Ụlọ Ọrụ Na-ahụ Maka N'Ịntanet, Canada Nweta Ụlọ, European Delivery Delivery

Epacadostat (INCB024360) ntụ ntụ

Rating:
5.00 si 5 dabere na 1 ahịa fim
SKU: 1204669-58-8. Category:

AASraw nwere njikọ na mmepụta site na gram ka usoro nchịkọta nke Epacadostat (INCB024360) ntụ ntụ (1204669-58-8), n'okpuru ụkpụrụ CGMP na usoro nchịkwa mma.

Product Description

Epacadostat (INCB024360) uzuzu uzuzu


Epacadostat (INCB024360) ntụ ntụ Njirimara

aha: Epacadostat (INCB024360) ntụ ntụ
CAS: 1204669-58-8
Molekụla Formula: C11H13BrFN7O4S
Ọbara arọ: 438.23
Melt Point: 151-153 ° C
Nchekwa Nche: -20 Celsius C Freezer
agba: White na-acha ọcha ntụ ntụ


Epacadostat (INCB024360) ntụ ntụ na ojiji

aha

Epacadostat ntụ ntụ; 1 na-emechi IDO; INCB 024360; 1204669-58-8; 1204669-37-3 INCB-024360

Epacadostat ntụ ntụ Usage

Epacadostat ntụ ntụ bụ hydroxyamidine nke nwere ọnụ okwu na onye na-emepụta 2,3-dioxygenase (IDO1), na-enwe ike ịme ihe na-emetụtaghị ya. Epacadostat ntụ ntụ lekwasịrị ma jikọta ya na IDO1, enzyme nke na-ahụ maka oxidation nke tryptophan n'ime kynurenine. Site n'ibido IDO1 ma belata kynurenine na mkpụrụ ndụ tumo, INCB024360 na-abawanye ma weghachite ntanye na mmalite nke mkpụrụ ndụ dịgasị iche iche, gụnyere mkpụrụ ndụ dendritic (DCs), sel NK, na lymphocytes T, yana mmepụta interferon (IFN), na mbelata na mkpụrụ ndụ T regulatory T (Tregs). Ịmalite ọrụ nke usoro ahụ ji alụso ọrịa ọgụ, nke a na-agbanye n'ọtụtụ ọrịa, nwere ike igbochi uto nke IDO1-na-akọwa mkpụrụ ndụ tumo. IDO1 na-egosipụta ọtụtụ ụdị tumor cell na DCs.

E jiriwo ntụ ntụ nke INCB024360 mee ihe n'ule na-amụ banyere ọgwụgwọ HL, Melanoma, Glioblastoma, Mucosal Melanoma, na Ovarian Carcinoma, n'etiti ndị ọzọ.

Ịdọ aka ná ntị na INCB024360 ntụ ntụ

Onyinye data gbaara aka na Incyte kwere na usoro nke ihe Epacadostat ntụ ntụ. Tumors na-emezi ihe dị na nje IDO1 iji zere usoro ahụ. Epacadostat ntụ ntụ na-egbochi enzyme a iji kpochapụ nnwere onwe a, na-enyere usoro ahụ ji alụso ọrịa ọgụ aka imeri ụta na ike zuru ezu ya. Ọ bụ ezie na ịchọrọ data dị mkpa iji gosi nkwenye ahụ, nke ahụ nwere ike ịpụta maka nyocha maka ahịa immuno-oncology.

Ihe ndekọ nke Incyte na-ejikọta nke ọma megide nchikota nke Bristol-Myers 'Opdivo na Yervoy, bụ ndị meriri nkwado FDA ná mmalite afọ gara aga na ike nke PFS nke ọnwa 11.5 na ndị ọrịa na melanoma dị elu.

E nwere ihe ndị mere ị ga-eji chee na obere ihe dị iche n'etiti PFS ga-esi na nsogbu ndị ahụ ga-emesị ghọọ nsụgharị maka Incyte. Usoro ikpe Bristol-Myers debara ndị ọrịa na-agwọ ọrịa, ma ụfọdụ isiokwu dị na Incyte na-emeso ya. Nchịkọta na-elekọta nhụjuanya nke Incyte agaghị enweta PFS ma ọ bụ ọnụego nke isii, ọnwa 12 na 18 na-egosi na ọ bụ na usoro iji mee ka nsonaazụ Opdivo-Yervoy.

Incyte nwekwara ike na-ezo aka na nchekwa nchekwa na-arụ ụka na ya nwere ike mma nke Bristol-Myers. Nwelite ohuru a kwuru na 17% nke ndị ọrịa na-ata ọkwa atọ ma ọ bụ njọ kachasị njọ. Nke ahụ na-atụle nke ọma na nsonaazụ Bristol-Myers kpatara, nke, n'ime mmelite mbụ nke afo a, jikọtara ọnụ ọgụgụ 58% nke ọkwa atọ ma ọ bụ anọ na-emejọ.

Ntuziaka ọzọ

Epacadostat ntụ ntụ bụ onye na-emechi 2,3-dioxygenase 1 (IDO1) na uru IC50 nke NNNUMX nM n'ime mkpụrụ ndụ HeLa nke gosipụtara obere ọrụ megide IDO7.1 enzymes yiri ma ọ bụ tryptophan 2-dioxygenase (TDO) .2,3 E gosipụtara iji kwalite T na mkpụrụ ndụ na-egbu egbu, iji mụbaa mmepụta IFN-γ, na iji belata nsụgharị na usoro T (Treg) dị ka mkpụrụ ndụ na-arụkọ ọrụ nke mkpụrụ ndụ lymphocytes nke mmadụ na mkpụrụ ndụ dendritic ma ọ bụ mkpụrụ ndụ tumo .1 Epacadostat ntụ ntụ pụkwara igbochi ụta na-eto eto na-amị mkpụrụ na-adabere n'ụdị lymphocyte.

Mmiri hydroxyamidine na-ekwu okwu ọnụ na onye na-emepụta ihe na-egosi 2,3-dioxygenase (IDO1), na-enwe ike ịme ihe na-emetụtaghị ya. INCB024360 ntụ ntụ lekwasịrị ma jikọta ya na IDO1, bụ enzyme nke na-ahụ maka oxidation nke tryptophan n'ime kynurenine. Site n'ibido IDO1 na ibelata kynurenine na mkpụrụ ndụ akwara, Epacadostat ntụba na-aba ụba ma weghachite ụba na mmalite nke mkpụrụ ndụ dịgasị iche, gụnyere mkpụrụ ndụ dendritic (DCs), sel NK, na T-lymphocytes, yana mmepụta interferon (IFN), na Mbelata nke mkpụrụ ndụ T (regulatory T) (Tregs). Ịmalite ọrụ nke usoro ahụ ji alụso ọrịa ọgụ, nke a na-agbanye n'ọtụtụ ọrịa, nwere ike igbochi uto nke IDO1-na-akọwa mkpụrụ ndụ tumo. IDO1 na-egosipụta ọtụtụ ụdị tumor cell na DCs. Lelee maka ule na-ahụ maka ahụike na-arụ ọrụ na-eji nke a.

Indoleamine 2,3-dioxygenase 1 (IDO1) bụ mmeghe nkwụnye nsogbu nke na-agbanwe usoro mgbochi mgbochi ahụ site n'ịkwalite ọkpụkpụ T cell usoro iwu na igbochi mmepụta ụbụrụ T, na-eme ka ụbụrụ na-emewanye site n'ikwe ka mkpụrụ ndụ kansa ghara izere nyocha. Epacadostat ntụ ntụ bụ nyocha, onye na-eme ihe na-edozi ahụ nke nje IDO1 nke na-achịkwa ụbụrụ na-adịghịzi enwe microenvironment, si otú ahụ weghachite azịza ndị na-enweghị nchịkwa dị irè. N'ọmụmụ ihe otu, ogwe aka INCB024360 na ndị na-eme nchọpụta na-enweghị nyocha egosiwo ndị na-arịa ọrịa na-adịghị ahụkebe ma ọ bụ metastatic melanoma. N'ime nchọpụta ndị a, INCB024360 ntụ ntụ jikọtara ya na CTLA-4 inhibitor ipilimumab ma ọ bụ PD-1 inhibitor KEYTRUDA mere ka ọnụ ọgụgụ nzaghachi dịkwuo tụnyere nyocha nke ndị na-emechi ihe nkwụnye nsogbu.

Njikọta onye nkedo IDO Epacadostat ntụ ntụ na nivolumab (Opdivo) gosipụtara ihe ịrịba ama nke ọrụ maka ndị ọrịa nwere carcinoma cell carmaoma nke isi na n'olu (SCCHC) na ndị nwere mịkọm, dịka nchọpụta sitere na nchọpụta I / II ECHO-204 na-egosi na nzukọ 2017 ASCO kwa afọ.

Nchikota a gosipụtara usoro nkwụghachi omume (ORR) nke 63% na nzaghachi zuru ezu (CR) nke 5% maka ndị ọrịa na-agwọ ọrịa na-edozi na melanoma, na multi-ogwe aka, ikperede edemede. Na ndị nwere SCCHC, ORR bụ 23% na ọnụego CR bụ 3%. Nchikota abughi ihe di irè na ndi mmadu a na-achoputaghi na oria cancer na ovarian cancer (CRC).

"INCB024360 ntụ ntụ na nivolumab nọ na-arụsi ọrụ ike na phase II melanoma na squamous cell carcinoma nke isi na n'olu," kwuru na ọmụmụ na-eduzi Karl D. Lewis, MD, prọfesọ mmekọrịta, Division nke Medical Oncology, University of Colorado Anschutz Medical Campus. "A hụrụ azịza ọ bụla n'agbanyeghị ọnọdụ PD-L1 na ọnọdụ HPV. Nzaghachi niile na-aga n'ihu na nzere data. "

Na mpaghara m akụkụ nke ọmụmụ, na Epacadostat ntụ ntụ dose mụbara site 25 mg abụọ kwa ụbọchị na 300 mg ugboro abụọ kwa ụbọchị. Na akụkụ II, ndị ọrịa natara 100 mg ugboro abụọ kwa ụbọchị na 300 mg ugboro abụọ kwa ụbọchị Epacadostat ntụ ntụ. Nivolumab ka e nyere na 3 mg / kg kwa izu 2, nke gbanwere na 240 mg IV kwa izu 2 na akụkụ nke II nke ọmụmụ. Ihe nchoputa nke enyere na ASCO maka nchekwa bu site na ihe omumu nke ihe omumu ebe ihe nchoputa nke oma bu site na otu ulo oru II.

Maka ndị ọrịa na-enweghị melanoma (N = 40), ORR nwere nchịkọta 100-mg (n = 6) nke ntụ ntụ INCB024360 bụ 100%, nke gụnyere naanị nzaghachi anya. Site na 300-mg dose (n = 34), ORR bụ 56% na ọnụego CR bụ 6%. Ọnụ ọgụgụ ọrịa ọrịa (DCR; ORR tinyere ọrịa anụ ahụ) bụ 85%. Na ndị nwere PD-L1-positive tumors (n = 7), ORR bụ 71% na 29% na PD-L1-negative group (n = 7). Nzaghachi niile na-aga n'ihu, na ogologo oge nke 16 + izu.

N'akwụkwọ SCCHN, nke ndị ọrịa natara ≤2 tupu usoro ọgwụgwọ ahụ, ORR na dose 100-mg (n = 7) nke Epacadostat ntụ ntụ bụ 14%, enweghị CR, na DCR bụ 61%. Na ogwe aka 300-mg (n = 24), ORR bụ 25%, na 1 CR na DCR nke 71%. Ndị ọrịa na PD-L1-positive tumors (n = 10) nwere ORR nke 30% na ndị na-arịa ọrịa ọjọọ (n = 8) nwere ORR nke 13%. Nzaghachi niile na-aga n'ihu na nyocha, nke nwere ogologo karịa 24 + izu.

N'ime ọrịa 29 ndị nwere ọrịa cancer ovarian, ORR bụ 14% na DCR bụ 31%. E nwere 1 CR na onye ọrịa nwere ọgwụgwọ na-adịghị mma, BRCA-negative, PD-L1-positive disease. Na ndị ọrịa 26 na CRC, ndị nwere nsogbu microsatellite (MSI) nwere ORR nke 25% ma ndị nwere ọrịa anụ ahụ microsatellite adịghị enweta nzaghachi.

"INCB024360 ntụ ntụ na nivolumab egosiputaghi ihe mgbaàmà na-arụ ọrụ n'ime ndị mmadụ na-adịghị ahụ anya nke cancer cancer ovarian na ndị ọrịa CRC," ka Lewis kwuru banyere ihe ọ rụpụtara. Banyere nchọpụta ndị ga-eme n'ọdịnihu, o kwuru na "nchebe mbụ na nrụpụta ọrụ na-ebute aka n'ihu nyocha banyere nivolumab na Epacadostat ntụ ntụ n'ime ndị ọrịa na-agwọ ọrịa na melanoma na ndị ọrịa nwere SCCHN."

Epacadostat Pụrụ Izu

Min iji 10grams.
Ajuju ajuju nke di n'ogo (N'ime 1kg) nwere ike iziputa na 12 awa mgbe ugwo.
Maka usoro ka ukwuu (N'ime 1kg) nwere ike zipụ na 3 ụbọchị ọrụ mgbe ịkwụ ụgwọ.

INCB024360 ntụ ntụ Marketing

A ga-enye ha n'ọdịnihu na-abịa.


Esi zụta Epacadostat ntụ ntụ: zụta INCB024360 ntụ ntụ si AASraw

1.To kpọtụrụ anyị site na email anyị usoro nyocha, ma ọ bụ skypeonye na-ahụ maka ndị ahịa (CSR).
2.To nye anyị ọnụọgụgụ na adreesị gị.
3.OUR CSR ga-enye gị nkọwa, okwu nkwụ ụgwọ, nọmba nchịkọta, ụzọ nnyefe na ụbọchị mbata echere (ETA).
4.Bayment done and the goods will be sent out na 12 awa (N'ihi na iwu n'ime 10kg).
5.Goods natara ma kwuo ihe.


Nkowa gbasara ngwaahịa bara uru,Nabata ebe a.


=

COA

HNMR

Epacadostat (INCB024360) ntụ ntụ (1204669-58-8) hplc ma98% | AASraw

Ezi ntụziaka

Epacadostat Nri ntụ ntụ ntụ ntụ:

Ịjụ ajụjụ maka ndị na - anọchite anya anyị (CSR) maka nkọwa, maka amaokwu gị.

Ntughari & akwukwo akwukwo

Zụrụ Epacadostat (INCB024360) Ntụ ntụ: Nchapụta Nyocha Site na Ihe Ngwọta AASraw