| CAT # | Magaca Alaabta | Sharaxaada |
| CPD100654 | PD-169316 | PD-169316 waa horjooge door ah ee p38 MAPK. Waxay ka hortagtaa p38 MAPK leh IC50 ee 89 nM. PD169316, waxay joojisaa isbeddelka isbeddelka koritaanka beta ee Smad ee unugyada kansarka ugxansidaha. |
| CPD100653 | LDN-193189 | LDN193189 waa molecule BMP inhibitor yar oo aad u awood badan leh IC50 ee 5 iyo 30 nM ee ALK2 iyo ALK3, siday u kala horreeyaan. LDN193189 sidoo kale waxay joojisaa nooca BMP I reseptors ALK6 (TGFβ1 / BMP signaling) iyo fosforyaalka SMAD ee xiga. |
| CPD100652 | K02288 | K02288 waa horjooge awood leh ee BMP signaling. K02288 waxay leedahay firfircooni in vitro oo liddi ku ah ALK2 oo ah uruurin hoose oo nanomolar ah oo la mid ah xarunta hadda jirta ee LDN-193189. K02288 waxay si gaar ah u joojisay dariiqa Smad ee ay keentay BMP iyada oo aan saamaynayn TGF-β calaamadinta |
| CPD100650 | SB-431542 | SB-431542 waa horjooge molecule yar oo cusub oo ah nooca I TGF-beta reseptor, oo ku yaal guddi ka mid ah khadadka unugyada glioma malignant bini'aadamka. SB-431542 waxay xannibtay fosforyaalka iyo tarjumaada nukliyeerka ee SMADs, dhexdhexaadiyeyaasha intracellular ee calaamadaynta TGF-beta, iyada oo hoos u dhac ku yimid qoraalka dhexdhexaadinta TGF-beta. Intaa waxaa dheer, SB-431542 waxay joojisay muujinta laba saameyn oo muhiim ah oo ah TGF-beta-vascular endothelial factor factor iyo plasminogen activator inhibitor-1. |
| CPD100649 | GW788388 | GW788388 waa nooc cusub oo TGF-beta I receptor inhibitor oo leh astaan farmaajo oo aad loo horumariyay marka la barbar dhigo SB431542. Waxaan ku barannay saameynteeda in vitro waxaana ogaanay in ay joojisay labadaba TGF-beta nooca I iyo nooca II ee hawlaha kinase reseptor-ka, laakiin maaha mid la xidhiidha nooca borotiinka morphogenic lafaha II. Dheeraad ah, waxay xannibtay firfircoonida TGF-beta ee Smad iyo muujinta hiddo-wadaha bartilmaameedka ah, iyada oo hoos u dhigaysa kala-guurka epithelial-mesenchymal iyo fibrogenesis. |
| CPD100648 | SB-525334 | SB525334 waa horjooge awood leh oo la xushay ee isbeddelka koritaanka factor-beta1 (TGF-beta1) reseptor, activin receptor-like kinase (ALK5). SB525334 waxay joojisay dhaqdhaqaaqa ALK5 kinase IC(50) ee 14.3 nM waxayna ahayd ku dhawaad 4-laab ka awood yar sidii horjooge ALK4 (IC(50) = 58.5 nM). SB-525334 wuxuu ahaa mid aan firfircoonayn sidii horjooge ALK2, ALK3, iyo ALK6 (IC(50)> 10,000 nM). Baaritaannada unugyada ku saleysan, SB-525334 (1 microM) waxay xannibtay fosforyaalka TGF-beta1-ku-soo-baxa iyo beddelka nukliyeerka ee Smad2 / 3 ee unugyada tuubada u dhow ee kelyaha iyo kordhinta TGF-beta1-ku-kordhinta ee plasminogen activator inhibitor-1 (PAI-1) ) iyo procollagen alpha1(I) mRNA muujinta kelyaha A498 unugyada kansarka epithelial. |
| CPD100647 | BIBF0775 | BIBF0775 waa horjoogaha isbeddelka isbeddelka koritaanka β receptor I (TGFβRI). Falanqaynta qaab-dhismeedka raajada ayaa muujisay in BIBF0775 ay ku qooshay qaybta kinase ee TGFβRI |
| CPD100646 | LY3023414 | LY3023414 waa molecule yar oo lagu muujiyay in vitro in uu yahay horjoogaha tartanka ATP-door ee PI3KA iyo mTOR, DNA-PK, iyo xubnaha kale ee qoyska PI3K. In vitro, LY3023414 waxay muujisay waxqabad ka hortag ah oo ka dhan ah PI3K iyo mTOR ee unugyada burooyinka, iyo sidoo kale waxqabadka ka hortagga iyo saameynta wareegga unugyada. Intaa waxaa dheer, in vitro, LY3023414 waxay xannibaysaa awoodda PI3K iyo mTOR inay ku shubaan substrate-ka PI3K/mTOR. LY3023414 waxaa lagu baarayaa tijaabada caafimaadka wajiga I. |
| CPD100645 | Onatasertib | CC-223 waa horjoogaha afka laga heli karo ee bartilmaameedka naasleyda ee rapamycin (mTOR) oo leh firfircoonida antineoplastic ee suurtagalka ah. mTOR kinase inhibitor CC-223 waxay joojisaa dhaqdhaqaaqa mTOR, taas oo laga yaabo inay keento kicinta apoptosis unugyada burooyinka iyo hoos u dhac ku yimaada kororka unugyada burooyinka. mTOR, serine/threonine kinase oo lagu hagaajiyay burooyin kala duwan, ayaa door muhiim ah ka ciyaara dariiqa calaamadaynta PI3K/AKT/mTOR, kaas oo si joogto ah u habaysan kansarrada aadanaha. |
| CPD100644 | Bimiralisib | Bimiralisib, oo sidoo kale loo yaqaan PQR309, waa digsiga afka laga heli karo oo xakameynaya phosphoinotide-3-kinases (PI3K) iyo horjoogaha bartilmaameedka naasleyda ee rapamycin (mTOR), oo leh waxqabad antineoplastic ah. PI3K/mTOR kinase inhibitor PQR309 waxay joojisaa PI3K kinase isoforms alpha, beta, gamma iyo delta iyo, ilaa xad ka yar, mTOR kinase, taas oo keeni karta apoptosis unugyada burooyinka iyo xakameynta koritaanka unugyada si xad dhaaf ah PI3K/mTOR. Firfircoonida dariiqa PI3K/mTOR waxay kor u qaadaa korriinka unugyada, badbaadada, iyo iska caabinta daaweynta kemotherabi iyo shucaaca labadaba. |
| CPD100643 | CZ415 | CZ415 waa awood awood leh oo ATP-tartanka mTOR ah oo leh doorasho aan horay loo arag oo ka duwan kinase kasta (IC50 = 14.5 nM IC50 ee pS6RP iyo 14.8 nM ee pAKT) oo leh awood unug aad u wanaagsan (Kd app = 6.9 nM). Astaamaha dawooyinka ee nadiifinta dhexdhexaadka ah iyo bioavailability afka ee wanaagsan ayaa muujisay ku habboonaanta CZ415 ee horumarka daraasadaha vivo. CZ415 waxay u taagan tahay molecule ku habboon baaritaanka dawooyinka ee doorka pathophysiological mTOR ee vivo. |
| CPD100642 | GDC-0084 | GDC-0084, oo sidoo kale loo yaqaan RG7666 iyo Paxalisib, waa fosfatidylinositol 3-kinase (PI3K) inhibitor oo leh firfircoonida antineoplastic ee suurtagalka ah. PI3K inhibitor GDC-0084 ayaa si gaar ah u xannibaya PI3K ee PI3K/AKT kinase (ama borotiinka kinase B) dariiqa calaamadaynta, taas oo joojinaysa firfircoonida dariiqa calaamadaynta PI3K. Tani waxay keeni kartaa in la joojiyo koritaanka unugyada iyo badbaadada labadaba unugyada unugyada burooyinka. Dhaqdhaqaaqa dariiqa calaamadaynta ee PI3K waxa ay inta badan la xidhiidha burada. |
| CPD100641 | CC-115 | CC-115 waa laba-horjooge ah DNA-ku-tiirsanaanta borotiinka kinase (DNA-PK) iyo bartilmaameedka naasleyda ee rapamycin (mTOR), oo leh waxqabad antineoplastic ah oo suurtagal ah. CC-115 waxay ku xidhan tahay oo joojisaa dhaqdhaqaaqa DNA-PK iyo labadaba raptor-mTOR (TOR complex 1 ama TORC1) iyo rictor-mTOR (TOR complex 2 ama TORC2), taas oo keeni karta hoos u dhac ku yimaada kororka unugyada kansarka ee muujinaya DNA-PK iyo TOR. DNA-PK, serine/threonine kinase iyo xubin ka tirsan qoyska kinase ee la xidhiidha PI3K ee kinases borotiinka, ayaa lagu hawlgeliyay dhaawaca DNA-da wuxuuna door muhiim ah ka ciyaaraa hagaajinta jajabyada DNA-da ee laba-jibbaaran iyada oo loo marayo dariiqa DNA-da ee ku biiritaanka aan-homologous (NHEJ) . |
| CPD100640 | XL388 | XL388 waa Fasalka Novel ee Awood Sare leh, Xulasho, ATP-Tartanka, iyo Ka Hortagga Biyo-nololeedka Afka ah ee Bartilmaameedka Naasleyda ee Rapamycin (mTOR). XL388 waxay joojisay fosforyaalka gacanta ee mTOR complex 1 (p-p70S6K, pS6, iyo p-4E-BP1) iyo mTOR complex 2 (pAKT (S473)) substrates. XL388 wuxuu soo bandhigay farmashiyokinetics wanaagsan iyo soo-gaadhista afka ee noocyo badan oo leh noole dhexdhexaad ah. Maamulka afka ee XL388 ee jiirarka qaawan ee athymic ee lagu dhex beeray buro bini'aadmi xenografts ayaa siisay firfircooni ka hortag ah oo ku-tiirsan oo muhiim ah. |
| CPD100639 | GDC-0349 | GDC-0349 waa musharrax dawada anticaner molecule yar, oo ay soo saartay Genentech. Laga bilaabo Juulaay 2012, Genentech waxay xaraysay wajiga I ee GDC-0349 si ay u qiimeyso Badbaadada iyo Dulqaadashada GDC-0349 ee Bukaanka Maxalli ah ee Horumarsan ama Metastatic Solid Tumors ama Non Hodgkin's Lymphoma. |
| CPD100638 | ETP-46464 | ETP46464 waa horjoogaha jawaabta dhaawaca DNA kinase Ataxia-telangiectasia mutated (ATM) - iyo Rad3 la xiriira (ATR). |
| CPD100637 | WAY-600 | WAY-600 waa mid awood leh, ATP-tartan leh iyo horjooge door ah ee mTOR oo leh IC50 ee 9 nM |
| CPD100636 | WYE-687 | WYE-687 waa mid awood leh oo ATP-tartame leh oo xakameynaya mTOR oo leh IC50 ee 7 nM. |
| CPD100635 | Palomid-529 | Palomid 529, oo sidoo kale loo yaqaan P529, waa PI3K/Akt/mTOR inhibitor cusub. Palomid 529 (P529) waxay joojisaa dhismayaasha TORC1 iyo TORC2 waxayna muujisaa labadaba joojinta calaamadaha Akt iyo mTOR si la mid ah buro iyo xididada xididada. Waxaa la muujiyay in P529 ay joojisay korriinka burooyinka, angiogenesis, iyo qulqulka xididdada. Waxay xajistay dhinacyada faa'iidada leh ee caadiga ah ee xididdada buro ee rapamycin ay ku faanto. Si kastaba ha ahaatee, P529 waxay muujisay faa'iidada dheeraadka ah ee xannibaadda calaamadaha pAktS473 oo la socota xannibaadda TORC2 ee dhammaan unugyada oo sidaas awgeed ka gudubta wareegyada jawaab-celinta taas oo horseedaysa kororka calaamadaha Akt ee unugyada burooyinka qaarkood. (Isha: Kansarka Res 008;68(22):9551?–7). |
| CPD100634 | BGT226-maleate | BGT226 waa fosfatidylinositol 3-kinase (PI3K) inhibitor oo leh firfircoonida antineoplastic ee suurtagalka ah. PI3K inhibitor BGT226 ayaa si gaar ah u xannibaya PIK3 ee PI3K/AKT kinase (ama borotiinka kinase B) dariiqa calaamadaynta, taas oo kicin karta u beddelka cytosolic Bax ee xuubka sare ee mitochondrial, kordhinta xuubka mitochondrial; Dhimashada unugyada apoptotic ayaa iman karta. Bax waa xubin ka tirsan qoyska Bcl2 proapoptotic ee borotiinnada. |
| CPD100633 | WYE-125132 | WYE-125132, oo sidoo kale loo yaqaan WYE-132, waa mid aad u awood badan, ATP-tartan leh, iyo mTOR kinase inhibitor gaar ah (IC(50): 0.19 +/- 0.07 nmol/L;> 5,000-laab la doortay oo ka soo horjeeda PI3Ks). WYE-132 waxay joojisay mTORC1 iyo mTORC2 ee noocyada kansarka ee kala duwan ee vitro iyo in vivo. Muhiimad ahaan, la jaanqaadida hidde-sidaha mTORC2, WYE-132 ee la beegsaday P-AKT (S473) iyo shaqada AKT iyada oo aan si weyn loo dhimin heerka-joogta ah ee PI3K/PDK1 biomarker hawl-maalmeedka P-AKT (T308), oo muujinaya nidaam caan ah oo toos ah ee AKT by mTORC2 ee unugyada kansarka. |
| CPD100632 | Vistusertib | Vistusertib, oo sidoo kale loo yaqaan AZD2014, waa horjoogaha afka laga heli karo ee bartilmaameedka naasleyda ee rapamycin (mTOR) oo leh firfircoonida antineoplastic ee suurtagalka ah. mTOR kinase inhibitor AZD2014 waxay joojisaa dhaqdhaqaaqa mTOR, taas oo laga yaabo inay keento kicinta apoptosis unugga buro iyo hoos u dhac ku yimaada kororka unugyada burooyinka. mTOR, serine/threonine kinase oo lagu hagaajiyay burooyin kala duwan, ayaa door muhiim ah ka ciyaara dariiqa calaamadaynta PI3K/Akt/mTOR. |
| CPD100631 | WYE-354 | WYE-354 waa horjooge awood leh oo unug-fasaara ah ee mTOR (IC50 = 4.3 nM) kaas oo xannibaya calaamadaynta labadaba mTOR complex 1 (mTORC1) iyo mTORC2. |
| CPD100630 | Gedatolisib | Gedatolisib, oo sidoo kale loo yaqaan PKI-587 iyo PF-05212384, waa wakiil beegsanaya fosfatidylinositol 3 kinase (PI3K) iyo bartilmaameedka naasleyda ee rapamycin (mTOR) ee dariiqa calaamadaynta PI3K/mTOR, oo leh firfircoonida antineoplastic. Marka la maamulo xididada, PI3K/mTOR kinase inhibitor PKI-587 waxay joojisaa labadaba PI3K iyo mTOR kinases, taas oo keeni karta apoptosis iyo korriinka koritaanka unugyada kansarka oo si xad dhaaf ah u muujinaya PI3K/mTOR. Firfircoonida dariiqa PI3K/mTOR waxay kor u qaadaa korriinka unugyada, badbaadada, iyo iska caabinta kemotherabi iyo daaweynta shucaaca; mTOR, serine/threonine kinase ka hooseeya ee PI3K, waxa kale oo laga yaabaa in la hawlgeliyo si ka madax bannaan PI3K. |
