

43、itor of the tropomyosin-related kinase (TRK)family receptors, with low nanomolar 50%inhibitory concentrations against all threeisoforms (TRKA, B, and C).Larotrectinib-d7 (LOXO-101-d7) is the deuteriumlabeled Larotrectinib.Purity: 99.57%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100

44、 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Lestaurtinib.html Lestaurtinib HYPERLINK https:/www.MedChemE/Lestaurtinib.html HYPERLINK https:/www.MedChemE/LM22A-4.html LM22A-4(CEP-701; KT-5555) Cat. No.: HY-50867Cat. No.: HY-100673Lestaurtinib (CE

45、P-701;KT-5555) is anATP-competitive multi-kinase inhibitor with potentactivity against the Trk family of receptortyrosine kinases. Lestaurtinib inhibits JAK2,FLT3 and TrkA with IC s of 0.9, 3 and less than5025 nM, respectively.LM22A-4 is a specific agonist of tyrosine kinasereceptor B, used for neur

46、ological diseaseresearch.Purity: 99.92%Clinical Data: Phase 3Size: 5 mgPurity: 98.0%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/LM22B-10.html LM22B-10 HYPERLINK https:/www.MedChemE/LM22B-10.html HYPERLINK https:/www.MedChemE

47、/lpm4870108.html LPM4870108Cat. No.: HY-104047 Cat. No.: HY-132229LM22B-10 is an activator of TrkB/TrkCneurotrophin receptor, and can induce TrkB,TrkC, AKT and ERK activation in vitro and invivo.Purity: 99.72%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg, 100 mgLPM

48、4870108 is a potent and orally active pan-Trk(WT and MT) inhibitor, with IC s of 0.2 nM,502.4 nM, 3.5 nM and 2.3 nM for TrkC, TrkA,TrkAG595R and TrkAG667C, respectively.LPM4870108 shows selectivity for Trk over ALK(IC =182 nM).50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg4 Tel:

49、 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/N-Acetyl-5-hydroxytryptamine.html N-Acetyl-5-hydroxytryptamine(N-Acetylserotonin; Normelatonin; O-Demethylmelatonin) Cat. No.: HY-107854 HYPERLINK https:/www.MedChemE/n-acetyl-5-hydroxytryptamine-d3.html N-Acetyl-5-hy

50、droxytryptamine-d3 HYPERLINK https:/www.MedChemE/n-acetyl-5-hydroxytryptamine-d3.html (N-Acetylserotonin-d3;Normelatonin-d3; O-Demethylmelatonin-d3) Cat. No.: HY-107854SN-Acetyl-5-hydroxytryptamine is a Melatoninprecursor, and that it can potently activate TrkBreceptor.N-Acetyl-5-hydroxytryptamine-d

51、3(N-Acetylserotonin-d3) is the deuterium labeledN-Acetyl-5-hydroxytryptamine.N-Acetyl-5-hydroxytryptamine is a Melatoninprecursor, and that it can potently activate TrkBreceptor.Purity: 99.90%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 50 mgPurity: 98%Clinical Data: No Development Report

52、edSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ono-7475.html ONO-7475 HYPERLINK https:/www.MedChemE/ono-7475.html HYPERLINK https:/www.MedChemE/paltimatrectinib.html PaltimatrectinibCat. No.: HY-114358 Cat. No.: HY-145587ONO-7475 is a potent, selective, and orally activeAxl/Mer inhibitor with IC v

53、alues of 0.7 nM50and 1.0 nM, respectively. ONO-7475 sensitizesAXL-overexpressing EGFR-mutant NSCLC cells tothe EGFR-TKIs, suppresses the emergence andmaintenance of tolerant cells.Paltimatrectinib (compound I-147) is a potenttyrosine kinase inhibitor with an IC of 98%Clinical Data: No Development Re

54、portedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/pan-trk-in-2.html Pan-Trk-IN-2 HYPERLINK https:/www.MedChemE/pan-trk-in-2.html HYPERLINK https:/www.MedChemE/pan-trk-in-3.html Pan-Trk-IN-3Cat. No.: HY-144028 Cat. No.: HY-144069Compound cpd-1 is a small molecule Trks inhibitorwith good antitumor

55、activity.Pan-Trk-IN-3 (Compound 11g) is a potent inhibitorof pan-Trk and their drug-resistant mutants withIC values of 2, 3, 2, 21, 26, 5, 7 and 6 nM50against TrkA, TrkB, TrkC, TrkAG595R,TrkAG667C, TrkAG667S, TrkAF589L andTrkCG623R, respectively.Purity: 98%Clinical Data: No Development ReportedSize:

56、 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/pf-06273340.html PF-06273340 HYPERLINK https:/www.MedChemE/pf-06273340.html HYPERLINK https:/www.MedChemE/Trk-IN-3.html PF-06733804Cat. No.: HY-122616 Cat. No.: HY-112434PF-06273340 is a potent

57、, selective, orallybioavailable and peripherally restricted pan Trkinhibitor.PF-06733804 is a potent pan-Trk inhibitor incell-based assays with IC s of 8.4 nM, 6.2 nM and502.2 nM for TrkA, TrkB and TrkC, respectively.Anti-hyperalgesic effect.Purity: 98%Clinical Data: No Development ReportedSize: 1 m

58、g, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Trk-IN-5.html PF-06737007 HYPERLINK https:/www.MedChemE/Trk-IN-5.html HYPERLINK https:/www.MedChemE/Trk-IN-4.html PF-6683324Cat. No.: HY-112437(Trk-IN-4) Cat. No.: HY-112436PF-06737007 is a potent

59、pan-Trk inhibitor incell-based assays with IC s of 7.7 nM, 15 nM and503.9 nM for TrkA, TrkB and TrkC, respectively.Anti-hyperalgesic effect.PF-6683324 (Trk-IN-4) is a potent pan-Trkinhibitor in cell-based assays with IC s of 1.950nM, 2.6 nM and 1.1 nM for TrkA, TrkB and TrkC,respectively. Anti-hyper

60、algesic effect.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgwww.MedChemE 5 HYPERLINK https:/www.MedChemE/TPX-0005.html Repotrectinib(TPX-0005) Cat. No.: HY-103022 HYPERLINK https:/www.MedChemE