1、 HYPERLINK https:/www.MedChemE/Targets/IGF-1R.html IGF-1RInsulin-like growth factor-1 receptorIGF-1R (Insulin-like growth factor 1 receptor), a receptor tyrosine kinase, is activated upon binding to the ligands IGF-1 or IGF-2leading to cell growth, survival and migration of both normal and cancerous

2、 cells.IGF-1R can initiate the activation of the PI3K/AKT/mTOR signaling and Ras/Raf/MEK/MAPK pathways resulting in the activation ofmultiple transcription factors such as ELK-1, CREB and AP-1 to modulate cell proliferation, survival, differentiation, motility, invasionand angiogenesis. IGF-1R overe

3、xpression or increased IGF-1R kinase activity is associated with a broad range of human cancers andtherefore the IGF-1R is widely considered as a very promising target for cancer treatment.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/IGF-1R.html IGF-1R HYPERLINK https:/www.MedChemE/Targets/I

4、GF-1R.html HYPERLINK https:/www.MedChemE/Targets/IGF-1R.html Inhibitors HYPERLINK https:/www.MedChemE/Targets/IGF-1R.html HYPERLINK https:/www.MedChemE/Targets/IGF-1R.html & HYPERLINK https:/www.MedChemE/Targets/IGF-1R.html HYPERLINK https:/www.MedChemE/Targets/IGF-1R.html Agonists HYPERLINK https:/

5、www.MedChemE/AG1024.html AG1024(Tyrphostin AG 1024) Cat. No.: HY-10253 HYPERLINK https:/www.MedChemE/az12253801.html AZ12253801Cat. No.: HY-125102AG1024 (Tyrphostin AG 1024) is a reversible,competitive and selective IGF-1R inhibitor with anIC50 of 7 M. AG1024 inhibits phosphorylation of IR(IC =57 M)

6、. AG1024 induces and has50 apoptosisanti-cancer activity.Purity: 98.86%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgAZ12253801 is an ATP-competitive IGF-1R tyrosinekinase inhibitor that shows 10-fold selectivityover the insulin receptor. AZ12253801 inhibitsIGF-1R

7、driven proliferation in 3T3 mousefibroblasts (transfected with human IGF-1R) withan IC of 17 nmol/L.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/AZ7550.html AZ7550 HYPERLINK https:/www.MedChemE/AZ7550.html HYPERLINK https:/www.MedChemE/AZ7550_hydr

8、ochloride.html AZ7550 HYPERLINK https:/www.MedChemE/AZ7550_hydrochloride.html HYPERLINK https:/www.MedChemE/AZ7550_hydrochloride.html hydrochlorideCat. No.: HY-B0794 Cat. No.: HY-B0794AAZ7550 is an active metabolite of AZD9291 andinhibits the activity of IGF1R with an IC of 1.650M.AZ7550 hydrochlori

9、de is an active metabolite ofAZD9291 and inhibits the activity of IGF1R with anIC of 1.6 M.50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.66%Clinical Data: Phase 1Size: 5 mg, 10 mg HYPERLINK https:/www.MedChemE/AZ7550_Mesylate.html AZ7550 HYPERLINK https:/www.MedChemE/

10、AZ7550_Mesylate.html HYPERLINK https:/www.MedChemE/AZ7550_Mesylate.html Mesylate(AZ7550 trimesylate salt) Cat. No.: HY-B0794B HYPERLINK https:/www.MedChemE/azd-3463.html AZD-3463(ALK/IGF1R inhibitor) Cat. No.: HY-15609AZ7550 Mesylate is an active metabolite of AZD9291and inhibits the activity of IGF

11、1R with an IC of501.6 M.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: 99.34%Clinical Data: Phase 1Size: 10 mM 1 mL, 5 mg, 10 mgPurity: 99.96%Clinical Data: No Development Repor

12、tedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/BMS-536924.html BMS-536924 HYPERLINK https:/www.MedChemE/BMS-536924.html HYPERLINK https:/www.MedChemE/BMS-754807.html BMS-754807Cat. No.: HY-10262 Cat. No.: HY-10200BMS-536924 is an orally active, competitive andselective

13、 insulin-like growth factor receptor(IGF-1R) kinase and insulin receptor (IR) inhibitorwith IC s of 100 nM and 73 nM, respectively.50BMS-536924 has anti-cancer activity.BMS-754807 is a potent and reversible IGF-1R/IRinhibitor (IC =1.8 and 1.7 nM, respectively;50K=98%Clinical Data: No Development Rep

14、ortedSize: 1 mg, 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/LDK378-dihydrochloride.html Ceritinib HYPERLINK https:/www.MedChemE/LDK378-dihydrochloride.html HYPERLINK https:/www.MedChemE/LDK378-dihydrochloride.html dihydrochloride(LDK378 dihydrochlori

15、de) Cat. No.: HY-15656A HYPERLINK https:/www.MedChemE/Ginsenoside-Rg5.html Ginsenoside HYPERLINK https:/www.MedChemE/Ginsenoside-Rg5.html HYPERLINK https:/www.MedChemE/Ginsenoside-Rg5.html Rg5Cat. No.: HY-N0908Ceritinib dihydrochloride (LDK378 dihydrochloride)is a selective, orally bioavailable andA

16、TP-competitive ALK tyrosine kinase inhibitorwith an IC of 200 pM.50Ginsenoside Rg5 is the main component of Redginseng. Ginsenoside blocks binding of IGF-1 to itsreceptor with an IC of 90 nM. Ginsenoside Rg550also inhibits the mRNA expression of COX-2 viasuppression of the DNA binding activities ofN

17、F-B p65.Purity: 99.83%Clinical Data: LaunchedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.86%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/GSK1838705A.html GSK1838705A HYPERLINK https:/www.MedChemE/GSK1838705A.html HYPERLINK https:/www.Me

18、dChemE/GSK1904529A.html GSK1904529ACat. No.: HY-13020 Cat. No.: HY-10524GSK1838705A 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.50GSK1904529A is a potent, selective, orally active,and ATP-com

19、petitive inhibitor of insulin-likegrowth factor-1 receptor (IGF-1R) and insulinreceptor (IR), with IC s of 27 and 25 nM,50respectively.Purity: 99.28%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.22%Clinical Data: No Development ReportedSize: 10 mM 1 mL,

20、 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/i-ome-tyrphostin-ag-538.html I-OMe-Tyrphostin HYPERLINK https:/www.MedChemE/i-ome-tyrphostin-ag-538.html HYPERLINK https:/www.MedChemE/i-ome-tyrphostin-ag-538.html AG HYPERLINK https:/www.MedChemE/i-ome-tyrphostin-ag-538.html HYPERLINK https:/www.M

21、edChemE/i-ome-tyrphostin-ag-538.html 538(I-OMe-AG 538) Cat. No.: HY-135680 HYPERLINK https:/www.MedChemE/igf-1r-inhibitor-2.html IGF-1R HYPERLINK https:/www.MedChemE/igf-1r-inhibitor-2.html HYPERLINK https:/www.MedChemE/igf-1r-inhibitor-2.html inhibitor-2Cat. No.: HY-145110I-OMe-Tyrphostin AG 538 (I

22、-OMe-AG 538) is aspecific inhibitor of IGF-1R (insulin-like growthfactor-1 receptor tyrosine kinase).IGF-1R inhibitor-2 (example 121) is aninsulin-like growth factor-1 receptor (IGF-1R)inhibitor. Downregulation of IGF-1R can reversethe transformed phenotype of tumor cells andpotentially render them

23、susceptible to apoptosis.Purity: 99.34%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/Indirubin_Derivative_E804.html Indirubin HYPERLINK https:/www.MedChemE/Indirubin_Derivat

24、ive_E804.html HYPERLINK https:/www.MedChemE/Indirubin_Derivative_E804.html Derivative HYPERLINK https:/www.MedChemE/Indirubin_Derivative_E804.html HYPERLINK https:/www.MedChemE/Indirubin_Derivative_E804.html E804 HYPERLINK https:/www.MedChemE/Indirubin_Derivative_E804.html HYPERLINK https:/www.MedCh

25、emE/Linsitinib.html LinsitinibCat. No.: HY-18785(OSI-906) Cat. No.: HY-10191Indirubin Derivative E804 is a potent inhibitor ofInsulin-like Growth Factor 1 Receptor (IGF1R), withan IC of 0.65 M for IGF1R.50Linsitinib (OSI-906) is a potent, selective andorally bioavailable dual inhibitor of the IGF-1r

26、eceptor and insulin receptor (IR) with IC s of 3550and 75 nM, respectively.Purity: 99.79%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 99.88%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/linsitinib-d3.htm

27、l Linsitinib-d3 HYPERLINK https:/www.MedChemE/linsitinib-d3.html HYPERLINK https:/www.MedChemE/nbi-31772.html NBI-31772(OSI-906-d3) Cat. No.: HY-10191SCat. No.: HY-110135Linsitinib-d3 (OSI-906-d3) is the deuteriumlabeled Linsitinib. Linsitinib (OSI-906) is apotent, selective and orally bioavailable

28、dualinhibitor of the IGF-1 receptor and insulinreceptor (IR) with IC s of 35 and 75 nM,50respectively.NBI-31772 is the potent and nonselective inhibitorof IGFBP with a K value of 47 nM. NBI-31772 hasithe potential for the research of IGF-responsivediseases.Purity: 98%Clinical Data: No Development Re

29、portedSize: 1 mg, 5 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgwww.MedChemE 3 HYPERLINK https:/www.MedChemE/nbi-31772-hydrate.html NBI-31772 HYPERLINK https:/www.MedChemE/nbi-31772-hydrate.html HYPERLINK https:/www.MedChemE/nbi-31772-hydrate.html hydrateCat. No.: HY-110135A H

30、YPERLINK https:/www.MedChemE/NVP-ADW742.html NVP-ADW742(ADW742; GSK 552602A; ADW) Cat. No.: HY-10252NBI-31772 hydrate is a potent inhibitor ofinteraction between insulin-like growth factor (IGF)and IGF-binding proteins (IGFBPs).NVP-ADW742 (ADW742) is an orally active, selectiveIGF-1R tyrosine kinase

31、 inhibitor with an IC of500.17 M. NVP-ADW742 inhibits insulin receptor (InsR)with an IC of 2.8 M. NVP-ADW742 induces50pleiotropic antiproliferative/proapoptotic biologicsequelae in tumor cells.Purity: 98.0%Clinical Data: No Development ReportedSize: 5 mgPurity: 99.30%Clinical Data: No Development Re

32、portedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/NVP-AEW541.html NVP-AEW541(AEW541) Cat. No.: HY-50866 HYPERLINK https:/www.MedChemE/NVP-TAE-226.html NVP-TAE HYPERLINK https:/www.MedChemE/NVP-TAE-226.html HYPERLINK https:/www.MedChemE/NVP-TAE-226.html 226(TAE226) Cat.

33、 No.: HY-13203NVP-AEW541 (AEW541) is a potent inhibitor of IGF-1Rwith IC50 of 0.15 M, also inhibits InsR, with IC50of 0.14 M.NVP-TAE 226 (TAE226) is a potent andATP-competitive dual FAK and IGF-1R inhibitor withIC s of 5.5 nM and 140 nM, respectively. NVP-TAE50226 (TAE226) also effectively inhibits

34、Pyk2 andinsulin receptor (InsR) with IC s of 3.5 nM and 4450nM, respectively.Purity: 98.90%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 2 mg, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.92%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/AXL1717.html Picropodophyllin(AXL1717; Picropodophyllin; PPP) Cat. No.: HY-15494 HYPERLINK https:/www.MedChemE/picropodophyllotoxin-d6.html Picropodophyllotoxin-d6Cat. No.: HY-15494S1Picropodophyllin (AXL1717) is a selectiveinsulin-like growth factor-1 receptor (IG