Syk-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Syk.html SykSpleen tyrosine kinaseSyk (Spleen tyrosine kinase) is a cytosolic non-receptor protein tyrosine kinase (PTK) that is expressed at high levels, both inhematopoietic cells (such as mast cells, B lymphocytes, T lymphocytes, neutrophils, dendritic cells

2、, and macrophages) and innon-hematopoietic cells.Syk mediates key signal transduction pathways following the activation of immune cell receptors. Syk associates with differentreceptors on the surface of various cells such as B cells, mast cells, monocytes, macrophages, and neutrophils, and even oste

3、oclastsand breast cancer cells. Following the engagement of these receptors with their ligands, SYK is activated and orchestrates diversecellular responses, including cytokine production (in T cells and monocytes) and phagocytosis (in macrophages).www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets

4、/Syk.html Syk HYPERLINK https:/www.MedChemE/Targets/Syk.html HYPERLINK https:/www.MedChemE/Targets/Syk.html Inhibitors HYPERLINK https:/www.MedChemE/bay-61-3606.html BAY HYPERLINK https:/www.MedChemE/bay-61-3606.html HYPERLINK https:/www.MedChemE/bay-61-3606.html 61-3606 HYPERLINK https:/www.MedChem

5、E/bay-61-3606.html HYPERLINK https:/www.MedChemE/BAY-61-3606-dihydrochloride.html BAY HYPERLINK https:/www.MedChemE/BAY-61-3606-dihydrochloride.html HYPERLINK https:/www.MedChemE/BAY-61-3606-dihydrochloride.html 61-3606 HYPERLINK https:/www.MedChemE/BAY-61-3606-dihydrochloride.html HYPERLINK https:/

6、www.MedChemE/BAY-61-3606-dihydrochloride.html dihydrochlorideCat. No.: HY-76474 Cat. No.: HY-14985BAY 61-3606 is an orally available,ATP-competitive, reversible and highly selectiveSyk Ki IC50inhibitor with a of 7.5 nM and an of10 nM. BAY 61-3606 reduces ERK1/2 and Aktphosphorylation in neuroblastom

7、a cell.BAY 61-3606 dihydrochloride is an orallyavailable, ATP-competitive, reversible and highlyselective Syk inhibitor with a K of 7.5 nM aniIC of 10 nM. BAY 61-3606 dihydrochloride reduces50ERK1/2 and Akt phosphorylation in neuroblastomacell.Purity: 98.21%Clinical Data: No Development ReportedSize

8、: 1 mg, 5 mgPurity: 98.37%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg HYPERLINK https:/www.MedChemE/Cerdulatinib.html Cerdulatinib(PRT062070; PRT2070) Cat. No.: HY-15999 HYPERLINK https:/www.MedChemE/cerdulatinib-hydrochloride.html Cerdulatinib HYPERLINK https:/www.Med

9、ChemE/cerdulatinib-hydrochloride.html HYPERLINK https:/www.MedChemE/cerdulatinib-hydrochloride.html hydrochloride(PRT062070 hydrochloride; PRT2070 hydrochloride) Cat. No.: HY-15999ACerdulatinib (PRT062070) is a selective Tyk2inhibitor with an IC of 0.5 nM. Cerdulatinib50(PRT062070) also is a dual JA

10、K and SYK inhibitorwith IC s of 12, 6, 8 and 32 for JAK1, 2, 3 and50SYK, respectively.Cerdulatinib hydrochloride (PRT062070) is aselective, oral active and reversibleATP-competitive inhibitor of dual SYK and JAK,with IC s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM50for SYK and Tyk2, JAK1, 2, 3, respecti

11、vely.Purity: 99.0%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mgPurity: 99.54%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/cevidoplenib.html Cevidoplenib HYPERLINK https:/www.MedChemE/cevidoplenib.html HY

12、PERLINK https:/www.MedChemE/cevidoplenib-dimesylate.html Cevidoplenib HYPERLINK https:/www.MedChemE/cevidoplenib-dimesylate.html HYPERLINK https:/www.MedChemE/cevidoplenib-dimesylate.html dimesylateCat. No.: HY-109082 Cat. No.: HY-109082ACevidoplenib is an orally available inhibitor ofspleen tyrosin

13、e kinase (Syk), with potentialanti-inflammatory and immunomodulating activities.Cevidoplenib is an orally available inhibitor ofspleen tyrosine kinase (Syk), with potentialanti-inflammatory and immunomodulating activities.Purity: 98.08%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg,

14、50 mg, 100 mgPurity: 98.48%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/GS-9973.html Entospletinib HYPERLINK https:/www.MedChemE/GS-9973.html HYPERLINK https:/www.MedChemE/r788.html Fostamatinib(GS-9973) Cat. No.: HY-15968 (R788) Cat. No

15、.: HY-13038AEntospletinib (GS-9973) is an orally bioavailable,selective Syk inhibitor with an IC of 7.7 nM.50Fostamatinib (R788) is the oral prodrug of theactive compound R406. R406 is an orally availableand competitive Syk/FLT3 inhibitor with a K ofi30 nM and an IC of 41 nM. R406 also inhibits Lyn5

16、0(IC =63 nM) and Lck (IC =37 nM).50 50Purity: 99.86%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mgPurity: 99.20%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/r788_prodrug-of-r406_.html Fostamatinib HYPERLINK https:/www.M

17、edChemE/r788_prodrug-of-r406_.html HYPERLINK https:/www.MedChemE/r788_prodrug-of-r406_.html Disodium HYPERLINK https:/www.MedChemE/r788_prodrug-of-r406_.html HYPERLINK https:/www.MedChemE/R788-disodium-hexahydrate.html Fostamatinib HYPERLINK https:/www.MedChemE/R788-disodium-hexahydrate.html HYPERLI

18、NK https:/www.MedChemE/R788-disodium-hexahydrate.html disodium HYPERLINK https:/www.MedChemE/R788-disodium-hexahydrate.html HYPERLINK https:/www.MedChemE/R788-disodium-hexahydrate.html hexahydrate(R788(Disodium) Cat. No.: HY-13038 (R788 disodium hexahydrate) Cat. No.: HY-13038BFostamatinib Disodium

19、(R788 Disodium) is the oralprodrug of the active compound R406. R406 is anorally available and competitive Syk/FLT3inhibitor with a Ki of 30 nM and an IC50 of 41 nM.R406 also inhibits Lyn (IC =63 nM) and Lck (IC =3750 50nM).Fostamatinib (R788) disodium hexahydrate is theoral prodrug of the active co

20、mpound R406. R406 isan orally available and competitive Syk/FLT3inhibitor with a Ki of 30 nM and an IC50 of 41 nM.R406 also inhibits Lyn (IC =63 nM) and Lck (IC =3750 50nM).Purity: 99.88%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98.94%Clinical Data: LaunchedSize: 10

21、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/fostamatinib-d9.html Fostamatinib-d9(R788-d9) Cat. No.: HY-13038AS HYPERLINK https:/www.MedChemE/gsk143.html GSK143Cat. No.: HY-12736Fostamatinib-d9 (R788-d9) is the deuterium

22、labeledFostamatinib. Fostamatinib (R788) is the oralprodrug of the active compound R406. R406 is anorally available and competitive Syk/FLT3inhibitor with a Ki of 30 nM and an IC50 of 41 nM.GSK143 is an orally active and highly selectivespleen tyrosine kinase (SYK) inhibitor with apIC of 7.5. GSK143

23、 inhibits phosphorylated Erk50(pErk: pIC =7.1). GSK143 reduces inflammation and50prevents recruitment of immune cells in theintestinal muscularis in mice.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https

24、:/www.MedChemE/gsk143-dihydrochloride.html GSK143 HYPERLINK https:/www.MedChemE/gsk143-dihydrochloride.html HYPERLINK https:/www.MedChemE/gsk143-dihydrochloride.html dihydrochlorideCat. No.: HY-12736A HYPERLINK https:/www.MedChemE/ASN-002.html Gusacitinib(ASN-002) Cat. No.: HY-103018GSK143 dihydroch

25、loride is an orally active andhighly selective spleen tyrosine kinase (SYK)inhibitor with a pIC of 7.5. GSK14350dihydrochloride inhibits phosphorylated Erk (pErk:pIC =7.1).50Gusacitinib (ASN-002) is an orally active andpotent dual inhibitor of spleen tyrosine kinase(SYK) and janus kinase (JAK) with

26、IC values of505-46 nM. Gusacitinib has anti-cancer activity inboth solid and hematological tumor types.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.41%Clinical Data: Phase 2Size: 10 mM 1 mL, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/lanraplenib.html Lanrapleni

27、b(GS-9876) Cat. No.: HY-109091 HYPERLINK https:/www.MedChemE/lanraplenib-monosuccinate.html Lanraplenib HYPERLINK https:/www.MedChemE/lanraplenib-monosuccinate.html HYPERLINK https:/www.MedChemE/lanraplenib-monosuccinate.html monosuccinate(GS-9876 monosuccinate) Cat. No.: HY-109091ALanraplenib (GS-9

28、876) is a highly selective andorally active SYK inhibitor (IC =9.5 nM) in50development for the treatment of inflammatorydiseases.Lanraplenib monosuccinate (GS-9876 monosuccinate)is a highly selective and orally active SYKinhibitor (IC =9.5 nM) in development for the50treatment of inflammatory diseas

29、es.Purity: 98.22%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: Phase 2Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/lanraplenib-succinate.html Lanraplenib HYPERLINK https:/www.MedChemE/lanraplenib-succinate.html HYPERLINK https:/www.MedChemE/lanraplenib

30、-succinate.html succinate HYPERLINK https:/www.MedChemE/lanraplenib-succinate.html HYPERLINK https:/www.MedChemE/MNS.html MNS(GS-9876 succinate) Cat. No.: HY-109091B (NSC 170724; 5-(2-Nitrovinyl)benzodioxole) Cat. No.: HY-78263Lanraplenib succinate (GS-9876 succinate) is ahighly selective and orally

31、 active SYK inhibitor(IC =9.5 nM) in development for the treatment of50inflammatory diseases.MNS (NSC 170724), the beta-nitrostyrenederivative, is a potent tyrosine kinase inhibitorand a broad-spectrum antiplatelet agent.Purity: 98.21%Clinical Data: Phase 2Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 m

32、gPurity: 99.55%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 100 mg, 200 mg, 500 mg HYPERLINK https:/www.MedChemE/oxsi-2.html OXSI-2 HYPERLINK https:/www.MedChemE/oxsi-2.html HYPERLINK https:/www.MedChemE/Piceatannol.html PiceatannolCat. No.: HY-112386(Astringenin; trans-Piceatannol) Cat.

33、No.: HY-13518OXSI-2 is a bioavailable, cell-permeable Sykinhibitor with an EC50 of 313 nM and an IC50 of14 nM.Piceatannol is a well-known Syk inhibitor andreduces the expression of iNOS induced by TNF.Piceatannol is an effective agent for research ofacute lung injury (ALI).Purity: 98%Clinical Data:

34、No Development ReportedSize: 1 mg, 5 mgPurity: 98.09%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 10 mg, 25 mg, 50 mg, 100 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/PRT-060318.html PRT-060318(PRT318) Cat. No.: HY-12974 HYPERLINK https:/www.MedChemE/PRT062607.html PRT062607(P505-15; P

35、RT-2607; BIIB-057) Cat. No.: HY-15322PRT-060318 (PRT318) is a novel selective inhibitorof the tyrosine kinase Syk with an IC of 4 nM.50PRT062607(P505-15; PRT-2607; BIIB-057) is a highlyspecific and potent inhibitor of Syk with IC50 of1-2 nM; 80-fold selective for Syk than Fgr,Lyn, FAK, Pyk2 and Zap7

36、0.Purity: 99.50%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: Phase 2Size: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/PRT062607-Hydrochloride.html PRT062607 HYPERLINK https:/www.MedChemE/PRT062607-Hydrochloride.html HYPERLINK https:/

37、www.MedChemE/PRT062607-Hydrochloride.html Hydrochloride(P505-15 Hydrochloride) Cat. No.: HY-15323 HYPERLINK https:/www.MedChemE/R112.html R112Cat. No.: HY-16420PRT062607 Hydrochloride (P505-15 Hydrochloride) isa highly specific and potent inhibitor of purifiedSyk (IC 1-2 nM).50R112 is an ATP-competi

38、tive inhibitor of Syk kinasewith a Ki of 96 nM. R112 inhibits Syk kinaseactivity with an IC50 of 226 nM.Purity: 98.68%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mgPurity: 99.23%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK h

39、ttps:/www.MedChemE/R406.html R406 HYPERLINK https:/www.MedChemE/R406.html HYPERLINK https:/www.MedChemE/R406-free-base.html R406 HYPERLINK https:/www.MedChemE/R406-free-base.html HYPERLINK https:/www.MedChemE/R406-free-base.html free HYPERLINK https:/www.MedChemE/R406-free-base.html HYPERLINK https:

40、/www.MedChemE/R406-free-base.html baseCat. No.: HY-12067 Cat. No.: HY-11108R406 is an orally available and competitiveSyk/FLT3 inhibitor for ATP binding with a K ofi30 nM, potently inhibits Syk kinase activity invitro with an IC of 41 nM, measured at an ATP50concentration corresponding to its K valu

41、e.mR406 free base is an orally available andcompetitive Syk/FLT3 inhibitor for ATP bindingwith a K of 30 nM, potently inhibits Syk kinaseiactivity in vitro with an IC of 41 nM, measured50at an ATP concentration corresponding to its Kmvalue.Purity: 96.67%Clinical Data: No Development ReportedSize: 10

42、 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.69%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/RO9021.html RO9021 HYPERLINK https:/www.MedChemE/RO9021.html HYPERLINK https:/www.MedChemE/sovleplenib.html SovleplenibCat. No.: HY-16902

43、(HMPL-523) Cat. No.: HY-145598RO9021 is an orally bioavailable, novelATP-competitive inhibitor of SYK, with an averageIC of 5.6 nM.50Sovleplenib (HMPL-523) is a highly potent, orallyavailable and selective SYK inhibitor with anIC of 25 nM. Anti-tumor activity. Sovleplenib50can be used for the resear

44、ch of immunethrombocytopenia (ITP).Purity: 98.76%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 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/srx3207.html SRX3207 HYPERLINK https:/www.MedChemE/srx32

45、07.html HYPERLINK https:/www.MedChemE/syk-inhibitor-ii.html Syk HYPERLINK https:/www.MedChemE/syk-inhibitor-ii.html HYPERLINK https:/www.MedChemE/syk-inhibitor-ii.html Inhibitor HYPERLINK https:/www.MedChemE/syk-inhibitor-ii.html HYPERLINK https:/www.MedChemE/syk-inhibitor-ii.html IICat. No.: HY-136

46、198 Cat. No.: HY-112390ASRX3207 is an orally active and first-in-classdual Syk/PI3K inhibitor, with IC values of 10.750nM and 861 nM for Syk and PI3K, respectively.SRX3207 relieves tumor immunosuppression.Syk Inhibitor II is a potent, high selective andATP-competitive Syk inhibitor with an IC of 415

47、0nM. Syk Inhibitor II inhibits 5-HT release fromRBL-cells with an IC of 460 nM. Syk Inhibitor II50shows less potent against other kinases and hasanti-allergic effect.Purity: 98.92%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98.05%Clinical Data: No Development

48、 ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg4 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/syk-kinase-peptide-substrate.html Syk HYPERLINK https:/www.MedChemE/syk-kinase-peptide-substrate.html HYPERLINK https:/www.MedChemE/syk-kinase-peptide-substrate.html

49、Kinase HYPERLINK https:/www.MedChemE/syk-kinase-peptide-substrate.html HYPERLINK https:/www.MedChemE/syk-kinase-peptide-substrate.html Peptide HYPERLINK https:/www.MedChemE/syk-kinase-peptide-substrate.html HYPERLINK https:/www.MedChemE/syk-kinase-peptide-substrate.html Substrate HYPERLINK https:/ww

50、w.MedChemE/syk-kinase-peptide-substrate.html HYPERLINK https:/www.MedChemE/syk-kinase-peptide-substrate-biotin-labeled.html Syk HYPERLINK https:/www.MedChemE/syk-kinase-peptide-substrate-biotin-labeled.html HYPERLINK https:/www.MedChemE/syk-kinase-peptide-substrate-biotin-labeled.html Kinase HYPERLI

51、NK https:/www.MedChemE/syk-kinase-peptide-substrate-biotin-labeled.html HYPERLINK https:/www.MedChemE/syk-kinase-peptide-substrate-biotin-labeled.html Peptide HYPERLINK https:/www.MedChemE/syk-kinase-peptide-substrate-biotin-labeled.html HYPERLINK https:/www.MedChemE/syk-kinase-peptide-substrate-bio

52、tin-labeled.html Substrate, HYPERLINK https:/www.MedChemE/syk-kinase-peptide-substrate-biotin-labeled.html HYPERLINK https:/www.MedChemE/syk-kinase-peptide-substrate-biotin-labeled.html Biotin HYPERLINK https:/www.MedChemE/syk-kinase-peptide-substrate-biotin-labeled.html HYPERLINK https:/www.MedChem

53、E/syk-kinase-peptide-substrate-biotin-labeled.html labeledCat. No.: HY-P2505 Cat. No.: HY-P2504Syk Kinase Peptide Substrate is a Syk kinasepeptide substrate.Syk Kinase Peptide Substrate, Biotin labeled is abiotin-labled Syk kinase peptide substrate.Purity: 98%Clinical Data: No Development ReportedSi

54、ze: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/syk-in-1.html Syk-IN-1 HYPERLINK https:/www.MedChemE/syk-in-1.html HYPERLINK https:/www.MedChemE/syk-in-3.html Syk-IN-3Cat. No.: HY-12657 Cat. No.: HY-130680Syk-IN-1 (compound 4) is a potent Syk inhibitor,with an IC of 35 nM.50Syk-IN-3, a potent spleen tyrosine kinase (Syk)inhibitor, extracted from patent WO2011075515A1,compound example 152, has an IC of 150nM.Pur