ROS-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/ROS.html ROSThe transmembrane proto-oncogene receptor tyrosine kinase (RTK) ROS is one of the last two remaining orphan receptor tyrosinekinases. Its normal expression pattern is tightly spatiotemporally restricted during development. The ectopic expression, as

2、 well asthe production of variable mutant forms of ROS kinase, has been reported in a number of cancers, such as glioblastomamultiforme, and non-small cell lung cancer, suggesting a role for ROS kinase in deriving such tumors. It is thought also that thec-ROS gene may have a role in some cardiovascu

3、lar diseases, and the fact that homozygous male mice targeted against the c-ROSgene are healthy but infertile has inspired researchers to think about ROS inhibition as a method for the development of new malecontraceptives.ROS1 is a transmembrane receptor tyrosine kinase proto-oncogene that has been

4、 shown to have rearrangements with severalgenes in glioblastoma, non-small-cell lung cancer (NSCLC), and other neoplasms, including intrachromosomal fusion with GOPCdue to microdeletions at 6q22.1. ROS1 fusion events are important findings in these tumors, as they are potentially targetablealteratio

5、ns with newer tyrosine kinase inhibitors.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/ROS.html ROS HYPERLINK https:/www.MedChemE/Targets/ROS.html HYPERLINK https:/www.MedChemE/Targets/ROS.html Inhibitors, HYPERLINK https:/www.MedChemE/Targets/ROS.html HYPERLINK https:/www.MedChemE/Targets/RO

6、S.html Activators, HYPERLINK https:/www.MedChemE/Targets/ROS.html HYPERLINK https:/www.MedChemE/Targets/ROS.html Modulators HYPERLINK https:/www.MedChemE/Targets/ROS.html HYPERLINK https:/www.MedChemE/Targets/ROS.html & HYPERLINK https:/www.MedChemE/Targets/ROS.html HYPERLINK https:/www.MedChemE/Tar

7、gets/ROS.html Inducers HYPERLINK https:/www.MedChemE/alk-ros1-in-1.html ALK/ROS1-IN-1 HYPERLINK https:/www.MedChemE/alk-ros1-in-1.html HYPERLINK https:/www.MedChemE/antibacterial-agent-69.html Antibacterial HYPERLINK https:/www.MedChemE/antibacterial-agent-69.html HYPERLINK https:/www.MedChemE/antib

8、acterial-agent-69.html agent HYPERLINK https:/www.MedChemE/antibacterial-agent-69.html HYPERLINK https:/www.MedChemE/antibacterial-agent-69.html 69Cat. No.: HY-130794 Cat. No.: HY-144252ALK/ROS1-IN-1 (compound 2e) is a potent andselective anti crizotinib-resistant ALK/ROS1 dualinhibitor, with IC s o

9、f 0.174 M and 0.530 M for50ALK and ROS1 enzyme, respectively.Antimicrobial agent 69 is a novel structuralantimicrobial regulator and has been used to fightdeadly multidrug-resistant bacterial infections,and its MICs value is2.978 M.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPur

10、ity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/antibacterial-agent-70.html Antibacterial HYPERLINK https:/www.MedChemE/antibacterial-agent-70.html HYPERLINK https:/www.MedChemE/antibacterial-agent-70.html agent HYPERLINK https:/www.MedChemE/antibacterial

11、-agent-70.html HYPERLINK https:/www.MedChemE/antibacterial-agent-70.html 70 HYPERLINK https:/www.MedChemE/antibacterial-agent-70.html HYPERLINK https:/www.MedChemE/anticancer-agent-15.html Anticancer HYPERLINK https:/www.MedChemE/anticancer-agent-15.html HYPERLINK https:/www.MedChemE/anticancer-agen

12、t-15.html agent HYPERLINK https:/www.MedChemE/anticancer-agent-15.html HYPERLINK https:/www.MedChemE/anticancer-agent-15.html 15Cat. No.: HY-144255 Cat. No.: HY-139860Antibacterial agent 70 is a newdihydropyrimidinone imidazole hybrid antibacterialagent, and its MIC valueis 0.5 g/mL.Anticancer agent

13、 15 is capable of significantlyincreasing the cellular level of ROS and inducingmelanoma cancer cell death via necroptosis.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/anticancer-agent

14、-42.html Anticancer HYPERLINK https:/www.MedChemE/anticancer-agent-42.html HYPERLINK https:/www.MedChemE/anticancer-agent-42.html agent HYPERLINK https:/www.MedChemE/anticancer-agent-42.html HYPERLINK https:/www.MedChemE/anticancer-agent-42.html 42 HYPERLINK https:/www.MedChemE/anticancer-agent-42.h

15、tml HYPERLINK https:/www.MedChemE/antitumor-agent-55.html Antitumor HYPERLINK https:/www.MedChemE/antitumor-agent-55.html HYPERLINK https:/www.MedChemE/antitumor-agent-55.html agent-55Cat. No.: HY-146516 Cat. No.: HY-146038Anticancer agent 42 (compound 10d) is an orallyactive anticancer agent, and s

16、hows a potentantitumor activity against MDA-MB-231 cell with anIC of 0.07 M. Anticancer agent 42 can exert its50anticancer activity by activating apoptoticpathway and p53 expression.Antitumor agent-55 (compound 5q) is a potentantitumor agent. Antitumor agent-55 effectivelyinhibits PC3, with an IC of

17、 0.91 M. Antitumor50agent-55 effectively inhibits the colonyformation, suppresses the cell migration in PC3.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/apogossypolone.html Apogossypol

18、one HYPERLINK https:/www.MedChemE/apogossypolone.html HYPERLINK https:/www.MedChemE/capillarisin.html Capillarisin(ApoG2) Cat. No.: HY-19551Cat. No.: HY-121192Apogossypolone (ApoG2) is an orally active Bcl-2family proteins inhibitor with K values of 35, 25iand 660 nM for Bcl-2, Mcl-1 and Bcl-X ,Lres

19、pectively. Apogossypolone shows antitumoractivities, induces cell apoptosis and autophagy.Apogossypolone also has antifungal activity.Capillarisin, as a constituent from ArtemisiaeCapillaris herba, is found to exertanti-inflammatory and antioxidant properties.Purity: 98%Clinical Data: No Development

20、 ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg HYPERLINK https:/www.MedChemE/capsanthin.html Capsanthin HYPERLINK https:/www.MedChemE/capsanthin.html HYPERLINK https:/www.MedChemE/chol-ctpp.html Chol-CTPPCat. No.: HY-125711 Cat. No.: HY-144825Capsa

21、nthin is a carotenoid that has been found inC. annuum. Capsanthin has antioxidantantitumorand anti-inflammatory effects.Chol-CTPP is a ligand with dual targeting effecton blood-brain barrier (BBB) and glioma cells.Lip-CTPP can be gained by Chol-CTPP and anothermitochondria targeting ligand (Chol-TPP

22、).Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/cinnamtannin-b-1.html Cinnamtannin HYPERLINK https:/www.MedChemE/cinnamtannin-b

23、-1.html HYPERLINK https:/www.MedChemE/cinnamtannin-b-1.html B-1Cat. No.: HY-130237 HYPERLINK https:/www.MedChemE/Crizotinib.html Crizotinib(PF-02341066) Cat. No.: HY-50878Cinnamtannin B-1 is a proanthocyanidin withmultiple biological functions, includingantioxidant effects. Cinnamtannin B-1 inhibits

24、RANKL-induced osteoclastogenesis and preventsovariectomy-induced osteoporosis in vivo.Crizotinib (PF-02341066) is an orallybioavailable, ATP-competitive ALK and c-Metinhibitor with IC s of 20 and 8 nM, respectively.50Purity: 95.0%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 9

25、9.97%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mg, 500 mg 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

26、hydrochloride) Cat. No.: HY-50878A HYPERLINK https:/www.MedChemE/crizotinib-d5.html Crizotinib-d5(PF-02341066-d5) Cat. No.: HY-50878SCrizotinib hydrochloride (PF-02341066hydrochloride) is an orally bioavailable,selective, and ATP-competitive dual ALK andc-Met inhibitor with IC s of 20 and 8 nM,50res

27、pectively.Crizotinib-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 and 8 nM,50respectively.Purity: 99.86%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mg, 500 mgPu

28、rity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/derrone.html DerroneCat. No.: HY-N3737 HYPERLINK https:/www.MedChemE/Entrectinib.html Entrectinib(NMS-E628; RXDX-101) Cat. No.: HY-12678Derrone, a prenylated isoflavones, is an Aurorakinase inhibitor, with

29、IC values of 6 and 22.3 M50against Aurora B and Aurora A, respectively.Derrone shows anti-tumor activity.Entrectinib (NMS-E628) is a potent, orallyavailable, and CNS-active pan-Trk, ROS1, andALK inhibitor. Entrectinib inhibits TrkA, TrkB,TrkC, ROS1 and ALK with IC values of 1, 3, 5, 1250and 7 nM, re

30、spectively. Antitumor activity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.32%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/f-1.html F-1 HYPERLINK https:/www.MedChemE/f-1.html HYPERLINK https:/www.MedChemE/fascaplysi

31、n.html FascaplysinCat. No.: HY-112801 Cat. No.: HY-112328F-1 is a potent ALK and ROS1 dual inhibitor,suppresses phospho-ALK and its relative downstreamsignaling pathways, with IC s of 2.1 nM, 2.3 nM,501.3 nM and 3.9 nM for ALKWT, ROS1WT,ALKL1196M and ALKG1202R, respectively.Fascaplysin is an antimic

32、robial and cytotoxic redpigment, that can come from the marine sponge(Fascaplysinopsis sp.). Fascaplysin has beensynthesized in seven steps from indole (65%yield).Purity: 98.65%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development Repor

33、tedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ggti-2154.html GGTI-2154 HYPERLINK https:/www.MedChemE/ggti-2154.html HYPERLINK https:/www.MedChemE/ggti-2154-hydrochloride.html GGTI-2154 HYPERLINK https:/www.MedChemE/ggti-2154-hydrochloride.html HYPERLINK https:/www.MedChemE/ggti-2154-hydrochlorid

34、e.html hydrochlorideCat. No.: HY-16229 Cat. No.: HY-16229AGGTI-2154 is a potent and selective inhibitor ofgeranylgeranyltransferase I (GGTase I), with an ICof 21 nM. GGTI-2154 shows more than 200-foldselectivity for GGTase I over FTase (IC50=5600nM). GGTI-2154 can be used for the research ofcancer.5

35、0GGTI-2154 hydrochloride is a potent and selectiveinhibitor geranylgeranyltransferase I (GGTase I),with an IC of 21 nM. GGTI-2154 hydrochloride50shows more than 200-fold selectivity for GGTase Iover FTase (IC50=5600 nM). GGTI-2154 hydrochloridecan be used for the research of cancer.Purity: 98%Clinic

36、al Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.13%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/ggti-2418.html GGTI-2418Cat. No.: HY-16231 HYPERLINK https:/www.MedChemE/iruplinalkib.html Ir

37、uplinalkib(WX-0593) Cat. No.: HY-145574GGTI-2418 is a highly potent, competitive, andselective geranylgeranyltransferase I (GGTase I)inhibitor. GGTI-2418 inhibits GGTase I and FTaseactivities with IC s of 9.5 nM and 53 M,50respectively.Iruplinalkib (WX-0593) is a potent, selective, andorally active

38、inhibitor of ALK and ROS1 tyrosinekinase. Iruplinalkib (WX-0593) shows favorablesafety and promising antitumor activity inadvanced NSCLC with ALK or ROS1 rearrangement.Purity: 98.04%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development Repo

39、rtedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/PF-06463922.html Lorlatinib(PF-06463922) Cat. No.: HY-12215 HYPERLINK https:/www.MedChemE/lorlatinib-13c-d3.html Lorlatinib-13C,d3(PF-06463922-13C,d3) Cat. No.: HY-12215SLorlatinib (PF-06463922) is a selective, orallyactive, brain-penetrant and ATP-

40、competitiveROS1/ALK inhibitor. Lorlatinib has Ks ofi0.025 nM, 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/malvidin-3-galactoside-chloride.html Malvidin-3-galactoside HYPERLINK https:/www.MedChemE/malvidin-3-galactoside-chloride.html HYPERLINK https:/www.Me

41、dChemE/malvidin-3-galactoside-chloride.html chloride HYPERLINK https:/www.MedChemE/malvidin-3-galactoside-chloride.html HYPERLINK https:/www.MedChemE/mao-b-in-7.html MAO-B-IN-7Cat. No.: HY-N6623 Cat. No.: HY-146762Malvidin-3-galactoside chloride, an anthocyaninmonomer, induces hepatocellular carcino

42、ma (HCC)cells cycle arrest and apoptosis.Malvidin-3-galactoside chloride inhibits theproduction and accumulation of ROS.MAO-B-IN-7 is a potent and blood-brain barrierpermeable MAO-B and AChE inhibitor with IC s50of 41 nM, 87 nM and 0.3 M for human AChE,electric eel AChE and MAO-B, respectively.MAO-B

43、-IN-7 can effectively alleviate oxidativestress and neuroinflammatory damage.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/LY2801653.html Merestinib HYPERLINK https:/www.MedChemE

44、/LY2801653.html HYPERLINK https:/www.MedChemE/LY2801653-dihydrochloride.html Merestinib HYPERLINK https:/www.MedChemE/LY2801653-dihydrochloride.html HYPERLINK https:/www.MedChemE/LY2801653-dihydrochloride.html dihydrochloride(LY2801653) Cat. No.: HY-15514 (LY2801653 dihydrochloride) Cat. No.: HY-155

45、14AMerestinib (LY2801653) is a potent, orallybioavailable c-Met inhibitor (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

46、, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.36%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/mitopq.html MitoPQ HYPERLINK https:/www.MedChemE/mitopq.html HYPERLINK https:/www.MedChemE/nrf2-are-hmao-b-qr2-modulator-1.html Nrf2-ARE/hMAO-B/QR2 HYPERLINK htt

47、ps:/www.MedChemE/nrf2-are-hmao-b-qr2-modulator-1.html HYPERLINK https:/www.MedChemE/nrf2-are-hmao-b-qr2-modulator-1.html modulator HYPERLINK https:/www.MedChemE/nrf2-are-hmao-b-qr2-modulator-1.html HYPERLINK https:/www.MedChemE/nrf2-are-hmao-b-qr2-modulator-1.html 1(MitoParaquat) Cat. No.: HY-130278

48、Cat. No.: HY-144635MitoPQ is a mitochondria-targeted redox cycler.MitoPQ produces superoxide by redox cycling at theflavin site of complex I, selectively increasingsuperoxide production within mitochondria. MitoPQcan be used in antioxidant study.Nrf2-ARE/hMAO-B/QR2 modulator 1 is aResveratrol-based

49、multitarget-directed ligandswith IC s of 8.05, 9.83 and 0.57 M for50hMAO-B, NRF2 and QR2.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.M

50、edChemE/nrf2-ho-1-in-1.html Nrf2/HO-1-IN-1Cat. No.: HY-146971 HYPERLINK https:/www.MedChemE/orniplabin.html Orniplabin(SMTP-7) Cat. No.: HY-122311Nrf2/HO-1-IN-1 is a potent Nrf2/HO-1 pathwayinhibitor, with an IC50 value of 0.38 M for NO.Nrf2/HO-1-IN-1 can significantly reduce the levelof ROS in cell

51、s. Nrf2/HO-1-IN-1 can be used forresearching anti-inflammatory.Orniplabin (SMTP-7) is a low-molecular-weightcompound that enhances plasminogenfibrin binding,urokinase-catalyzed activation of plasminogen, andurokinase and plasminogen-mediated fibrindegradation.Purity: 98%Clinical Data: No Development

52、 ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/p38-mapk-in-3.html p38 HYPERLINK https:/www.MedChemE/p38-mapk-in-3.html HYPERLINK https:/www.MedChemE/p38-mapk-in-3.html MAPK-IN-3 HYPERLINK https:/www.MedChemE/p38-mapk-in-3.html

53、 HYPERLINK https:/www.MedChemE/phyltetralin.html PhyltetralinCat. No.: HY-144697 Cat. No.: HY-121397p38 MAPK-IN-3 (Compound 2c) is a p38 MAPKinhibitor. p38 MAPK-IN-3 has antitumor activitiesand induces apoptosis and ROS.Phyltetralin (Compound 10) is a natural productthan can be isolated from the hex

54、ane-ethyl acetateextract of Phyllanthus amarus leaves.Phyltetralin possesses immunosuppressive effectson different lineages of innate immune system.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.

55、MedChemE/TPX-0005.html Repotrectinib(TPX-0005) Cat. No.: HY-103022 HYPERLINK https:/www.MedChemE/taletrectinib.html Taletrectinib(DS-6051b; AB-106) Cat. No.: HY-131003Repotrectinib (TPX-0005) is a potent ROS1(IC =0.07 nM) and ( =0.83/0.05/0.1 nM for50 TRK IC50TRKA/B/C) inhibitor. Repotrectinib poten

56、tlyinhibits WT ALK (IC =1.01 nM). Repotrectinib has50anti-cancer activity.Taletrectinib (DS-6051b) is a potent, orallyactive, and next-generation selective ROS1/NTRKinhibitor. Taletrectinib potently inhibitsrecombinant ROS1, NTRK1, NTRK2, and NTRK3 withIC s of 0.207, 0.622, 2.28, and 0.98 nM,50respe

57、ctively.Purity: 99.81%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mgPurity: 99.96%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/taletrectinib-free-base.html Taletrectinib HYPERLINK https:/www.MedChemE/taletrectinib-free-bas

58、e.html HYPERLINK https:/www.MedChemE/taletrectinib-free-base.html free HYPERLINK https:/www.MedChemE/taletrectinib-free-base.html HYPERLINK https:/www.MedChemE/taletrectinib-free-base.html base HYPERLINK https:/www.MedChemE/taletrectinib-free-base.html HYPERLINK https:/www.MedChemE/topo-i-in-1.html

59、Topo HYPERLINK https:/www.MedChemE/topo-i-in-1.html HYPERLINK https:/www.MedChemE/topo-i-in-1.html I-IN-1(DS-6051b free base; AB-106 free base) Cat. No.: HY-131003ACat. No.: HY-145859Taletrectinib (DS-6051b) free base is a potent,orally active, and next-generation selectiveROS1/NTRK inhibitor. Talet

60、rectinib free basepotently inhibits recombinant ROS1, NTRK1, NTRK2,and NTRK3 with IC s of 0.207, 0.622, 2.28, and500.98 nM, respectively.Topo I-IN-1 (Compound 14d) is a potent Topo Iinhibitor with antitumor activity and DNAintercalative capability. Topo I-IN-1 induces cellapoptosis.Purity: 98%Clinic