Discoidin-Domain-Receptor-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/Discoidin Domain Receptor.html Discoidin HYPERLINK https:/www.MedChemE/Targets/Discoidin Domain Receptor.html HYPERLINK https:/www.MedChemE/Targets/Discoidin Domain Receptor.html Domain HYPERLINK https:/www.MedChemE/Targets/Discoidin Domain Receptor.html HYPERL

2、INK https:/www.MedChemE/Targets/Discoidin Domain Receptor.html ReceptorDiscoidin domain receptors (DDRs) are members of the transmembrane receptor tyrosine kinase (RTK) superfamily which aredistinguished from others by the presence of a discoidin motif in the extracellular domain and their utilizati

3、on of collagens asinternal ligands. Two types of DDRs, DDR1 and DDR2, have been identified with distinct expression profiles and ligand specificities.Upon collagen binding, DDRs transduce cellular signaling involved in various cell functions, including cell adhesion, proliferation,differentiation, m

4、igration, and matrix homeostasis. Altered DDR function resulting from either mutations or overexpression hasbeen implicated in several types of disease, including atherosclerosis, inflammation, cancer, and tissue fibrosis. DDRs have beenconsidered as novel potential molecular targets for drug discov

5、ery and increasing efforts are being devoted to the identification ofnew small molecule inhibitors targeting the receptors.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/Discoidin Domain Receptor.html Discoidin HYPERLINK https:/www.MedChemE/Targets/Discoidin Domain Receptor.html HYPERLINK http

6、s:/www.MedChemE/Targets/Discoidin Domain Receptor.html Domain HYPERLINK https:/www.MedChemE/Targets/Discoidin Domain Receptor.html HYPERLINK https:/www.MedChemE/Targets/Discoidin Domain Receptor.html Receptor HYPERLINK https:/www.MedChemE/Targets/Discoidin Domain Receptor.html HYPERLINK https:/www.M

7、edChemE/Targets/Discoidin Domain Receptor.html Inhibitors HYPERLINK https:/www.MedChemE/DDR1-IN-2.html 7rh(DDR1-IN-2) Cat. No.: HY-U00444 HYPERLINK https:/www.MedChemE/DDR_Inhibitor.html DDR HYPERLINK https:/www.MedChemE/DDR_Inhibitor.html HYPERLINK https:/www.MedChemE/DDR_Inhibitor.html InhibitorCa

8、t. No.: HY-W0189317rh (DDR1-IN-2) is a potent inhibitor of discoidindomain receptor 1 (DDR1), with an IC of 13.150nM, and also less potently inhibits DDR2, with anIC of 203 nM.50DDR Inhibitor is a potent discoidin domain receptor(DDR) inhibitor, with an IC of 3.3 nM for DDR2,50and shows 53% inhibiti

9、on on DDR1 at 1.5 nM.Purity: 98.62%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mgPurity: 99.43%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg HYPERLINK https:/www.MedChemE/DDR1-IN-3.html DDR-TRK-1 HYPERLINK https:/www.MedChemE/DDR1-IN-3.html HYPERLINK

10、 https:/www.MedChemE/DDR1-IN-1.html DDR1-IN-1Cat. No.: HY-100695 Cat. No.: HY-13979DDR-TRK-1 is a selective Discoidin Domain Receptor1 (DDR1) inhibitor, with an IC value of 9.4 nM.50DDR-TRK-1 also inhibits TRK family.DDR1-IN-1 is a potent and selective DDR1 receptortyrosine kinase inhibitor with an

11、IC of 105 nM;504-fold less potent for DDR2 (IC = 413 nM).50Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.20%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/ddr1-in-1-dihydrochloride.html DDR1-IN-1 HYPERLIN

12、K https:/www.MedChemE/ddr1-in-1-dihydrochloride.html HYPERLINK https:/www.MedChemE/ddr1-in-1-dihydrochloride.html dihydrochloride HYPERLINK https:/www.MedChemE/ddr1-in-1-dihydrochloride.html HYPERLINK https:/www.MedChemE/ddr1-in-4.html DDR1-IN-4Cat. No.: HY-13979A Cat. No.: HY-114173DDR1-IN-1 dihydr

13、ochloride is a potent andselective DDR1 receptor tyrosine kinase inhibitorwith an IC of 105 nM; 4-fold less potent for50DDR2 (IC = 413 nM).50DDR1-IN-4 (Compound 2.45) is a selective andpotent Discoidin Domain Receptor 1 (DDR1)autophosphorylation inhibitor, with IC values of5029 nM and 1.9 M for DDR1

14、 and DDR2, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98.01%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/ddr1-in-5.html DDR1-IN-5 HYPERLINK https:/www.MedChemE/ddr1-in-5.html HYPERLINK https:/ww

15、w.MedChemE/ddr1-in-6.html DDR1-IN-6Cat. No.: HY-133669 Cat. No.: HY-133670DDR1-IN-5 is a selective Discoidin Domain Receptorfamily, member 1 (DDR1) inhibitor with an IC of507.36 nM. DDR1-IN-5 inhibits auto-phosphorylationDDR1b (Y513) with an IC of 4.1 nM. DDR1-IN-5 has50anti-cancer activity.DDR1-IN-

16、6 is a selective Discoidin Domain Receptorfamily, member 1 (DDR1) inhibitor with an IC of509.72 nM. DDR1-IN-6 inhibits auto-phosphorylationDDR1b (Y513) with an IC of 9.7 nM. DDR1-IN-6 has50anti-cancer activity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 98%Clinical Data:

17、 No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/ddr2-in-1.html DDR2-IN-1 HYPERLINK https:/www.MedChemE/ddr2-in-1.html HYPERLINK https:/www.MedChemE/fgfr1-ddr2-inhibitor-1.html FGFR1/DDR2 HYPERLINK https:/www.MedChemE/fgfr1-ddr2-inhibitor-1.html HYPERLINK https:/www.MedChemE/fg

18、fr1-ddr2-inhibitor-1.html inhibitor HYPERLINK https:/www.MedChemE/fgfr1-ddr2-inhibitor-1.html HYPERLINK https:/www.MedChemE/fgfr1-ddr2-inhibitor-1.html 1Cat. No.: HY-112545 Cat. No.: HY-114311DDR2-IN-1 is potent DDR2 inhibitor with an IC50of 26 nM. DDR2-IN-1, compound 129, can be used forosteoarthri

19、tis research.FGFR1/DDR2 inhibitor 1 is an orally activeinhibitor of fibroblast growth factor receptor 1(FGFR1) and discoindin domain receptor 2 (DDR2),with IC values of 31.1 nM and 3.2 nM,50respectively. Antitumor activity.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.0

20、3%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/LY2801653.html Merestinib(LY2801653) Cat. No.: HY-15514 HYPERLINK https:/www.MedChemE/LY2801653-dihydrochloride.html Merestinib HYPE

21、RLINK https:/www.MedChemE/LY2801653-dihydrochloride.html HYPERLINK https:/www.MedChemE/LY2801653-dihydrochloride.html dihydrochloride(LY2801653 dihydrochloride) Cat. No.: HY-15514AMerestinib (LY2801653) is a potent, orallybioavailable c-Met inhibitor (K=2 nM) withianti-tumor activities.Merestinib di

22、hydrochloride (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, 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 http

23、s:/www.MedChemE/ml786-dihydrochloride.html ML786 HYPERLINK https:/www.MedChemE/ml786-dihydrochloride.html HYPERLINK https:/www.MedChemE/ml786-dihydrochloride.html dihydrochlorideCat. No.: HY-14979A HYPERLINK https:/www.MedChemE/Sitravatinib.html Sitravatinib(MGCD516; MG-516) Cat. No.: HY-16961ML786

24、dihydrochloride is a potent and orallybioavailable Raf inhibitor, with IC s of 2.1,504.2, and 2.5 nM for V600EB-Raf, wt B-Raf,and C-Raf, respectively. ML786 dihydrochloridealso inhibits Abl-1, DDR2, EPHA2, KDR, and RET(IC =98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgSitravatinib (MGCD51

25、6) is an orally bioavailablereceptor tyrosine kinase (RTK) inhibitor withIC s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 850nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER,VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1,TRKA, TRKB, respectively.Purity: 99.59%Clinical Data: Phase 3Size: 10 mM 1 mL, 5 mg,

26、10 mg, 25 mg, 50 mg, 100 mg, 200 mg HYPERLINK https:/www.MedChemE/sitravatinib-malate.html Sitravatinib HYPERLINK https:/www.MedChemE/sitravatinib-malate.html HYPERLINK https:/www.MedChemE/sitravatinib-malate.html malate(MGCD516 malate; MG-516 malate) Cat. No.: HY-16961A HYPERLINK https:/www.MedChemE/vu6015929.html VU6015929Cat. No.: HY-135401Sitravatinib malate (MGCD516 malate) is an orallybioavailable receptor tyrosine kinase (RTK)inhibitor with IC s of 1.5 nM