BCRP-Inhibitors-Modulators-MCE

1、 HYPERLINK https:/www.MedChemE/Targets/BCRP.html BCRPBreast cancer resistance protein; ABCG2Breast cancer resistance protein (BCRP/ABCG2/MXR/ABCP) is an ATP-dependent efflux transporter, which belongs to the largeATP-binding cassette (ABC) transporter family present on cell membranes, and it is clas

2、sified into the G subfamily of thesetransporters. BCRP is expressed in a variety of normal cells and acts as a xenobiotic efflux transporter. BCRP is often associated withcancer chemotherapeutic resistance. BCRP confers multidrug resistance (MDR) to a series of antitumor agents such asMitoxantrone,

3、Daunorubicin, SN-38, and Topotecan, and often limits the efficacy of chemotherapy.BCRP physiologically functions as a part of a self-defense mechanism for the organism. It enhances elimination of toxic xenobioticsubstances and harmful agents in the gut and biliary tract, as well as through the blood

4、-brain, placental, and possibly blood-testisbarriers. BCRP recognizes and transports numerous anticancer drugs including conventional chemotherapeutic and targeted smalltherapeutic molecules relatively new in clinical use. Thus, BCRP expression in cancer cells directly causes MDR by active efflux of

5、anticancer drugs. Because BCRP is also known to be a stem cell marker, its expression in cancer cells could be a manifestation ofmetabolic and signaling pathways that confer multiple mechanisms of drug resistance, self-renewal (stemness), and invasiveness(aggressiveness), and thereby impart a poor p

6、rognosis. Therefore, blocking BCRP-mediated active efflux may provide a therapeuticbenefit for cancers.www.MedChemE 1 HYPERLINK https:/www.MedChemE/Targets/BCRP.html BCRP HYPERLINK https:/www.MedChemE/Targets/BCRP.html HYPERLINK https:/www.MedChemE/Targets/BCRP.html Inhibitors HYPERLINK https:/www.M

7、edChemE/BCRP-IN-1.html (S)-ML753286Cat. No.: HY-100390 HYPERLINK https:/www.MedChemE/6-8-diprenylnaringenin.html 6,8-Diprenylnaringenin(Lonchocarpol A; Senegalensin) Cat. No.: HY-122416(S)-ML753286 is a breast cancer resistance protein(BCRP) inhibitor with an IC of 0.6 M on BCRP50efflux transporter.

8、6,8-Diprenylnaringenin (Lonchocarpol A;Senegalensin), a hop prenylflavonoid, is ainhibitor of breast cancer resistance protein(BCRP/ABCG2).Purity: 98.90%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25

9、 mg HYPERLINK https:/www.MedChemE/ac32az19.html Ac32Az19 HYPERLINK https:/www.MedChemE/ac32az19.html HYPERLINK https:/www.MedChemE/cp-100356-hydrochloride.html CP-100356 HYPERLINK https:/www.MedChemE/cp-100356-hydrochloride.html HYPERLINK https:/www.MedChemE/cp-100356-hydrochloride.html hydrochlorid

10、eCat. No.: HY-132934 Cat. No.: HY-108347Ac32Az19 is a potent, nontoxic, and highlyselective BCRP inhibitor with an EC value of5013 nM in the BCRP-overexpressed HEK293/R2 cells.CP-100356 hydrochloride is an orally active dualMDR1 (P-gp)/BCRP inhibitor, with an IC s of500.5 and 1.5 M for inhibiting MD

11、R1-mediatedCalcein-AM transport and BCRP-mediated Prazosintransport, respectively.Purity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mgPurity: 99.68%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg HYPERLINK https:/www.MedChemE/elacridar.html Elacridar(GF120918; GW09

12、18; GG918; GW120918) Cat. No.: HY-50879 HYPERLINK https:/www.MedChemE/fd-12-9.html FD HYPERLINK https:/www.MedChemE/fd-12-9.html HYPERLINK https:/www.MedChemE/fd-12-9.html 12-9(Ac12Az9) Cat. No.: HY-128685Elacridar (GF120918) is a potent P-glycoprotein(Pgp) and BCRP inhibitor.FD 12-9 is a flavonoid

13、dimer, acts as a dualinhibitor of P-gp and BCRP, with EC s of 28550nM and 0.9 nM, respectively. Anti-glioblastomaactivity.Purity: 99.80%Clinical Data: No Development ReportedSize: 10 mg, 50 mg, 100 mg, 200 mg, 500 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/w

14、ww.MedChemE/Fumitremorgin_C.html Fumitremorgin HYPERLINK https:/www.MedChemE/Fumitremorgin_C.html HYPERLINK https:/www.MedChemE/Fumitremorgin_C.html C HYPERLINK https:/www.MedChemE/Fumitremorgin_C.html HYPERLINK https:/www.MedChemE/Ko-143.html Ko HYPERLINK https:/www.MedChemE/Ko-143.html HYPERLINK h

15、ttps:/www.MedChemE/Ko-143.html 143(12-Fumitremorgin C) Cat. No.: HY-N2143Cat. No.: HY-10010Fumitremorgin C is a potent and selectiveABCG2/BRCP inhibitor.Ko 143 is a potent and selective ATP-bindingcassette subfamily G member 2 (ABCG2/BCRP)inhibitor. Ko 143 displays 200-foldselectivity over P-gp and

16、MRP-1 transporters.Purity: 98.26%Clinical Data: No Development ReportedSize: 250 g, 1 mgPurity: 99.83%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg HYPERLINK https:/www.MedChemE/KS176.html KS176 HYPERLINK https:/www.MedChemE/KS176.html HYPERLINK https:/www

17、.MedChemE/ml230.html ML230Cat. No.: HY-19753(CID44640177; SID 88095709) Cat. No.: HY-111678KS176 is a potent and selective inhibitor of thebreast cancer resistance protein (BCRP) multidrugtransporter (IC50 values are 0.59 and 1.39 M inPheo A and Hoechst 33342 assays respectively).Displays no inhibit

18、ory activity against P-gp orMRP1.ML230 (CID44640177; SID 88095709) is a selectiveinhibitor of ATP-binding cassette (ABC) transporterABCG2, and 36-fold selective for ABCG2 over ABCB1with EC s values of 0.13 M and 4.65 M,50respectively.Purity: 98.01%Clinical Data: No Development ReportedSize: 10 mM 1

19、mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 99.12%Clinical Data: No Development ReportedSize: 5 mg2 Tel: 609-228-6898 Fax: 609-228-5909 Email: salesMedChemE HYPERLINK https:/www.MedChemE/ml753286.html ML753286 HYPERLINK https:/www.MedChemE/ml753286.html HYPERLINK https:/www.MedChemE/p-gp-bcrp-in-1.html P-

20、gp/BCRP-IN-1Cat. No.: HY-116494 Cat. No.: HY-144393ML753286 is an orally active and selective BCRP(Breast cancer resistance protein) inhibitor withan IC of 0.6 M. ML753286 has high permeability50and low to medium clearance in rodent and humanliver S9 fractions, and is stable in plasma crossspecies.P

21、-gp/BCRP-IN-1 (compound 19) is a potential,relatively safe, orally active and efficientefflux transporter (P-gp and BCRP) inhibitor.P-gp/BCRP-IN-1 exerts resistance reversal byinhibiting the efflux function of P-gp and BCRP.Purity: 99.79%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 1 mg,

22、5 mg, 10 mgPurity: 98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/PCI-29732.html PCI HYPERLINK https:/www.MedChemE/PCI-29732.html HYPERLINK https:/www.MedChemE/PCI-29732.html 29732 HYPERLINK https:/www.MedChemE/PCI-29732.html HYPERLINK https:/www.MedChemE/pd1

23、66326.html PD166326Cat. No.: HY-18010 Cat. No.: HY-118144PCI 29732 is a potent, orally active, reversibleBTK inhibitor with Kapp values of 8.2, 4.6, andi2.5 nM for BTK, Lck and Lyn, respectively. PCI29732 shows only modest inhibitory activityagainst Itk, another Tec family kinase.PD166326 is a pyrid

24、opyrimidine-type inhibitor ofreceptor tyrosine kinases, with IC s of 6 nM and508 nM for Src and Abl, respectively. PD166326exhibits antileukemic activity.Purity: 99.68%Clinical Data: No Development ReportedSize: 10 mM 1 mL, 5 mg, 10 mg, 50 mg, 100 mgPurity: 98%Clinical Data: No Development ReportedS

25、ize: 1 mg, 5 mg HYPERLINK https:/www.MedChemE/triclabendazole-sulfoxide.html Triclabendazole HYPERLINK https:/www.MedChemE/triclabendazole-sulfoxide.html HYPERLINK https:/www.MedChemE/triclabendazole-sulfoxide.html sulfoxide(TCBZ-SO) Cat. No.: HY-136450 HYPERLINK https:/www.MedChemE/triclabendazole-

26、sulfoxide-13c-d3.html Triclabendazole HYPERLINK https:/www.MedChemE/triclabendazole-sulfoxide-13c-d3.html HYPERLINK https:/www.MedChemE/triclabendazole-sulfoxide-13c-d3.html sulfoxide-13C,d3(TCBZ-SO-13C,d3) Cat. No.: HY-136450S1Triclabendazole sulfoxide (TCBZ-SO) is the mainplasma metabolite of Tric

27、labendazole, and exhibitsanti-parasite effects. Triclabendazole sulfoxidecan inhibit membrane transporter ABCG2/BCRP.Triclabendazole sulfoxide-13C,d3 is the 13C- anddeuterium labeled. Triclabendazole sulfoxide(TCBZ-SO) is the main plasma metabolite ofTriclabendazole, and exhibits anti-parasiteeffect

28、s. Triclabendazole sulfoxide can inhibitmembrane transporter ABCG2/BCRP.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/triclabendazole-sulfoxide-d3.html Triclabendazole HYPERLINK https:/

29、www.MedChemE/triclabendazole-sulfoxide-d3.html HYPERLINK https:/www.MedChemE/triclabendazole-sulfoxide-d3.html sulfoxide-d3 HYPERLINK https:/www.MedChemE/triclabendazole-sulfoxide-d3.html HYPERLINK https:/www.MedChemE/ur-mb108.html UR-MB108(TCBZ-SO-d3) Cat. No.: HY-136450SCat. No.: HY-146676Triclabe

30、ndazole sulfoxide-d3 (TCBZ-SO-d3) is thedeuterium labeled Triclabendazole sulfoxide.Triclabendazole sulfoxide (TCBZ-SO) is the mainplasma metabolite of Triclabendazole, and exhibitsanti-parasite effects. Triclabendazole sulfoxidecan inhibit membrane transporter ABCG2/BCRP.UR-MB108 (Compound 57) is a

31、 potent, selectiveABCG2 (BCRP) inhibitor with an IC of 79 nM.50UR-MB108 is stable in blood plasma.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/YHO-13177.html YHO-13177 HYPERLINK https:

32、/www.MedChemE/YHO-13177.html HYPERLINK https:/www.MedChemE/YHO-13351.html YHO-13351Cat. No.: HY-12757 Cat. No.: HY-12758YHO-13177 is a potent and specific inhibitor ofBCRP; potentiated the cytotoxicity of SN-38 incancer cells and no effect onP-glycoproteinmediated paclitaxel resistance inMDR1-transduced human leukemia K562 cells.YHO-13351 is the prodrug of YHO-13177, which is apotent and specific inhib