ALK-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/ALK.html ALKAnaplastic lymphoma kinase; ALK tyrosine kinase receptor; CD246; Cluster of differentiation 246Anaplastic lymphoma kinase (ALK), a receptor tyrosine kinase in the insulin receptor superfamily, is predominantly expressed in thebrain and implicated in

2、 neuronal development and cognition. ALK catalyzes the transference of a gamma-phosphate group fromadenosine triphosphate (ATP) to a tyrosine residue on a substrate protein. Therefore, it catalyzes a tyrosine residue phosphorylationreaction on its substrate proteins. The phosphorylation and dephosph

3、orylation of proteins are critical reactions catalyzed bydifferent enzymes (kinases and phosphatases), which play critical roles in various cellular functions.ALK gene activation is involved in the carcinogenesis process of several human cancers such as anaplastic large cell lymphoma, lungcancer, in

4、flammatory myofibroblastic tumors and neuroblastoma, as a consequence of fusion with other oncogenes (NPM, EML4,TIM, etc) or gene amplification, mutation or protein overexpression. ALK is a transmembrane tyrosine kinase receptor that, uponligand binding to its extracellular domain, undergoes dimeriz

5、ation and subsequent autophosphorylation of the intracellular kinasedomain. When activated in cancer it represents a target for specific inhibitors, such as Crizotinib, Ceritinib, Alectinib etc. which usehas demonstrated significant effectiveness in ALK-positive non-small cell lung cancer particular

6、ly.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/ALK.html ALK HYPERLINK https:/www.MedChemE/Targets/ALK.html HYPERLINK https:/www.MedChemE/Targets/ALK.html Inhibitors HYPERLINK https:/www.MedChemE/PF-06260182.html 2-Keto HYPERLINK https:/www.MedChemE/PF-06260182.html HYPERLINK https:/www.MedC

7、hemE/PF-06260182.html Crizotinib(PF-06260182) Cat. No.: HY-13320 HYPERLINK https:/www.MedChemE/6-demethoxytangeretin.html 6-DemethoxytangeretinCat. No.: HY-N41262-Keto Crizotinib (PF-06260182) is an activelactam metabolite of crizotinib.6-Demethoxytangeretin is a citrus flavonoidisolated from Citrus

8、 depressa.Purity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mgPurity: 99.28%Clinical Data: No Development ReportedSize: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/CH5424802.html Alectinib(CH5424802; RO5424802; AF802) Cat. No.: HY-13011 HYPERLINK https:/www.MedChemE/CH5424802-Hydr

9、ochloride.html Alectinib HYPERLINK https:/www.MedChemE/CH5424802-Hydrochloride.html HYPERLINK https:/www.MedChemE/CH5424802-Hydrochloride.html Hydrochloride HYPERLINK https:/www.MedChemE/CH5424802-Hydrochloride.html (CH5424802 Hydrochloride; RO5424802Hydrochloride; AF-802 Hydrochloride) Cat. No.: HY

10、-13011AAlectinib (CH5424802) is a potent, selective, andorally available ALK inhibitor with an IC of501.9 nM and a K value of 2.4 nM (in andATP-competitive manner), and also inhibits ALKF1174L and ALK R1275Q with IC s of 1 nM and503.5 nM, respectively.Alectinib Hydrochloride (CH5424802 Hydrochloride

11、;RO5424802 Hydrochloride; AF-802 Hydrochloride) isa potent, selective, and orally available ALKinhibitor with an IC50 of 1.9 nM and a Kd valueof 2.4 nM (in an ATP-competitive manner), and alsoinhibits ALK F1174L and ALK R1275Q withPurity: 99.87%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 5

12、0 mg, 100 mg, 200 mgPurity: 99.89%Clinical Data: LaunchedSize: 5 mg, 10 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/alectinib-d6.html Alectinib-d6(CH5424802-d6; RO5424802-d6; AF802-d6) Cat. No.: HY-13011S1 HYPERLINK https:/www.MedChemE/alectinib-d8.html Alectinib-d8(CH5424802-d8; RO54248

13、02-d8; AF802-d8) Cat. No.: HY-13011SAlectinib-d6 is deuterium labeled Alectinib.Alectinib-d8 (CH5424802-d8) is the deuteriumlabeled Alectinib.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChe

14、mE/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 HYPER

15、LINK 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-153

16、58ALK 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 ap

17、otent 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 mg

18、 HYPERLINK https:/www.MedChemE/alk-kinase-inhibitor-1.html ALK HYPERLINK https:/www.MedChemE/alk-kinase-inhibitor-1.html HYPERLINK https:/www.MedChemE/alk-kinase-inhibitor-1.html kinase HYPERLINK https:/www.MedChemE/alk-kinase-inhibitor-1.html HYPERLINK https:/www.MedChemE/alk-kinase-inhibitor-1.htm

19、l inhibitor-1 HYPERLINK https:/www.MedChemE/alk-kinase-inhibitor-1.html HYPERLINK https:/www.MedChemE/ALK-IN-1.html ALK-IN-1Cat. No.: HY-19990(Brigatinib analog) Cat. No.: HY-13464ALK kinase inhibitor-1 is an anaplastic lymphomakinase (ALK) inhibitor extracted from patentUS20130261106A1 compound I-2

20、02.ALK-IN-1 (Brigatinib analog) is a potent andselective active inhibitor of anaplastic lymphomakinase(ALK), Patent US20140066406 A1.Purity: 99.85%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.94%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg,

21、50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/alk-in-12.html ALK-IN-12 HYPERLINK https:/www.MedChemE/alk-in-12.html HYPERLINK https:/www.MedChemE/alk-in-13.html ALK-IN-13Cat. No.: HY-108230 Cat. No.: HY-12973ALK-IN-12 is a potent and orally act

22、ive ALKinhibitor with an IC of 0.18 nM. ALK-IN-12 also50inhibits IGF1R and InsR (IC =20.3 and 90.6 nM).50Antitumor activities.ALK-IN-13 is an ALK inhibitor, extracted frompatent US20130225528A1, example 19.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No

23、Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/alk-in-5.html ALK-IN-5 HYPERLINK https:/www.MedChemE/alk-in-5.html HYPERLINK https:/www.MedChemE/alk-in-6.html ALK-IN-6Cat. No.: HY-128569 Cat. No.: HY-128596ALK-IN-5 is a potent, selective, andbrain-penetrant inhibitor of anaplastic

24、 lymphomakinase (ALK), with an IC of 2.9 nM.50ALK-IN-6 (compound 11) is an orally bioavailableinhibitor of anaplastic lymphoma kinase (ALK),with IC values of 71 nM, 18.72 nM and 36.81 nM50for ALK wild, ALK F1196M and ALK F1174L,respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg

25、, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/alk-in-9.html ALK-IN-9 HYPERLINK https:/www.MedChemE/alk-in-9.html HYPERLINK https:/www.MedChemE/alk-ros1-in-1.html ALK/ROS1-IN-1Cat. No.: HY-131244 Cat. No.: HY-130794ALK-IN-9 (compound 40) is a po

26、tent ALK inhibitor.ALK-IN-9 inhibits cell proliferation with IC s of500.2 nM, 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/alk5-in-6.html ALK5-IN-6 HYPERLINK https:/www.MedChemE/alk5-in-6.html

27、 HYPERLINK https:/www.MedChemE/alk5-in-7.html ALK5-IN-7Cat. No.: HY-142950 Cat. No.: HY-142949ALK5-IN-6 is a potent inhibitor of ALK5. ALK5-IN-7 is a potent inhibitor of ALK5.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg,

28、 5 mg HYPERLINK https:/www.MedChemE/ASP3026.html ASP3026 HYPERLINK https:/www.MedChemE/ASP3026.html HYPERLINK https:/www.MedChemE/azd-3463.html AZD-3463Cat. No.: HY-13326(ALK/IGF1R inhibitor) Cat. No.: HY-15609ASP3026 is a potent, selective and orally activeinhibitor of anaplastic lymphoma kinase (A

29、LK).ASP3026 induces apoptosis of tumor cells. ASP3026can be used for the research of non-small celllung cancer (NSCLC).AZD-3463 (ALK/IGF1R inhibitor) is an orally activeALK/IGF1R inhibitor, with a K of 0.75 nM for ALK.iAZD3463 induces apoptosis and autophagy inneuroblastoma cells.Purity: 99.90%Clini

30、cal Data: Phase 1Size: 10 mM 1 mL, 50 mg, 100 mgPurity: 99.96%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/Belizatinib.html Belizatinib(TSR-011) Cat. No.: HY-17603 HYPERLINK https:/www.MedChemE/Brigatinib.html Brigatin

31、ib(AP-26113) Cat. No.: HY-12857Belizatinib is an oral, dual, potent inhibitor ofALK and TRKA, TRKB, and TRKC, with IC of 0.7nM50for wild-type recombinant ALK kinase.Brigatinib (AP-26113) is a highly potent andselective ALK inhibitor, with an IC of 0.6 nM.50Purity: 99.66%Clinical Data: Phase 2Size: 1

32、0 mM 1 mL, 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.98%Clinical Data: LaunchedSize: 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/brigatinib-13c6.html Brigatinib-13C6(AP-26113-13C6) Cat. No.: HY-12857S HYPERLINK https:/www.MedChemE/brigatinib-d3.html Brigatinib-d3(AP-26113-d3) Ca

33、t. No.: HY-12857S1Brigatinib-13C6 (AP-26113-13C6) is the 13C-labeledBrigatinib. Brigatinib (AP-26113) is a highlypotent and selective ALK inhibitor, with an IC50of 0.6 nM.Brigatinib-d3 (AP-26113-d3) is the deuteriumlabeled Brigatinib. Brigatinib (AP-26113) is ahighly potent and selective ALK inhibit

34、or, withan IC of 0.6 nM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/CEP-28122.html CEP-28122 HYPERLINK https:/www.MedChemE/CEP-28122.html HYPERLINK https:/www.MedChemE/CEP-28122-mes

35、ylate-salt.html CEP-28122 HYPERLINK https:/www.MedChemE/CEP-28122-mesylate-salt.html HYPERLINK https:/www.MedChemE/CEP-28122-mesylate-salt.html mesylate HYPERLINK https:/www.MedChemE/CEP-28122-mesylate-salt.html HYPERLINK https:/www.MedChemE/CEP-28122-mesylate-salt.html saltCat. No.: HY-18030 Cat. N

36、o.: HY-18030ACEP-28122 is a highly potent and selective orallyactive ALK inhibitor with IC50 of 1.9 0.5 nM inan enzyme-based TRF assay. IC50 value: 1.9 0.5nM Target: ALK in vitro: CEP-28122 is a potentinhibitor of recombinant ALK activity and cellularALK tyrosine phosphorylation.CEP-28122 mesylate s

37、alt, a diaminopyrimidinederivative, is a potent, selective, and orallybioavailable ALK inhibitor, with an IC value of501.9 nM for recombinant ALK kinase activity.CEP-28122 has antitumor activity in experimentalmodels of ALK-positive human cancers.Purity: 98%Clinical Data: No Development ReportedSize

38、: 1 mg, 5 mgPurity: 99.85%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/CEP-37440.html CEP-37440 HYPERLINK https:/www.MedChemE/CEP-37440.html HYPERLINK https:/www.MedChemE/LDK378.html CeritinibCat. No.: HY-15841(LDK378) Cat. No.: HY-

39、15656CEP-37440 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).Ceritinib (LDK378) is a selective, orallybioavailable, and ATP-competitive ALK tyrosinekinase inhibitor with an IC of 200 pM. Ceritinib50(LDK378) also inh

40、ibits IGF-1R, InsR, and STK22Dwith IC values of 8, 7, and 23 nM, respectively.50Ceritinib (LDK378) shows great antitumor potency.Purity: 99.97%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.97%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg H

41、YPERLINK https:/www.MedChemE/ceritinib-d7.html Ceritinib HYPERLINK https:/www.MedChemE/ceritinib-d7.html HYPERLINK https:/www.MedChemE/ceritinib-d7.html D7 HYPERLINK https:/www.MedChemE/ceritinib-d7.html HYPERLINK https:/www.MedChemE/LDK378-dihydrochloride.html Ceritinib HYPERLINK https:/www.MedChem

42、E/LDK378-dihydrochloride.html HYPERLINK https:/www.MedChemE/LDK378-dihydrochloride.html dihydrochloride(LDK378 D7) Cat. No.: HY-15656S (LDK378 dihydrochloride) Cat. No.: HY-15656ACeritinib D7 (LDK378 D7) is a deuterium labeledCeritinib. Ceritinib is a selective, orallybioavailable and ATP-competitiv

43、e ALK tyrosinekinase inhibitor.Ceritinib dihydrochloride (LDK378 dihydrochloride)is a selective, orally bioavailable andATP-competitive ALK tyrosine kinase inhibitorwith an IC of 200 pM.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.83%Clinical Data: LaunchedSize: 10 m

44、M 1 mL, 5 mg, 10 mg, 50 mg, 100 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/cj-2360.html CJ-2360 HYPERLINK https:/www.MedChemE/cj-2360.html HYPERLINK https:/www.MedChemE/con-b-1.html Con HYPERLINK https:/www.MedChemE/con-b-1.html HYPERLINK https:/www.Me

45、dChemE/con-b-1.html B-1Cat. No.: HY-131909 Cat. No.: HY-142287CJ-2360 is a potent and orally active ALKinhibitor with IC s of 2.2, 4.0, 8.8, 6.3, and508.9 nM against wild-type ALK and F1197M, G1269A,L1196M, and S1206Y ALK mutants, respectively.ConB-1 is a potent and selective ALK inhibitorwith low t

46、oxicity to normal cells.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: Phase 1Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Crizotinib.html Crizotinib(PF-02341066) Cat. No.: HY-50878 HYPERLINK https:/www.MedChemE/Crizotinib-hydrochloride.html Crizotinib H

47、YPERLINK https:/www.MedChemE/Crizotinib-hydrochloride.html HYPERLINK https:/www.MedChemE/Crizotinib-hydrochloride.html hydrochloride(PF-02341066 hydrochloride) Cat. No.: HY-50878ACrizotinib (PF-02341066) is an orallybioavailable, ATP-competitive ALK and c-Metinhibitor with IC s of 20 and 8 nM, respe

48、ctively.50Crizotinib hydrochloride (PF-02341066hydrochloride) is an orally bioavailable,selective, and ATP-competitive dual ALK andc-Met inhibitor with IC s of 20 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

49、 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(PF-02341066-d5) Cat. No.: HY-50878S HYPERLINK https:/www.MedChemE/EML4-ALK_kinase_inhibitor_1.html EML4-ALK HYPERLINK https:/www.MedChemE/EML4-ALK_kinase_inhibitor_1.h

50、tml HYPERLINK https:/www.MedChemE/EML4-ALK_kinase_inhibitor_1.html kinase HYPERLINK https:/www.MedChemE/EML4-ALK_kinase_inhibitor_1.html HYPERLINK https:/www.MedChemE/EML4-ALK_kinase_inhibitor_1.html inhibitor HYPERLINK https:/www.MedChemE/EML4-ALK_kinase_inhibitor_1.html HYPERLINK https:/www.MedChe

51、mE/EML4-ALK_kinase_inhibitor_1.html 1Cat. No.: HY-111752Crizotinib-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.EML4-ALK kinase inhibitor 1 is a potent orallya

52、ctive inhibitor of echinodermmicrotubule-associated protein-like 4-anaplasticlymphoma kinase (EML4-ALK), with an IC of 150nM.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.49%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERL

53、INK https:/www.MedChemE/X-396.html Ensartinib HYPERLINK https:/www.MedChemE/X-396.html 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) Cat. No.: HY-1

54、03714 (X-396 dihydrochloride) Cat. No.: HY-103714AEnsartinib (X-396) is a potent and 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 mgPur

55、ity: 99.46%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/Entrectinib.html Entrectinib HYPERLINK https:/www.MedChemE/Entrectinib.html HYPERLINK https:/www.MedChemE/envonalkib.html Envonalkib(NMS-E628; RXDX-101) Cat. No.: HY-12678Cat. No.: HY-

56、145566Entrectinib (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, respectively. Antitumor activity.Envonalkib is a potent and orally active inhibitorof ALK, with IC s

57、of 1.96 nM, 35.1 nM, and 61.350nM for WT and mutated L1196M andG1269S-ALK. Envonalkib can be used for theresearch of non-small cell lung cancer.Purity: 99.32%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChe

58、mE 5 HYPERLINK https:/www.MedChemE/f-1.html F-1 HYPERLINK https:/www.MedChemE/f-1.html HYPERLINK https:/www.MedChemE/GSK1838705A.html GSK1838705ACat. No.: HY-112801 Cat. No.: HY-13020F-1 is a potent ALK and ROS1 dual inhibitor,suppresses phospho-ALK and its relative downstreamsignaling pathways, wit

59、h IC s of 2.1 nM, 2.3 nM,501.3 nM and 3.9 nM for ALKWT, ROS1WT,ALKL1196M and ALKG1202R, respectively.GSK1838705A is a potent and reversible IGF-IR andthe insulin receptor inhibitor with IC s of 2.050and 1.6 nM, respectively. It also inhibits ALKwith an IC of 0.5 nM.50Purity: 98.65%Clinical Data: No

60、Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.28%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/HG-14-10-04.html HG-14-10-04Cat. No.: HY-15801 HYPERLINK https:/www.MedChemE/iruplinalkib.html Iruplinalkib(WX-059