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Epacadostat (INCB024360) ipowder

Akukho kalo
5.00 ngaphandle kwe 5 ngenxa ye 1 ireyithingi abathengi
SKU: 1204669-58-8. Udidi:

I-AASraw ikunye kunye nokukwazi ukuvelisa kwigram ukuya kwi-epacadostat (INCB024360) ipowder (1204669-58-8), phantsi komgaqo weCGMP kunye nolawulo lwekhwalithi ephezulu.

Ingcaciso yeMveliso

Epacadostat (INCB024360) ividiyo ye powder


I-Epacadostat (INCB024360) Iifowuni ze powder

igama: Epacadostat (INCB024360) ipowder
CAS: 1204669-58-8
I-molecular Formula: C11H13BrFN7O4S
Isisindo somzimba: 438.23
Melt Point: 151-153 ° C
Isitoreji sokugcina: -20 ° C Ifreezer
umbala: Umhlophe ukuya kutsho-omhlophe


Epacadostat (INCB024360) ipowder ekusebenziseni

Amagama

Epacadostat powder; IDO inhibitor 1; INCB 024360; 1204669-58-8; 1204669-37-3 INCB-024360

Ukusetyenziswa kwePacadostat powder

I-Epacadostat powder yi-hydroxyamidine yomlomo kunye ne-inhibitor ye-indoleamine i-2,3-dioxygenase (i-IDO1), enezinto ezinokuthi zenze i-immunomodulating kunye ne-antineoplastic. Iithagethi zepacadostat zepowder kwaye zibophezela kwi-IDO1, i-enzyme ejongene ne-oxidation ye-tryptophan ibe yintambo. Ngokumvimbela i-IDO1 kunye nokunciphisa i-kynurenine kwiiseli zesisu, i-INCB024360 iyanda kwaye ibuyisela ukwanda kunye nokusebenza kwamaseli e-immune ahlukeneyo, kuquka amaseli e-dendritic (DCs), iiseli ze-NK kunye ne-T-lymphocytes, kunye ne-interferon (IFN) kunye nokunciphisa kwii-T ezilawulwa zizifo (Tregs) ezilawulwa yi-tumor. Ukuqaliswa kwesistim somzimba, esicinciweyo kwii-kanseri ezininzi, kunokuthintela ukukhula kwee-cells ze-tumor ze-IDO1. I-IDO1 ixhaswa ngokugqithiseleyo ngeentlobo zeentlobo zesununu zee-cell kunye ne-DCs.

I-INCB024360 powder isetyenziswe kwizilingo zokufunda unyango lwe-HL, iMelanoma, i-Glioblastoma, iMelanoma, ne-Ovarian Carcinoma, phakathi kwabanye.

Isixwayiso kwi-INCB024360 powder

Idatha ibolekisa inkolelo ye-Incyte kwindlela yokwenza i-Epacadostat powder. Ukuxhaphaza uhlalutye inzyme ye-IDO1 ukukhusela isistim somzimba. I-Epacadostat powder inqanda le enzyme ukuba idibanise le ntshukumo, ikuncede i-immune system ifuthe i-tumor ngamandla ayo. Ngelixa kudinga ulwazi oluthe xaxa ukuqinisekisa ukuxhomekeka kwezinto, oko kunokuba nefuthe kwi-market for the market.

Idatha ye-Incyte ifakwe kakuhle ngokuhambelana nokuhlanganiswa kweBristol-Myers 'Opdivo kunye neJervoy, eyamkela imvume ye-FDA ekuqaleni konyaka odlulileyo kwi-PFS yeenyanga ze-11.5 kwizigulane ezine-melanoma ephezulu.

Kukho izizathu zokucinga ukuba umehluko okhoyo phakathi kweziphumo ze-PFS kwiimvavanyo zekliniki ekugqibeleni ziya guqulela kwi-Incyte. Uvavanyo lweBristol-Myers lubhalisa izigulane zonyango, kanti ezinye izifundo ezifundwe kwi-Incyte ziye zanyangwa ngaphambili. I-incyte yonyango-ukuhlaselwa kwezinto ezingenakufikelela kwi-PFS kodwa amaxabiso afinyelelwe ezintandathu, iinyanga ze-12 kunye ne-18 zibonisa ukuba kulandelelaniso ukuphucula umphumo we-Opdivo-Yervoy.

I-Incyte ingakhokelela kwakhona kwiinkcukacha zokhuseleko ukuphikisana kwayo inokuthi ibhetele ngakumbi yeBristol-Myers. Ukuhlaziywa kwangoku kuxelelwe i-17% yezigulane zithintela ibanga lesithathu okanye iziganeko ezintle ezichaphazelekayo zonyango. Oku kuqhathaniswa neziphumo eziveliswe ngokuhlanganisana kweBristol-Myers, leyo, ekuhlaziyweni kwangaphambili konyaka, ixhunywe kwizinga le-58% lemigangatho yesithathu okanye eminye imicimbi engathandekiyo.

I mi yalelo

I-Epacadostat powder iyisimo se-indoleamine i-2,3-dioxygenase i-1 (IDO1) kunye nexabiso le-IC50 ye-7.1 nM kwiiseli ze-HeLa ezibonisa umsebenzi omncinci ngokuchasene ne-enzymes ene-IDO2 okanye i-tryptophan 2,3-dioxygenase (TDO) .1 Kuboniswe ukukhuthaza kunye nokukhula kokwemvelo kwamanzi, ukunyusa ukuveliswa kwe-IFN-γ, nokunciphisa ukuguqulwa kwiinkqubo ezilawulwayo (Treg) ezifana ne-Treg) kunye neeseli ze-allogeneic i-lymphocytes ezinomntu kunye neeseli ze-dendritic okanye iiseli ze-tumor.1 Epacadostat powder ingavimbela isisu Ukukhula kwimiba ephethe i-tumor ngendlela exhomekeke kuyo i-lymphocyte.

I-hydroxyamidine ekhoyo ngomlomo kunye ne-inhibitor ye-indoleamine i-2,3-dioxygenase (IDO1), enezinto ezinokuthi zenze i-immunomodulating kunye ne-antineoplastic. I-INCB024360 iithagethi zepowuni kwaye ibophezela kwi-IDO1, i-enzyme ejongene ne-oxidation ye-tryptophan kwi-kynurenine. Ngokumvimbela i-IDO1 kunye nokunciphisa i-kynurenine kwiiseli zesisu, i-epacadostat ikhupha i-powder iphinda ivuselele ukwanda kunye nokusebenza kwamaseli e-immune ahlukeneyo, kuquka amaseli e-dendritic (DCs), iiseli ze-NK kunye ne-T-lymphocyte, kunye ne-interferon (IFN), kunye ukunciphisa iiseli ze-T ezilawulwa zizifo (Tregs). Ukuqaliswa kwesistim somzimba, esicinciweyo kwii-kanseri ezininzi, kunokuthintela ukukhula kwee-cells ze-tumor ze-IDO1. I-IDO1 ixhaswa ngokugqithiseleyo ngeentlobo zeentlobo zesununu zee-cell kunye ne-DCs. Hlola iimvavanyo zekliniki ezisetyenziswayo usebenzisa le nkonzo.

I-Indoleamine i-2,3-dioxygenase i-1 (IDO1) iyinqobo ye-immunosuppressive enzyme eyenza ukuphendula impendulo ye-immune ye-anti-tumor ngokukhuthaza ukuveliswa kwesilwanyana esilawulayo kunye nokukhusela ukusebenza kweseli ye-T, ngaloo ndlela kuququzelela ukukhula kwe-tumor ngokuvumela iiseli zomhlaza ukuba ziphephe ukuvavanywa komzimba. I-epacadostat powder yiphando, inamandla kakhulu kwaye ikhetha inhibitor yomlomo we-IDO1 enzyme elawula i-tumor immune microenvironment, ngaloo ndlela ibuyiselwa iimpendulo ezikhuselweyo ze-immune. Kwiinkalo zengalo-nye, ukudibaniswa kwe-INCB024360 powder kunye ne-immune checkpoint inhibitors uye wabonisa ingqiqo-mbono kwizigulane ezine-melanoma ezingenakulungeleka okanye ezenziwe nge-metastatic melanoma. Kule zifundo, i-INCB024360 powder idibaniswe ne-CTLA-4 inhibitor ipilimumab okanye iP-1 inhibitor KEYTRUDA amazinga okuphendula okuphuculweyo xa kuthelekiswa nezifundo zokhuseleko lokuzivikela ngamajoni omzimba.

Ukudibanisa i-IDO inhibitor I-epacadostat powder kunye nevolumab (i-Opdivo) ibonise iimpawu ezithembisayo zomsebenzi kwizigulane ezine-squamous cell carcinoma yentloko nentamo (SCCHC) kunye nalabo abane-melanoma, ngokwezinto ezifunyenwe kwisigaba se-I / II ECHO-204 I-Annual Meeting 2017 ASCO.

Intsebenziswano iboniswe kwisilinganiselo sokwenza impendulo (ORR) ye-63% kunye neqondo elipheleleyo lempendulo (CR) ye-5% kwizigulane ezine-melanoma yonyango, kwi-arm-multi-trial, i-label-open label. Kulabo abane-SCCHC, i-ORR yayiyi-23% kunye ne-CR rate yayingu-3%. Ukudibanisa kwakungasebenzi kwizigulane ezingakhethiweyo kunye nomhlaza we-ovari kunye nomhlaza we-colorectal (CRC).

"I-INCB024360 powder kunye ne-nivolumab yayisebenza kwi-phase II i-melanoma kunye ne-squamous cell carcinoma yeentloko kunye nentamo yentamo," utshilo u-coauthor uKarl D. Lewis, MD, uprofesa onxulumene naye, uLahlulo lweeNzululwazi lwezoNyango, iYunivesithi yaseColorado Anschutz Medical Campus. "Impendulo yayigcinwe kungakhathaliseki ukuba iP PD-L1 ibinzana kunye ne-HPV. Zonke izimpendulo zaziqhubeka kwi-data cutoff. "

Kwisigaba sam inxalenye yesifundo, i-Epacadostat powder dose yanyuka kwi-25 mg kabini imihla ngemihla ukuya kwi-300 mg kabini imihla ngemihla. Kwiqendu lesigaba II, izigulane zithole i-100 mg kabini imihla ngemihla kwaye i-300 mg kabini i-dose ye-Epacadostat kabini. I-Nivolumab yayisetyenziswa ngokusemthethweni kwi-3 mg / kg nganye iiveki ze-2, ezatshintshelwe kwi-240 mg IV zonke iiveki ze-2 kwisigaba sesi-II sesifundo. Iziphumo ezinikezelwe kwi-ASCO ngokukhuselekileyo zivela kwiingxenye zombini zolu cwaningo ngelixa ukufunyanwa ngempumelelo kuvela kwinqanaba lesigaba II.

Kwizigulane ezingenagqirha i-melanoma (N = 40), i-ORR kunye ne-100-mg dose (n = 6) ye-INCB024360 powder yi-100%, eyayiquka iimpendulo ngokupheleleyo. Nge-dose ye-300-mg (n = 34), i-ORR yayiyi-56% kunye ne-CR rate yayingu-6%. Izinga lokulawula isifo (DCR; ORR kunye nesifo esisigxina) ngu-85%. Kulabo abaneemodumbu ze-PD-L1 (n = 7), i-ORR yayingu-71% ngokubhekiselele kwi-29% kwiqela le-PD-L1-negative (n = 7). Zonke iimpendulo zaqhubeka, kunye nexesha eliphakathi kwee-16 + iveki.

Kwiqela le-SCCHN, apho izigulane zafumene i-≤2 imigca yangaphambili yeyeza, i-ORR kunye ne-100-mg dose (n = 7) ye-epacadostat powder yayingu-14%, kwakungekho i-CRs, kunye ne-DCR yayingu-61%. Ngengalo ye-300-mg (n = 24), i-ORR yayingu 25%, kunye ne-1 CR kunye ne-DCR ye-71%. Izigulane ezine-PD-L1-positive tumors (n = 10) zine-ORR ye-30% kwaye abo abaneengxaki ezimbi (n = 8) babe ne-ORR ye-13%. Zonke iimpendulo zaziqhubekile kuhlalutyo, kunye ne-median ephezulu kuneeyunithi ze-24 +.

Kwi-29 izigulane ezivandlakanywe ngumhlaza we-ovari, i-ORR yayingu-14% kwaye i-DCR yayingu-31%. Kwakukho i-1 CR kwisigulane esinokunyanga, unyango lwe-BRCA, isifo se-PD-L1-positive. Kwizigulane ze-26 ezine-CRC, abo abanokungazinzi kwe-microsatellite (MSI) babe ne-ORR ye-25% kunye nalabo abanezifo ezizinzileyo ze-microsatellite abazange bafumane impendulo.

"I-INCB024360 powder kunye ne-nivolumab ayizange ibonise isalathisi esiphumeleleyo kubantu abangabonwanga ngumhlaza wesi-ovarian kunye nezigulane ze-CRC," kusho uL Lewis. Ngokuphathelele uphando lwexesha elizayo, wathi "ukuphepha kwangaphambili kunye nokuphumelela kweziphumo kukuxhasa uphando nge-nivolumab kunye ne-epacadostat powder kwizigulane zonyango ezine-melanoma kunye nezigulane ezine-SCCHN."

I-Epacadostat Raw Powder

I-10grams encinci.
Uphando malunga nobukhulu obuqhelekileyo (ngaphakathi kwe-1kg) lungathunyelwa kwiiyure ze-12 emva kokuhlawula.
Ukwenza umlinganiselo omkhulu (ngaphakathi kwe-1kg) ungathunyelwa kwimihla yokusebenza ye-3 emva kokuhlawula.

INCB024360 Ukukhishwa kwePowder

Ukubonelelwa kwikamva elizayo.


Indlela yokuthenga i-Epacadostat powder: uthenge i-INCB024360 powder esuka kwi-AASraw

1.Qhagamshelana nathi nge-imeyile yethu inkqubo yophando, okanye i-skype ye-intanethiummeli wenkonzo yamakhasimende (CSR).
2.Ukusibonelela ngobuninzi bakho kunye neadesi.
I-3.I-CSR yethu iya kukunika isingeniso, ixesha lokuhlawula, inombolo yokulandelela, iindlela zokuhambisa kunye nomhla wokufika oqikelelwayo (i-ETA).
I-4.Inkokhelo eyenziwe kwaye iimpahla ziya kuthunyelwa kwiiyure ze-12 (Ukuze ulandelwe ngaphakathi kwe-10kg).
5.Goods zifunyenwe kwaye zinike izimvo.

ISIQINISEKISO NESIBONELELO:

Le nto ithengiselwe uKwenziwa koPhando kuphela. Imigaqo yokuthengisa Faka isicelo. Ayisetyenziselwa uBuntu, okanye oNyango, iZilwanyana, okanye abaNtu.


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I-Epacadostat (INCB024360) ipowder (1204669-58-8) hplc =98% | AASraw

Recipes

I-Epacadostat Raw Powder Recipes:

Ukubuza ummeli wethu ummeli (Representative Representative) (CSR) ngeenkcukacha, ngokubhekiselele kuyo.

Iziqulatho kunye nokuqulunqwa kwemveliso

Thenga i-Epacadostat (INCB024360) Ubuninzi: Ukucima uphando Uphando lwe-AASraw Reagents