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Epacadostat (INCB024360) phofo

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SKU: 1204669-58-8. Category:

AASraw e na le bokhoni ba tlhahiso ea tlhahiso le tlhahiso ho tloha ho gram ho ea ka taelo e kholo ea Epacadostat (INCB024360) phofo (1204669-58-8), tlas'a taolo ea CGMP le tsamaiso ea mokhoa oa ho laola boleng.

Tlhaloso ea Sehlahisoa

Epacadostat (INCB024360) video ea phofo


Epacadostat (INCB024360) Batho ba sebetsang ka phofo

Name: Epacadostat (INCB024360) phofo
CAS: 1204669-58-8
Molecular Formula: C11H13BrFN7O4S
Boima ba 'mele: 438.23
Melt Point: 151-153 ° C
Temp Temp Storage: -20 ° C Freezer
Color: Tšoeu ho ea phofo e tšoeu


Epacadostat (INCB024360) phofo e sebelisitsoeng

Mabitso

Phofo ea epacadostat; IDO inhibitor 1; INCB 024360; 1204669-58-8; 1204669-37-3 INCB-024360

Tšebeliso ea phofo ea epacadostat

Phala ea epacadostat ke motsoako o fumanehang ka molomo oa hydroxyamidine le inhibitor ea indoleamine 2,3-dioxygenase (IDO1), e nang le mesebetsi e ka 'nang ea e-ba le immunomodulating le antinoplastic. Lipheo tsa phofo ea epacadost mme li tlamella ho IDO1, enzyme e ikarabellang bakeng sa khase ea tryptophan ka kynurenine. Ka ho thibela IDO1 le ho fokotseha ha kynurenine lisele tsa lisele, INCB024360 e eketseha 'me e tsosolosa ho ata le lisebelisoa tsa lisele tse fapaneng tsa' mele, ho kopanyelletsa lisele tsa dendritic (DCs), NK cells, le l-lymphocyte, le lisebelisoa tse fokolang ka lisele tsa T tse tsamaisanang le lithethefatsi (Tregs). Ho ts'ireletsa tsamaiso ea 'mele ea ho itšireletsa mafung, e thibelitsoeng ka kankere e mengata, ho ka thibela kholo ea IDO1-e hlahisang lisele tsa' mele. IDO1 e senyeha haholo ke mefuta e fapa-fapaneng ea liphatsa tsa lefutso le li-DC.

POSO ea INCB024360 e 'nile ea sebelisoa litekong tsa ho tšoaroa ha HL, Melanoma, Glioblastoma, Mucosal Melanoma, le Ovarian Carcinoma, har'a ba bang.

E lemosoa ka phofo ea INCB024360

Data e alima tumelong ea Incyte ka mochine oa ketso ea Epacadostat powder. Lithethefatsi li fetola li-enzyme tsa IDO1 ho qoba sesole sa 'mele. Phofo e phofshoana e thibela enzyme ena hore e fokolise tšenyo ena, ho thusa tsamaiso ea 'mele ea ho itšireletsa mafung hore e otle hlahala ka matla a eona. Le hoja ho na le lintlha tse ling tse hlokahalang ho netefatsa khopolo-taba, e ka 'na ea e-ba le tšusumetso bakeng sa maraka a marang-oncology.

Boitsebiso ba Incyte bo boloka hantle khahlanong le ho kopana ha Bristol-Myers 'Opdivo le Yervoy, e ileng ea hlōla FDA tumello qalong ea selemo se fetileng ka matla a PFS ea likhoeli tsa 11.5 ho bakuli ba melanoma e tsoetseng pele.

Ho na le mabaka a ho nahana phapang e fokolang pakeng tsa PFS ho tsoa litsing tsa meriana ea litleleniki, qetellong e tla fetolela moeli oa Incyte. Tlhahlobo ea Bristol-Myers e ile ea ngolisa bakuli ba nang le phekolo, athe tse ling tsa thuto ea Incyte li kile tsa phekoloa. Incyte ea phekolo ea batho ba bangata ha e sa ntse e tla finyella PFS e tloaelehileng empa lipalo tse fihletsoeng lilemong tse tšeletseng, 12 le 18 li fana ka maikutlo a hore e tla ntlafatsa liphello tsa Opdivo-Yervoy.

Incyte e ka boela ea lebisa tlhokomelo ho data e sireletsehileng ea ho phehisana khang ea eona e ka ntlafatsa ea Bristol-Myers. Litaba tsa morao-rao li tlalehile 17% ea bakuli ba nang le likhaolo tse tharo kapa tse ling tse mpe tse amanang le phekolo. Seo se bapisa liphello tse hlahisoang ke motsoako oa Bristol-Myers, oo, ts'ebetsong pejana selemong sena, o ne o amana le lebelo la 58% la liketsahalo tse tharo kapa tse 'nè tse bohloko.

Litaelo tse ling

Phala ea epacadostate ke inhibitor ea indoleamine 2,3-dioxygenase 1 (IDO1) e nang le lenane la IC50 la 7.1 nM liseleng tsa HeLa tse bonts'ang tšebetso e nyane khahlanong le li-enzyme tse amanang le IDO2 kapa tryptophan 2,3-dioxygenase (TDO) .1 E bontšitsoe ho khothalletsa T le ho bolaea ha tlhaho-lisele, ho eketsa tlhahiso ea IFN-γ, le ho fokotsa phetoho ho lisele tse laoloang tsa T (Treg) tse tsamaisanang le limela tsa allogeneic lymphocyte tse nang le lisele tsa dendritic kapa lisele tsa tumor.XXMUMX Epacadostat powder e ka boela ea thibela hlahala ho hōla litoeba tse nang le litoeele ka mokhoa o itšetlehileng ka lymphocyte.

Motsoako o fumanehang ka molomo oa hydroxyamidine le inhibitor ea indoleamine 2,3-dioxygenase (IDO1), e nang le mesebetsi e ka 'nang ea e-ba le immunomodulating le antinoplastic. Likarolo tsa phofo tsa INCB024360 mme li tlamella ho IDO1, enzyme e ikarabellang bakeng sa khase ea tryptophan ka kynurenine. Ka ho thibela IDO1 le ho fokotseha ha kynurenine lisele tsa lisele, ho eketseha ha phofo ea Epacadostat le ho tsosolosa ho ata le lisebelisoa tse sa tšoaneng tsa 'mele oa ho itšireletsa mafung, ho akarelletsa le lisele tsa dendritic (DCs), NK cells, le T-lymphocyte, hammoho le tlhahiso ea interferon (IFN), le ho fokotseha ha lisele tsa T tse amanang le likokoana-hloko (Tregs). Ho ts'ireletsa tsamaiso ea 'mele ea ho itšireletsa mafung, e thibelitsoeng ka kankere e mengata, ho ka thibela kholo ea IDO1-e hlahisang lisele tsa' mele. IDO1 e senyeha haholo ke mefuta e fapa-fapaneng ea liphatsa tsa lefutso le li-DC. Hlahloba liteko tsa kliniki tse sebetsang ho sebelisa moemeli ona.

Indoleamine 2,3-dioxygenase 1 (IDO1) ke sesebelisoa se sebetsang sa immunosuppressive enzyme e ikarabellang ka karabo ea ho itšireletsa mafung khahlanong le kokoana-hloko ka ho khothalletsa ts'ebetso ea T cell le thibelo ea ho thibela lisele tsa cell, e leng se thusang ho hōla ha lisele ka ho lumella lisele tsa kankere hore li qobe ho ts'oaetso ea 'mele. Peso ea epacadostat ke lipatlisiso, e matla haholo ebile e khetholla molomo oa li-enzyme tsa IDO1 e laolang kokoana-hloko ea immune microenvironment, ka tsela eo e tsosolosa likarabo tse sebetsang tsa ho itšireletsa mafung. Ka lithuto tsa matsoho a le mong, motsoako oa INCB024360 powder le immune checkpoint inhibitors o bontšitse mohopolo-bopaki ho bakuli ba nang le melanoma e sa tsitsang kapa ea metastatic. Liphuputsong tsena, phofshoana ea INCB024360 e kopantsoe le CTLA-4 inhibitor ipilimumab kapa PD-1 inhibitor KEYTRUDA likhallelo tsa likarabo tse ntlafetseng ha li bapisoa le liphuputso tsa boitsebiso ba meriana ea ho itšireletsa mafung.

Ho kopanya IDO inhibitor Epacadostat powder le nivolumab (Opdivo) ho bonts'itse matšoao a tšeptjoang a mesebetsi ho bakuli ba nang le squamous cell carcinoma ea hlooho le molala (SCCHC) le ba nang le melanoma, ho ea ka sephetho sa phuputso ea phase I / II ECHO-204 e hlahisitsoeng Seboka sa Selemo le Selemo sa 2017.

Kopano e bonts'itse tekanyo ea ho arabela ka sepheo (ORR) ea 63% le tekanyo e feletseng ea karabo ea (CR) ea 5% bakeng sa bakuli ba nang le melanoma ea kalafo, ka lehlakoreng le lengata, teko e bulehileng. Ho ba nang le SCCHC, ORR e ne e le 23% mme palo ea CR e ne e le 3%. Motsoako o ne o sa atlehe ho bakuli ba nang le kankere ea mahe a bomme le kankere e kholo (CRC).

"Palo ea INCB024360 hammoho le nivolumab e ne e sebetsa mafapheng a II ea melanoma le squamous cell carcinoma ea lihlopha tsa hlooho le molala," ho boletse motlatsi oa thuto ea bitsoang Karl D. Lewis, MD, moprofesa ea kopanelang, Division of Medical Oncology, Univesithi ea Colorado Anschutz Medical Campus. "Karabo e ne e nkoa ho sa tsotellehe polelo ea PD-L1 le boemo ba HPV. Likarabo tsohle li ne li ntse li tsoelapele ho fuputso ea data. "

Karolong eo ke nang le karolo ea thuto, peo ea Epacadostat phofo e ne e eketsehile ho tloha 25 mg ka makhetlo a mabeli letsatsi le leng le le leng ho ea ho 300 mg habeli ka letsatsi. Karolong ea II, bakuli ba fumana mokuli oa 100 ka makhetlo a mabeli letsatsi le leng le le leng le 300 mg ka makhetlo a mabeli letsatsi le leng le le leng ka tekanyo ea Epacadostat. Nakong ea pele Nivolumab e ne e fuoa 3 mg / kg libeke tse ling tse 2, tse fetiselitsoeng ho 240 mg IV libeke tse ling tsa 2 karolong ea II ea thuto. Liphuputso tse hlahisitsoeng ASCO bakeng sa polokeho li tsoa likarolong tse peli tsa thuto ha lintho tse fumanoang ka katleho li tsoa ho sehlopha sa sehlopha sa II feela.

Bakeng sa bakuli ba nang le melanoma e sa tšoaroeng (N = 40), ORR le tekanyo ea 100-mg (n = 6) ea INCB024360 phofo e ne e le 100%, e neng e e-na le likarabo tse fapaneng tsa likarolo. Ka tekanyo ea 300-mg (n = 34), ORR e ne e le 56% mme palo ea CR e ne e le 6%. Lebelo la taolo ea lefu (DCR; ORR hammoho le lefu le tsitsitseng) e ne e le 85%. Ho ba nang le lihlahala tsa PD-L1-positive (n = 7), ORR e ne e le 71% ho ea ho 29% sehlopheng se seng sa PD-L1 (n = 7). Likarabo tsohle li ne li tsoela pele, ka nako e kholo ea libeke tsa 16.

Sehlopheng sa SCCHN, moo bakuli ba neng ba amohetse mekhoa ea pele ea phekolo ea ≤2, ORR le dose ea 100-mg (n = 7) ea Epacadostat powder e ne e le 14%, ho ne ho se na CRs, 'me DCR e ne e le 61%. Ka letsoho la 300-mg (n = 24), ORR e ne e le 25%, e nang le 1 CR le DCR ea 71%. Bakuli ba nang le li-tumor tse ntle tsa PD-L1 (n = 10) ba ne ba e-na le ORR ea 30% mme ba nang le lihlahala tse mpe (n = 8) ba na le ORR ea 13%. Likarabo tsohle li ne li tsoela pele ho hlahlobisoa, ka libeke tse kholo ho feta libeke tsa 24.

Bakeng sa bakuli ba 29 ba hlakileng ba tšoeroeng ke kankere ea maeba, ORR e ne e le 14% 'me DCR e ne e le 31%. Ho ne ho e-na le 1 CR ho mokuli ea nang le phekolo ea ho kula, lefu la BRCA-negative, PD-L1-positive. Bakeng sa bakuli ba 26 ba nang le CRC, ba nang le botsitso ba microsatellite (MSI) ba na le ORR ea 25% mme ba nang le lefu le tsitsitseng la microsatellite ha ba ka ba fumana karabelo.

"Palo ea INCB024360 hammoho le nivolumab ha ea ka ea bontša pontšo e sebetsang ho batho ba sa khethoeng ba kankere ea mahe a mangata le bakuli ba CRC," Lewis o boletse ka liphello. Mabapi le lipatlisiso tsa nakong e tlang, o ile a bolela hore "liphello tsa pele tsa polokeho le katleho li tšehetsa lipatlisiso tse eketsehileng tsa bakuli ba navolumab le Epacadostat bathong ba nang le lefu la melanoma le bakuli ba nang le SCCHN."

Mokelikeli o Raha oa Epakado

Ntho e nyenyane 10grams.
Tlhahlobo ka bongata bo tloaelehileng (ka hare ho 1kg) e ka romeloa lihora tse 12 kamora ho lefa.
Bakeng sa tlhahiso e kholo (ka hare ho 1kg) e ka romeloa ka matsatsi a sebetsang a 3 ka mor'a ts'ebetso.

Khamiso ea phofo ea INCB024360

Ho fanoa nakong e tlang.


Tsela ea ho reka phofo ea Epacadostat: reka palo ea INCB024360 phofo ho tloha ho AASraw

1.To iteanye le rona ka imeile ea rona lenaneo la lipatlisiso, kapa skype ea inthanetengmoemeli oa tšebeletso ea bareki (CSR).
2.To re fane ka lipotso tsa hau le lipotso tsa hau.
3.Our CSR e tla u fa tlhaloso, nako ea ho lefa, nomoro ea ho latela, litsela tsa ho pepa le letsatsi la ho fihla ho fihlela (ETA).
4.Payment e entsoe mme thepa e tla romelloa ka lihora tsa 12 (Ho laela ka hare ho 10kg).
5.Goods e amohetse mme e fana ka litlhaloso.

TLHOKOMELISO LE TLHALOSO:

Boitsebiso bona bo rekisetsoe tšebeliso ea lipatlisiso. Lipehelo tsa thekiso Etsa kopo. Eseng molemong oa tšebeliso ea batho, kapa bongaka, bongaka ba liphoofolo kapa lisebelisoa tsa lapeng.


Lintlha tse ling tse mabapi le lihlahisoa tsa bohlokoa,amohela ho tobetsa mona.


COA

HNMR

Epacadostat (INCB024360) phofo (1204669-58-8) hplc≥98% | AASraw

Recipes

Likokoana-hloko tsa Raw Li-Recipes:

Ho botsa bareki ba rona baemeli ba rona (CSR) bakeng sa lintlha tse eketsehileng, bakeng sa boitsebiso ba hau.

Litlhaloso le lihlahisoa tsa lihlahisoa

Fumana Powder ea Epacadostat (INCB024360): Ho khaola Lipatlisiso ho tswa ho Aasraw Reagents