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Epacadostat (INCB024360) hmoov

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5.00 tawm ntawm 5 raws li nyob rau 1 neeg ntsuam xyuas
SKU: 1204669-58-8. Qeb:

AASraw yog nrog synthesis thiab muaj peev xwm ua tau los ntawm cov gram kom loj npaum li cas ntawm Epacadostat (INCB024360) hmoov (1204669-58-8), raws li CGMP kev tswj thiab kev tswj cov kev tswj qhov system.

Hauj lwm yam khoom

Epacadostat (INCB024360) hmoov yeeb yaj duab


Epacadostat (INCB024360) hmoov Cim

Lub npe: Epacadostat (INCB024360) hmoov
CAS: 1204669-58-8
Molecular Formula: C11H13BrFN7O4S
Molecular phaus: 438.23
Melt Point: 151-153 ° C
Cia Temp: -20 ° C Freezer
xim: Dawb rau hmoov zoo dawb


Epacadostat (INCB024360) hmoov hauv kev siv

npe

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

Epacadostat hmoov pab

Epacadostat hmoov yog ib qho ncauj lus muaj hydroxyamidine thiab inhibitor ntawm indoleamine 2,3-dioxygenase (IDO1), nrog rau kev tiv thaiv kab mob kev tiv thaiv kab mob thiab antineoplastic. Epacadostat hmoov lub hom phaj thiab khi rau IDO1, tus enzyme lub luag hauj lwm rau oxidation ntawm tryptophan rau hauv kynurenine. Los ntawm inhibiting IDO1 thiab txo qynurenine hauv qog hlwb, INCB024360 tsub kom rov ua dua thiab ua rau cov qoob lag luam ntau, xws li cov kab mob dendritic (DCs), NK hlwb, thiab T-lymphocytes, thiab lwm yam tshuaj interferon (IFN), thiab txo hauv qog-txuam ntxawg T hlwb (Tregs). Ua rau ntawm lub cev, uas yog suppressed nyob rau hauv ntau cov qog nqaij hlav, yuav inhibit qhov kev loj hlob ntawm IDO1-hnov qog hlwb. IDO1 yog overexpressed los ntawm ntau hom qog cell thiab DCs.

INCB024360 hmoov tau siv rau hauv kev tshawb fawb txog kev kho HL, Melanoma, Glioblastoma, Mucosal Melanoma, thiab Ovarian Carcinoma, ntawm lwm tus.

Ceeb toom rau INCB024360 hmoov

Cov ntaub ntawv muab qiv rau Incyte txoj kev ntseeg nyob rau hauv kev txiav txim ntawm Epacadostat hmoov. Cov hlab ntsws upregulate tus IDO1 enzyme mus nraim cev tsis muaj zog. Epacadostat hmoov tsis zoo no enzyme los xauj cov evade no, pab kev tiv thaiv kab mob mus ntaus cov qog nrog nws cov quab yuam tag nrho. Hos cov ntaub ntawv ntau ntxiv yuav tsum tau los xyuas qhov tseeb, uas yuav muaj qhov cuam tshuam rau lub tshuab rau kev lag luam immuno-oncology.

Incyte cov ntaub ntawv pawg tuaj yeem tiv thaiv ua ke ntawm Bristol-Myers 'Opdivo thiab Yervoy, uas tau pom zoo FDA kev pom zoo thaum pib xyoo tas los ntawm lub zog ntawm PFS ntawm 11.5 lub hlis hauv cov neeg mob uas mob siab heev melanoma.

Muaj cov laj thawj xav tias qhov txawv ntawm qhov PFS tau los ntawm qhov kev soj ntsuam yuav kawg txhais mus rau hauv ib qho chaw rau Incyte. Bristol-Myers 'sim cov neeg mob kho mob, tab sis qee qhov kev kawm hauv Incyte txoj kev tshawb no tau raug kho dua. Incyte txoj kev kho mob tsis zoo no tseem tsis tau mus cuag PFS cov nrab tab sis cov nqi tau tiav rau ntawm 6, 12 thiab 18 lub hlis qhia tias nws nyob ntawm txoj kev taug kom zoo dua ntawm qhov kev tshwm sim ntawm Opdivo-Yervoy.

Incyte tseem taw tes rau kev qhia txog kev nyab xeeb kom sib ceg nws txoj kev ua ke yuav zoo dua tuaj ntawm Bristol-Myers. Cov xov xwm tshiab tshaj tawm qhia txog 17% ntawm cov neeg mob tau raug mob rau qib peb los yog loj dua kev kho mob. Qhov sib piv no yog los ntawm Bristol-Myers 'ua ke, uas tau hloov ua ntej dhau xyoo no, tau txuas nrog 58% feem pua ​​ntawm qib peb los yog plaub yam teeb meem.

Cov lus qhia ntxiv

Epacadostat hmoov yog lub inhibitor ntawm indoleamine 2,3-dioxygenase 1 (IDO1) nrog rau tus nqi ntawm 50 nM hauv HeLa hlwb uas ua rau me ntsis kev tawm tsam tiv thaiv cov enzymes IDO7.1 los yog tryptophan 2-dioxygenase (TDO) .2,3 Nws tau pom tias yuav txhawb T thiab kom muaj kev loj hlob ntawm kev hnyuv ntawm lub cev, los tsim cov khoom loj zuj zus ntxiv, thiab kom txo tau cov kev hloov siab tshiab rau T (Treg) -huaj zoo li cov hlwb hauv cov coculture system ntawm tib neeg txhua yam kabmob qog nqaij hlav nrog lub hlwb lossis cov qog nqaij hlav ntawm lub cev.1 Epacadostat hmoov kuj ua rau tus neeg mob kev loj hlob nyob rau hauv cov hlab ntsha-cov kabmob ntawm cov kabmob qog.

Ib qho ncauj lus muaj hydroxyamidine thiab inhibitor ntawm indoleamine 2,3-dioxygenase (IDO1), uas muaj kev tiv thaiv kev txhaj tshuaj tiv thaiv kab mob thiab antineoplastic. INCB024360 hmoov lub hom phaj thiab khi rau IDO1, tus enzyme lub luag hauj lwm rau oxidation ntawm tryptophan rau hauv kynurenine. Los ntawm kev tiv thaiv IDO1 thiab qynurenine hauv qog hlwb, Epacadostat hmoov nce thiab rov ua rau cov qoob lag luam ntau ntxiv, nrog rau cov kab mob hlwb (DCS), NK hlwb, thiab T-lymphocytes, thiab cov tshuaj interferon (IFN), thiab txo qis qau-ntxawg T hlwb (Tregs). Ua rau ntawm lub cev, uas yog suppressed nyob rau hauv ntau cov qog nqaij hlav, yuav inhibit qhov kev loj hlob ntawm IDO1-hnov qog hlwb. IDO1 yog overexpressed los ntawm ntau hom qog cell thiab DCs. Tshawb xyuas cov kev kuaj mob uas siv cov neeg sawv cev no.

Indoleamine 2,3-dioxygenase 1 (IDO1) yog ib qho tseem ceeb ntawm immunosuppressive enzyme uas hloov qhov kev tiv thaiv kab mob tiv thaiv kab mob los ntawm kev txhawb T cell cell thiab thaiv kev txawb T cell, ua li no pab txhawb kev loj hlob ntawm cov kabmob hlwb kom tsis txhob muaj kev tiv thaiv kabmob. Epacadostat hmoov yog ib txoj kev tshawb nrhiav, muaj zog thiab xaiv lub qhov ncauj ntawm tus IDO1 enzyme uas tswj cov qog immune microenvironment, ua kom rov ua tau cov tshuaj tiv thaiv kab mob tsis muaj zog. Hauv kev tshawb xyuas ib leeg, kev sib xyaw ntawm INCB024360 hmoov thiab kev kuaj xyuas kabmob hauv cov neeg ua haujlwm tau pom tias muaj pov thawj-ntawm-cov tswvyim rau cov neeg mob uas tsis sib haum lossis metastatic melanoma. Hauv cov kev tshawb fawb no, INCB024360 hmoov sib xyaw nrog CTLA-4 inhibitor ipilimumab los sis PD-1 inhibitor KEYTRUDA txhim kho cov lus teb sib piv nrog cov kev tshawb fawb ntawm tus neeg kuaj xyuas kev tiv thaiv ib leeg ib leeg.

Ua ke nrog IDO inhibitor Epacadostat hmoov nrog nivolumab (Opdivo) tau qhia tias cov kev mob tshwm sim rau cov neeg mob uas muaj tus neeg mob taub hau thiab caj dab (SCCHC) thiab cov neeg mob melanoma, raws li kev tshawb pom los ntawm theem I / II ECHO-204 txoj kev tshawb xyuas ntawm 2017 ASCO Lub Rooj Sab Laj Txhua Xyoo.

Ua ke nrog pom lub hom phiaj ntawm lub hom phiaj (ORR) ntawm 63% thiab cov lus teb tiav (CR) ntawm 5% rau cov neeg mob cov tshuaj kho mob, qhov ntau txhais caj npab, qhib-daim ntawv lo. Nyob rau hauv cov uas muaj SCCHC, lub ORR yog 23% thiab tus nqi CR yog 3%. Kev sib xyaw ua ke tsis zoo nyob hauv cov neeg mob uas tsis mob hauv kev mob qog nqaij hlav cancer thiab mob qog nqaij hlav cancer (CRC).

"INCB024360 hmoov ntxiv nrog nivolumab tau khiav hauv Phaj II melanoma thiab squamous cell carcinoma ntawm lub taub hau thiab caj dab cohorts," said research coauthor Karl D. Lewis, MD, associate professor, Division of Medical Oncology, University of Colorado Anschutz Medical Campus. "Cov lus teb tau pom los tsis hais txog ntawm PD-L1 kev qhia thiab kev mob HPV. Tag nrho cov lus teb muaj nyob hauv cov ntaub ntawv txiav tawm. "

Hauv seem kuv txoj kev tshawb nrhiav, Epacadostat hmoov koob tau tawm ntawm 25 mg ob zaug ib hnub rau 300 mg ob zaug ib hnub. Nyob hauv theem II, cov neeg mob tau txais 100 mg ob zaug ib hnub thiab 300 mg ob zaug ib hnub twg ntawm Epacadostat hmoov. Nivolumab yog thawj coj ntawm 3 mg / kg txhua lub lim tiam 2, uas tau hloov mus rau 240 mg IV txhua lub lim tiam 2 hauv theem II ntawm txoj kev tshawb no. Cov kev tshawb pom tau los ntawm ASCO kev nyab xeeb yog los ntawm ob feem ntawm txoj kev tshawb nrhiav thaum lub txiaj ntsig kev tshawb pom tau los ntawm qhov theem II pawg.

Rau cov neeg mob uas tsis kho tsis tau melanoma (N = 40), lub ORR nrog 100-mg koob tshuaj (n = 6) ntawm INCB024360 hmoov yog 100%, uas muaj cov lus teb ib nrab. Nrog 300-mg koob tshuaj (n = 34), lub ORR yog 56% thiab tus nqi CR yog 6%. Tus kab mob tswj tus kab mob (DCR; ORR ntxiv ruaj khov) yog 85%. Hauv cov uas muaj cov kab mob PD-L1 zoo (n = 7), lub ORR yog 71% piv rau 29% hauv pawg PD-L1-negative (n = 7). Tag nrho cov lus teb muaj kev sib tham, nrog lub sij hawm nruab nrab ntawm 16 + lub lis piam.

Nyob hauv SCCHN pawg, uas cov neeg mob tau txais ≤2 ua ntej cov kev kho, lub ORR nrog 100-mg koob tshuaj (n = 7) ntawm Epacadostat hmoov yog 14%, tsis muaj CRS, thiab DCR yog 61%. Hauv 300-mg npab (n = 24), lub ORR yog 25%, nrog 1 CR thiab DCR ntawm 71%. Cov neeg mob uas muaj cov hlav PD-L1 zoo (n = 10) muaj ib qho ORR ntawm 30% thiab cov uas tsis zoo hlav (n = 8) muaj ib qho ORR ntawm 13%. Tag nrho cov lus teb tau tshwm sim ntawm qhov kev ntsuam xyuas, nrog ib tug neeg nruab nrab ntau dua 24 + lub lis piam.

Hauv 29 cov neeg mob kuaj mob qog nqaij hlav qe menyuam, lub ORR yog 14% thiab DCR yog 31%. Muaj 1 CR nyob rau hauv ib tug neeg mob uas muaj mob hlav, BRCA-negative, PD-L1 kab mob zoo. Hauv 26 cov neeg mob CRC, cov uas muaj instability tsis txaus (MSI) muaj ib qho ORR ntawm 25% thiab cov uas muaj kab mob hauv cov kab mob microsatellite tsis tau txais kev teb.

"INCB024360 hmoov ntxiv nrog nivolumab tsis pom tias muaj cov teebmeem hauv kev ua haujlwm ntawm cov neeg mob tsis zoo ntawm kev mob kheesxaws ntawm zes qe menyuam thiab CRC cov neeg mob," Lewis tau hais txog qhov kev tshwm sim. Hais txog kev tshawb nrhiav yav tom ntej, nws tau hais tias "qhov muaj kev nyab xeeb thiab ua tau zoo txhawb nqa kev tshawb xyuas ntxiv txog nivolumab thiab Epacadostat hmoov hauv cov neeg mob kho mob uas muaj melanoma thiab rau cov neeg mob SCCHN."

Epacadostat Raw Hmoov

Min yuam 10grams.
Cov lus nug txog ntawm ntau npaum li cas (Hauv 1kg) tuaj yeem xa tawm hauv 12 teev tom qab them nyiaj.
Rau kev loj dua (Hauv 1kg) tuaj yeem xa tawm hauv 3 hnub ua hauj lwm tom qab them nyiaj.

INCB024360 hmoov li

Kom muab rau yav tom ntej tom ntej.


Yuav ua li cas yuav tau Epacadostat hmoov: yuav INCB024360 hmoov los ntawm AASraw

1.To tiv tauj peb ntawm peb tus email nug qhov system, lossis hauv internettus sawv cev rau tus neeg sawv cev (CSR).
2.To muab peb nug koj qhov ntau thiab qhov chaw nyob.
3.Our CSR yuav muab nqe lus hais txog koj, qhov them nqi, tus lej nrhiav, kev xaib thiab kwv yees hnub uas tuaj txog (ETA).
4.Payment ua tiav thiab cov khoom xa tuaj rau 12 cov xuab moos (Rau kev txiav txim hauv 10kg).
5.Goods tau txais thiab muab tswv yim.

PRECAUTION THIAB DISCLAIMER:

Cov Khoom Siv No Yog Muag Rau Kev Tshawb Xyuas Siv Xwb. Cov ntsiab lus ntawm kev muag khoom Thov. Tsis Yog Rau Tib Neeg Noj, Tsis Kho Mob, Kho Tsiaj, lossis Tsev Neeg Siv.


Ntau yam hais txog cov khoom muag,txais tos nias ntawm no.


COA

HNMR

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

Zaub mov txawv

Epacadostat Raw Pluas Noj Zaub:

Yog xav paub txog peb Tus Neeg Sawv Cev Kev Nkag Siab (CSR) kom paub meej, rau qhov koj siv.

References & cov khoom citations

Yuav tsum Epacadostat (INCB024360) Hmoov: Kev Txiav Txim Siab Ntawm Ntiaj Teb Los ntawm AASraw Reagents