Bcr-Abl-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Bcr-Abl.html Bcr-AblBcr-Abl tyrosine-kinase inhibitors (TKI) are the first-line therapy for most patients with chronic myelogenous leukemia (CML). Morethan 90% of CML cases are caused by a chromosomal abnormality that results in the formation of a so-called Phi

2、ladelphiachromosome. This abnormality is a consequence of fusion between the Abelson (Abl) tyrosine kinase gene at chromosome 9 andthe break point cluster (Bcr) gene at chromosome 22, resulting in a chimeric oncogene (Bcr-Abl) and a constitutively active Bcr-Abltyrosine kinase that has been implicat

3、ed in the pathogenesis of CML. Compounds have been developed to selectively inhibit thetyrosine kinase.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Bcr-Abl.html Bcr-Abl HYPERLINK https:/www.MedChemE/Targets/Bcr-Abl.html HYPERLINK https:/www.MedChemE/Targets/Bcr-Abl.html Inhibitors HYPERLINK

4、https:/www.MedChemE/Targets/Bcr-Abl.html HYPERLINK https:/www.MedChemE/Targets/Bcr-Abl.html & HYPERLINK https:/www.MedChemE/Targets/Bcr-Abl.html HYPERLINK https:/www.MedChemE/Targets/Bcr-Abl.html Activators HYPERLINK https:/www.MedChemE/adaphostin.html Adaphostin(NSC 680410) Cat. No.: HY-103275 HYPE

5、RLINK https:/www.MedChemE/ag957.html AG957(Tyrphostin AG957; NSC 654705) Cat. No.: HY-117718Adaphostin (NSC 680410), the adamantyl ester ofAG957, is a potent p210bcr/abl inhibitor (IC =1450M). Adaphostin induces apoptosis inT-lymphoblastic human leukemia cell lines (IC50ranging from 17 to 216 nM).AG

6、957 (Tyrphostin AG957;NSC 654705) is a tyrosinekinase inhibitor with anti-BCR/ABL tyrosine kinaseactivity. AG957 is a bcr/abl kinase inhibitor withan IC of 2.9 M for autokinase50 p210bcr/ablactivity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Develop

7、ment ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Asciminib.html Asciminib(ABL001) Cat. No.: HY-104010 HYPERLINK https:/www.MedChemE/AST-487.html AST HYPERLINK https:/www.MedChemE/AST-487.html HYPERLINK https:/www.MedChemE/AST-487.html 487(NVP-AST 487) Cat. No.: HY-15002Asciminib (ABL001)

8、is a potent and selectiveallosteric BCR-ABL1 inhibitor, which inhibitsBa/F3 cells grown with an IC of 0.25 nM.50AST 487 is a RET kinase inhibitor with IC of50880 nM, inhibits RET autophosphorylation andactivation of downstream effectors, also inhibitsFlt-3 with IC of 520 nM.50Purity: 99.78%Clinical

9、Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.20%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/at9283.html AT9283 HYPERLINK https:/www.MedChemE/at9283.html HYPERLINK https:/www.MedChemE/azd0424.html AZD0424Cat.

10、 No.: HY-50514 Cat. No.: HY-112314AT9283 is a multi-targeted kinase inhibitor withpotent activity against Aurora A/B, JAK2/3, Abl(T315I) and Flt3 (IC s ranging from 1 to 30 nM).50AT9283 inhibits growth and survival of multiplesolid tumors in vitro and in vivo.AZD0424 is an orally active, and dual se

11、lectiveSrc/Abl kinase inhibitor with potentialantineoplastic activity. AZD0424 induces apoptosisand cell cycle arrest in lymphoma cells.Purity: 99.70%Clinical Data: Phase 2Size: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: Phase 1Size: 1 mg, 5 mg HYPERLINK https:/www.MedChem

12、E/Bafetinib.html Bafetinib HYPERLINK https:/www.MedChemE/Bafetinib.html HYPERLINK https:/www.MedChemE/BCR-ABL-IN-1.html BCR-ABL-IN-1(INNO-406; NS-187) Cat. No.: HY-50868Cat. No.: HY-100314Bafetinib is a potent and orally active Lyn/Bcr-Abltyrosine kinase inhibitor. Bafetinib augments theactivities o

13、f several proapoptotic Bcl-2 homology(BH)3-only proteins (Bim, Bad, Bmf and Bik) andinduces apoptosis in Ph+ leukemia cells via Bcl-2family-regulated intrinsic apoptosis pathway.BCR-ABL-IN-1 is an inhibitor of BCR-ABL tyrosinekinase, with a pIC of 6.46, and may be used in50the research of chronic my

14、elogenous leukemia.Purity: 99.76%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/BCR-ABL-IN-2.html BCR-ABL-IN-2 HYPERLINK https:/www.MedChemE/BCR-ABL-IN-2.html HYPERLINK https:/www.MedCh

15、emE/bcr-abl-in-3.html BCR-ABL-IN-3Cat. No.: HY-18819 Cat. No.: HY-136526BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosinekinase, with IC s of 57 nM, 773 nm for ABL1native50and ABL1T315I, respectively.BCR-ABL-IN-3 is a potent and irreversible Bcr-Ablinhibitor with an IC of 100 nM for50Ba/F Bcr-AblT31

16、51. BCR-ABL-IN-3 has anti-cancer3activity.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/bcr-abl-in-4.html BCR-ABL-IN-4Cat. No.:

17、 HY-142922 HYPERLINK https:/www.MedChemE/Bosutinib.html Bosutinib(SKI-606) Cat. No.: HY-10158BCR-ABL-IN-4 is a BCR-ABL inhibitor withanticancer effects. BCR-ABL-IN-4 inhibits thecancer cell growth with IC values of 0.67 nM and5016 nM for K562 cells and BCR-ABL T315I transfectedBa/F3 cells, respectiv

18、ely (WO2021143927A1;compound 11).Bosutinib is a dual Src/Abl inhibitor with IC s of501.2 nM and 1 nM, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.96%Clinical Data: LaunchedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/bosuti

19、nib-d8.html Bosutinib HYPERLINK https:/www.MedChemE/bosutinib-d8.html HYPERLINK https:/www.MedChemE/bosutinib-d8.html D8(SKI-606 D8) Cat. No.: HY-10158S HYPERLINK https:/www.MedChemE/c-abl-in-2.html c-ABL-IN-2Cat. No.: HY-146527Bosutinib D8 (SKI-606 D8) is a deuterium labeledBosutinib. Bosutinib is

20、a dual Src/Abl inhibitorwith IC s of 1.2 nM and 1 nM, respectively.50c-ABL-IN-2 is a potent inhibitor of c-Abl.Activation of c-Abl has been implicated in variousdiseases, notably cancer.Purity: 99.0%Clinical Data: No Development ReportedSize: 1 mgPurity: 98%Clinical Data: No Development ReportedSize

21、: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/cenisertib.html Cenisertib(AS-703569; R-763) Cat. No.: HY-13072 HYPERLINK https:/www.MedChemE/chmfl-abl-039.html CHMFL-ABL-039Cat. No.: HY-126143Cenisertib (AS-703569) is an ATP-competitivemulti-kinase inhibitor that blocks the activity ofAurora-kinase-A/B,

22、 ABL1, AKT, STAT5 and FLT3.CHMFL-ABL-039 is a type II native ABL kinase anddrug-resistant V299L mutant BCR-ABL inhibitorwith the IC s of 7.9 nM and 27.9 nM,50respectively. CHMFL-ABL-039 is used in theresearch of chronic myeloid leukemia.Purity: 99.64%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10

23、mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/chmfl-abl-121.html CHMFL-ABL-121 HYPERLINK https:/www.MedChemE/chmfl-abl-121.html HYPERLINK https:/www.MedChemE/chmfl-abl-kit-155.html CHMFL-ABL/KIT-155Cat. No.: HY-119370(CHMFL-ABL-KIT-1

24、55) Cat. No.: HY-101034CHMFL-ABL-121 is a highly potent type II ABLkinase inhibitor with IC s of 2 nM and 0.2 nM50against purified inactive ABL wt and T315I kinaseprotein, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgCHMFL-ABL/KIT-155 (CHMFL-ABL-KIT-155; compound 34)

25、is a highly potent and orally active type IIABL/c-KIT dual kinase inhibitor (IC s of 46 nM and5075 nM, respectively), and it also presentssignificant inhibitory activities to BLK (IC =8150nM), CSF1R (IC =227 nM), DDR1 ( =116 nM),Purity: 98%50 IC50Clinical Data: No Development ReportedSize: 1 mg, 5 m

26、g HYPERLINK https:/www.MedChemE/ct-721.html CT-721 HYPERLINK https:/www.MedChemE/ct-721.html HYPERLINK https:/www.MedChemE/CZC-8004.html CZC-8004Cat. No.: HY-108704(CZC-00008004) Cat. No.: HY-111138CT-721 is a potent and time-dependent Bcr-Abl kinaseinhibitor with an IC of 21.3 nM for wild-type50Bcr

27、-Abl kinase, and possesses anti-chronic myeloidleukemia (CML) activities.CZC-8004 is a pan-kinase inhibitor and binds arange of tyrosine kinases, including ABL kinase.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.61%Clinical Data: No Development ReportedSize: 10 mM 1 mL

28、, 5 mg, 10 mg, 25 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/Dasatinib.html Dasatinib(BMS-354825) Cat. No.: HY-10181 HYPERLINK https:/www.MedChemE/Dasatinib-hydrochloride.html Dasatinib HYPERLINK https:/www.MedChemE/Dasatinib-hydrochloride.html HYPERLINK https:/www.MedChemE/Dasatinib-hydrochlori

29、de.html hydrochloride(BMS-354825 hydrochloride) Cat. No.: HY-10181ADasatinib (BMS-354825) is a highly potent, ATPcompetitive, orally active dual Src/Bcr-Ablinhibitor with potent antitumor activity. The Ksiare 16 pM and 30 pM for Src and Bcr-Abl,respectively.Dasatinib (BMS-354825) hydrochloride is a

30、highlypotent, ATP competitive, orally active dualSrc/Bcr-Abl inhibitor with potent antitumoractivity. The Ks are 16 pM and 30 pM for Src andiBcr-Abl, respectively.Purity: 99.85%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 mg, 200 mg, 500 mgPurity: 98.86%Clinical Data: LaunchedSize: 10 mM 1 mL, 100 m

31、g, 200 mg, 500 mg HYPERLINK https:/www.MedChemE/dasatinib-monohydrate.html Dasatinib HYPERLINK https:/www.MedChemE/dasatinib-monohydrate.html HYPERLINK https:/www.MedChemE/dasatinib-monohydrate.html monohydrate(BMS-354825 monohydrate) Cat. No.: HY-10181B HYPERLINK https:/www.MedChemE/dasatinib-d8.ht

32、ml Dasatinib-d8(BMS-354825-d8) Cat. No.: HY-10181SDasatinib (BMS-354825) monohydrate is a highlypotent, ATP competitive, orally active dualSrc/Bcr-Abl inhibitor with potent antitumoractivity. The Ks are 16 pM and 30 pM for Src andiBcr-Abl, respectively.Dasatinib D8 is a deuterium labeled Dasatinib.D

33、asatinib is a dual Bcr-Abl and Src familytyrosine kinase inhibitor.Purity: 98%Clinical Data: LaunchedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/db07107.html DB07107 HYPERLINK https:/www.MedChemE/db07107.html HYPERLINK https:/www.Me

34、dChemE/debio-0617b.html Debio HYPERLINK https:/www.MedChemE/debio-0617b.html HYPERLINK https:/www.MedChemE/debio-0617b.html 0617BCat. No.: HY-123390 Cat. No.: HY-108417DB07107 is a potent drug resistant T315I mutantBcr-Abl tyrosine kinase inhibitor. DB07107 is alsoa potent Akt1 inhibitor with an IC

35、value of 36050nM.Debio 0617B, a multi-kinase inhibitor, reducesmaintenance and self-renewal of primary human AMLCD34+ stem/progenitor cells.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

36、/WP1130.html Degrasyn HYPERLINK https:/www.MedChemE/WP1130.html HYPERLINK https:/www.MedChemE/DPH.html DPH(WP1130) Cat. No.: HY-13264Cat. No.: HY-12070Degrasyn (WP1130) is a cell-permeabledeubiquitinase (DUB) inhibitor, directlyinhibiting DUB activity of USP9x, USP5, USP14, andUCH37. Degrasyn has be

37、en shown to downregulate theantiapoptotic proteins Bcr-Abl and JAK2.DPH is a potent cell permeable c-Abl activator,which displays potent enzymatic and cellularactivity in stimulating c-Abl activation. .Purity: 99.70%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPu

38、rity: 99.20%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/Flumatinib.html Flumatinib HYPERLINK https:/www.MedChemE/Flumatinib.html HYPERLINK https:/www.MedChemE/flumatinib-mesylate.html Flumatinib HYPERLINK https:/www.MedChemE/flumatinib-mesylate.

39、html HYPERLINK https:/www.MedChemE/flumatinib-mesylate.html mesylate(HHGV678) Cat. No.: HY-13904 (HHGV678 mesylate) Cat. No.: HY-13905Flumatinib (HHGV678) is an orally available,selective inhibitor of Bcr-Abl. Flumatinib inhibitsc-Abl, PDGFR and c-Kit with IC s of 1.2 nM, 307.650nM and 665.5 nM, res

40、pectively.Flumatinib mesylate (HHGV678 mesylate) is anorally available, selective inhibitor of Bcr-Abl.Flumatinib mesylate inhibits c-Abl, PDGFR andc-Kit with IC s of 1.2 nM, 307.6 nM and 665.5 nM,50respectively.Purity: 99.94%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 99.97%Cl

41、inical Data: Phase 4Size: 10 mM 1 mL, 500 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/flumatinib-d3.html Flumatinib-d3(HHGV678-d3) Cat. No.: HY-13904S HYPERLINK https:/www.MedChemE/gmb-475.html GMB-475Cat. No.: HY-125834Flumatinib-d3 is deuterium labele

42、d Flumatinib.Flumatinib (HHGV678) is an orally available,selective inhibitor of Bcr-Abl. Flumatinibinhibits c-Abl, PDGFR and c-Kit with IC50s of 1.2nM, 307.6 nM and 665.5 nM, respectively.GMB-475 is a degrader of BCR-ABL1 tyrosine kinasebased on PROTAC, overcoming BCR-ABL1-dependentdrug resistance.

43、GMB-475 targets BCR-ABL1 proteinand recruits the E3 ligase Von Hippel Lindau(VHL), resulting in ubiquitination and subsequentdegradation of the oncogenic fusion protein.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.20%Clinical Data: No Development ReportedSize: 10 mM 1

44、mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/GNF-2.html GNF-2 HYPERLINK https:/www.MedChemE/GNF-2.html HYPERLINK https:/www.MedChemE/GNF-5.html GNF-5Cat. No.: HY-11007 Cat. No.: HY-15738GNF-2 is a highly selective, allosteric, non-ATPcompetitive inhibitor of Bcr-Abl. GNF-2 inhibitsBa/F3.p210

45、 proliferation with an IC of 138 nM .50GNF-5, an analogue of GNF-2 with improvedpharmacokinetic properties, is a selective non-ATPcompetitive inhibitor of Bcr-Abl with an IC50value of 0.220.1 uM (Wild type Abl).Purity: 98.73%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg,

46、 100 mgPurity: 99.42%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/GNF-7.html GNF-7 HYPERLINK https:/www.MedChemE/GNF-7.html HYPERLINK https:/www.MedChemE/GZD856.html GZD856Cat. No.: HY-10943 Cat. No.: HY-101489GNF-7 is a multikinase inhib

47、itor. GNF-7 is aBcr-Abl inhibitor, with IC s of 133 nM and 61 nM50for Bcr-AblWT and Bcr-AblT315I, respectively.GZD856 formic is a potent and orally activePDGFR/ inhibitor, with IC s of 68.6 and 136.650nM, respectively. GZD856 formic is also aBcr-AblT315I inhibitor, with IC s of 19.9 and5015.4nM for

48、native Bcr-Abl and the T315I mutant.GZD856 formic has antitumor activity.Purity: 98.93%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, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/gzd85

49、6-formic.html GZD856 HYPERLINK https:/www.MedChemE/gzd856-formic.html HYPERLINK https:/www.MedChemE/gzd856-formic.html formic HYPERLINK https:/www.MedChemE/gzd856-formic.html HYPERLINK https:/www.MedChemE/hg-7-85-01.html HG-7-85-01Cat. No.: HY-101489A Cat. No.: HY-15814GZD856 formic is a potent and

50、orally activePDGFR/ inhibitor, with IC s of 68.6 and 136.650nM, respectively. GZD856 formic is also aBcr-AblT315I inhibitor, with IC s of 19.9 and5015.4nM for native Bcr-Abl and the T315I mutant.GZD856 formic has antitumor activity.HG-7-85-01 is a type II ATP competitive inhibitorof wild-type and ga

51、tekeeper mutations forms ofBcr-Abl, PDGFR, Kit, and Src kinases.Purity: 98.06%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: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ihmt-trk-284.html IHMT-TRK-284 HYPERL

52、INK https:/www.MedChemE/ihmt-trk-284.html HYPERLINK https:/www.MedChemE/Imatinib.html ImatinibCat. No.: HY-146697(STI571; CGP-57148B) Cat. No.: HY-15463IHMT-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 TRKA, B, andC respecti

53、vely. IHMT-TRK-284 displays greatselectivity profile in the kinome and good in vivoantitumor efficacies.Imatinib (STI571) is an orally bioavailabletyrosine kinases inhibitor that selectivelyinhibits BCR/ABL, v-Abl, PDGFR and c-kit kinaseactivity.Purity: 98%Clinical Data: No Development ReportedSize:

54、 1 mg, 5 mgPurity: 99.54%Clinical Data: LaunchedSize: 10 mM 1 mL, 200 mg, 500 mg, 1 g, 5 gwww.MedChemE 5 HYPERLINK https:/www.MedChemE/imatinib-d4.html Imatinib HYPERLINK https:/www.MedChemE/imatinib-d4.html HYPERLINK https:/www.MedChemE/imatinib-d4.html D4(STI571 D4; CGP-57148B D4) Cat. No.: HY-154

55、63S1 HYPERLINK https:/www.MedChemE/Imatinib-Mesylate.html Imatinib HYPERLINK https:/www.MedChemE/Imatinib-Mesylate.html HYPERLINK https:/www.MedChemE/Imatinib-Mesylate.html Mesylate(STI571 Mesylate; CGP-57148B Mesylate) Cat. No.: HY-50946Imatinib D4 (STI571 D4) is a deuterium labeledImatinib (STI571

56、). Imatinib is an orallybioavailable tyrosine kinases inhibitor thatselectively inhibits BCR/ABL, v-Abl, PDGFR andc-kit kinase activity.Imatinib Mesylate (STI571 Mesylate) is a tyrosinekinases inhibitor that inhibits c-Kit, Bcr-Abl, andPDGFR (IC =100 nM) tyrosine kinases.50Purity: 99.0%Clinical Data

57、: No Development ReportedSize: 1 mg, 5 mgPurity: 99.91%Clinical Data: LaunchedSize: 10 mM 1 mL, 200 mg, 500 mg, 1 g, 5 g HYPERLINK https:/www.MedChemE/imatinib-d8.html Imatinib-d8(STI571-d8; CGP-57148B-d8) Cat. No.: HY-15463S HYPERLINK https:/www.MedChemE/KW-2449.html KW-2449Cat. No.: HY-10339Imatin

58、ib D8 (STI571 D8) is a deuterium labeledImatinib (STI571). Imatinib is an orallybioavailable tyrosine kinases inhibitor thatselectively inhibits BCR/ABL, v-Abl, PDGFR andc-kit kinase activity.KW-2449 is a multi-targeted kinase inhibitor ofFLT3, ABL, ABLT315I and Aurora kinase with IC s50of 6.6, 14,

59、4 and 48 nM, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 5 mgPurity: 99.85%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/LXH254.html LXH254Cat. No.: HY-112089 HYPERLINK https:/www.MedChemE/Lyn-IN-1.html Lyn-IN-1(Bafetinib ana

60、log) Cat. No.: HY-12039LXH254 is a potent, selective, orally active, typeII BRAF and CRAF inhibitor, with IC values of500.072 and 0.21 nM against CRAF and BRAF,respectively.Lyn-IN-1 (Bafetinib analog) is a potent andselective dual Bcr-Abl/Lyn inhibitor, extractedfrom patent WO2014169128A1.Purity: 99