| KATSE # | Lebitso la Sehlahiswa | Tlhaloso |
| CPD100654 | PD-169316 | PD-169316 ke inhibitor e khethiloeng ea p38 MAPK. E thibela p38 MAPK ka IC50 ea 89 nM. PD169316, e thibela ho fetoha ha sekhahla sa kholo ea beta-induced Smad signing liseleng tsa mofetše oa mae a motho. |
| CPD100653 | LDN-193189 | LDN193189 ke molek'hule e nyane ea BMP inhibitor e matla haholo e nang le IC50 ea 5 le 30 nM bakeng sa ALK2 le ALK3, ka ho latellana. LDN193189 e boetse e thibela li-receptor tsa mofuta oa BMP ALK6 (TGFβ1 / BMP pontšo) le phosphorylation ea SMAD e latelang. |
| CPD100652 | K02288 | K02288 ke inhibitor e matla ea matšoao a BMP. K02288 e na le ts'ebetso ea in vitro khahlano le ALK2 maemong a tlase a nanomolar a tšoanang le motsoako oa hona joale oa lead LDN-193189. K02288 e ile ea thibela ka ho hlaka tsela ea Smad e susumetsoang ke BMP ntle le ho ama pontšo ea TGF-β le ho susumetsa dorsalization ea li-embryos tsa zebrafish. |
| CPD100650 | SB-431542 | SB-431542 ke "inhibitor" e nyane ea molek'hule ea mofuta oa I TGF-beta receptor, holim'a phanele ea mela e kotsi ea lisele tsa glioma. SB-431542 e thibetse phosphorylation le phetisetso ea nyutlelie ea li-SMAD, li-intercellular mediators tsa pontšo ea TGF-beta, ka mongolo o fokotsehileng oa TGF-beta-mediated. Ho feta moo, SB-431542 e ile ea thibela polelo ea liphello tse peli tsa bohlokoa tsa TGF-beta-vascular endothelial growth factor le plasminogen activator inhibitor-1. |
| CPD100649 | GW788388 | GW788388 ke TGF-beta mofuta oa I receptor inhibitor e ncha e nang le boemo bo ntlafetseng ba pharmacokinetic ha bo bapisoa le SB431542. Re ithutile phello ea eona ka har'a vitro mme ra fumana hore e thibela ka bobeli ts'ebetso ea TGF-beta ea mofuta oa I le mofuta oa II receptor kinase, empa eseng ea mofuta o amanang le morphogenic protein type II receptor. Ho feta moo, e thibetse ts'ebetso ea Smad e hlahisitsoeng ke TGF-beta le polelo ea mofuta oa sepheo, ha e ntse e fokotsa phetoho ea epithelial-mesenchymal le fibrogenesis. |
| CPD100648 | SB-525334 | SB525334 ke inhibitor e matla le e khethang ea phetoho ea kholo-beta1 (TGF-beta1) receptor, activin receptor-like kinase (ALK5). SB525334 e thibetse ts'ebetso ea ALK5 kinase ka IC(50) ea 14.3 nM mme e ne e batla e le matla ka makhetlo a 4 joalo ka inhibitor ea ALK4 (IC(50) = 58.5 nM). SB-525334 e ne e sa sebetse e le inhibitor ea ALK2, ALK3, le ALK6 (IC(50)> 10,000 nM). Litlhahlobong tse thehiloeng ho lisele, SB-525334 (1 microM) e thibetse phosphorylation ea TGF-beta1-induced phosphorylation le translocation ea nyutlelie ea Smad2 / 3 liseleng tsa renal proximal tubule le ho thibela keketseho e bakoang ke TGF-beta1 ho plasminogen activator inhibitor-1 (PAI-1). ) le polelo ea procollagen alpha1(I) mRNA ho A498 lisele tsa renal epithelial carcinoma. |
| CPD100647 | BIBF0775 | BIBF0775 ke inhibitor ea phetoho ea kholo ea β receptor I (TGFβRI). Tlhahlobo ea sebopeho sa X-ray e bonts'itse hore BIBF0775 e kenelletse sebakeng sa kinase sa TGFβRI. |
| CPD100646 | LY3023414 | LY3023414 ke molek'hule e nyenyane e bontšitsoeng ka hare ho vitro e le khetho ea ATP-competitive inhibitor ea PI3Kα le mTOR, DNA-PK, le litho tse ling tsa sehlopha sa I PI3K. In vitro, LY3023414 e bontšitse ts'ebetso ea inhibitory khahlanong le PI3K le mTOR ka lisele tsa tumor, hammoho le ts'ebetso ea antiproliferative le liphello tsa potoloho ea lisele. Ho phaella moo, in vitro, LY3023414 e thibela bokhoni ba PI3K le mTOR ho li-substrates tsa phosphorylate tseleng ea PI3K / mTOR. LY3023414 e ntse e fuputsoa tekong ea kliniki ea mohato oa I. |
| CPD100645 | Onatasertib | CC-223 ke inhibitor e fumanehang ka molomo ea sepheo sa mammalian sa rapamycin (mTOR) se nang le ts'ebetso e ka 'nang ea e-ba teng ea antineoplastic. mTOR kinase inhibitor CC-223 e thibela mosebetsi oa mTOR, e leng se ka 'nang sa fella ka ho kenngoa ha tumor cell apoptosis le ho fokotseha ha ho ata ha lisele tsa tumor. mTOR, serine / threonine kinase e laoloang ka har'a mefuta e sa tšoaneng ea lihlahala, e phetha karolo ea bohlokoa ka tlaase ho tsela ea pontšo ea PI3K/AKT/mTOR, e atisang ho senyeha ka har'a kankere ea batho. |
| CPD100644 | Bimiralisib | Bimiralisib, eo hape e tsejoang ka hore ke PQR309, ke pan inhibitor e ka sebelisoang ka molomo ea phosphoinositide-3-kinases (PI3K) le inhibitor ea sepheo sa mammalian sa rapamycin (mTOR), se nang le ts'ebetso e ka bang teng ea antineoplastic. PI3K/mTOR kinase inhibitor PQR309 e thibela PI3K kinase isoforms alpha, beta, gamma le delta mme, ho isa bohōleng bo fokolang, mTOR kinase, e leng se ka bakang tumor cell apoptosis le ho thibela kholo ho lisele tse fetang PI3K/mTOR. Ts'ebetso ea tsela ea PI3K/mTOR e khothalletsa kholo ea lisele, ho phela, le ho hanyetsa chemotherapy le radiotherapy. |
| CPD100643 | CZ415 | CZ415 ke mTOR inhibitor e matla ea tlholisano ea ATP e nang le khetho e e-so ka e bonoa holim'a kinase efe kapa efe (IC50 = 14.5 nM IC50 bakeng sa pS6RP le 14.8 nM bakeng sa pAKT) e nang le bokhoni bo botle haholo ba ho kenella ha lisele (Kd app = 6.9 nM). Thepa ea Pharmacokinetic ea tumello e itekanetseng le bioavailability e ntle ea molomo e bonts'itse ho lekana ha CZ415 bakeng sa tsoelo-pele ea lithuto tsa vivo. CZ415 e emela molek'hule e loketseng bakeng sa lipatlisiso tsa pharmacological ea karolo ea mTOR pathophysiological vivo. |
| CPD100642 | GDC-0084 | GDC-0084, e tsejoang hape ka hore ke RG7666 le Paxalisib, ke phosphatidylinositol 3-kinase (PI3K) inhibitor e nang le ts'ebetso e ka bang teng ea antineoplastic. PI3K inhibitor GDC-0084 e thibela ka ho khetheha PI3K tseleng ea pontšo ea PI3K/AKT kinase (kapa protheine kinase B), ka tsela eo e thibela ts'ebetso ea tsela ea pontšo ea PI3K. Sena se ka baka tšitiso ea kholo ea lisele le ho phela ho batho ba nang le bokooa ba lisele tsa hlahala. Ho kenya tšebetsong tsela ea PI3K hangata ho amahanngoa le tumorigenesis. |
| CPD100641 | CC-115 | CC-115 ke inhibitor e habeli ea DNA-dependent protein kinase (DNA-PK) le target ea mammalian ea rapamycin (mTOR), e nang le ts'ebetso e ka bang teng ea antineoplastic. CC-115 e tlama le ho thibela ts'ebetso ea DNA-PK le bobeli ba raptor-mTOR (TOR complex 1 kapa TORC1) le rictor-mTOR (TOR complex 2 kapa TORC2), e ka lebisang phokotsong ea ho ata ha lisele tsa kankere tse hlalosang DNA-PK le TOR. DNA-PK, serine/threonine kinase ebile e le setho sa PI3K e amanang le kinase subfamily ea protein kinases, e sebelisoa holim'a tšenyo ea DNA 'me e phetha karolo ea bohlokoa ho lokiseng likheo tsa DNA tse peli ka tsela ea DNA nonnhomologous end joining (NHEJ) . |
| CPD100640 | XL388 | XL388 ke Sehlopha sa Novel sa Li-Inhibitors tse Matla haholo, tse Khethiloeng, tse nang le Tlholisano ea ATP, le tsa molomo tsa Mammalian Target ea Rapamycin (mTOR). XL388 e thibela phosphorylation ea cellular ea mTOR complex 1 (p-p70S6K, pS6, le p-4E-BP1) le mTOR complex 2 (pAKT (S473)) substrates. XL388 e bonts'itse pharmacokinetics e ntle le ho pepeseha ha molomo mefuteng e mengata e nang le bioavailability e itekanetseng. Tsamaiso ea molomo ea XL388 ho litoeba tse hlobotseng tsa athymic tse kenngoeng ka li-tumor xenografts tsa motho li fane ka ts'ebetso e matla ea antitumor e itšetlehileng ka tekanyo. |
| CPD100639 | GDC-0349 | GDC-0349 ke molek'hule e monyane oa lithethefatsi tsa anticaner, e ntseng e ntlafatsoa ke Genentech. Ho tloha ka Phupu 2012, Genentech e kentse teko ea mohato oa pele oa GDC-0349 bakeng sa ho lekola Polokeho le Mamello ea GDC-0349 ho Bakuli ba nang le Lihlahala tse tsoetseng pele kapa tsa Metastatic Solid kapa Non Hodgkin's Lymphoma. |
| CPD100638 | ETP-46464 | ETP46464 ke inhibitor ea DNA damage response kinase Ataxia-telangiectasia mutated (ATM)- and Rad3-related (ATR). |
| CPD100637 | TSELA-600 | WAY-600 ke inhibitor e matla, ea tlholisano ea ATP le e khethang ea mTOR e nang le IC50 ea 9 nM. |
| CPD100636 | WYE-687 | WYE-687 ke inhibitor e matla le ea ATP ea tlholisano le e khethang ea mTOR e nang le IC50 ea 7 nM. |
| CPD100635 | Palomid-529 | Palomid 529, eo hape e tsejoang e le P529, ke buka ea PI3K/Akt/mTOR inhibitor. Palomid 529 (P529) e thibela li-complexes tsa TORC1 le TORC2 'me e bonts'a ho thibela pontšo ea Akt le pontšo ea mTOR ka mokhoa o ts'oanang ka tumor le vasculature. Ho ile ha bontšoa hore P529 e thibela ho hōla ha hlahala, angiogenesis, le ho phunyeha ha methapo ea mali. E bolokile likarolo tse molemo tsa tumor vascular normalization eo rapamycin e ithorisang ka eona. Leha ho le joalo, P529 e bontšitse molemo o eketsehileng oa ho thibela pontšo ea pAktS473 e tsamaellanang le ho thibela TORC2 liseleng tsohle 'me kahoo e feta li-loops tsa maikutlo tse lebisang ho eketseha ha pontšo ea Akt liseleng tse ling tsa tumor. (Mohloli: Cancer Res 008;68(22):9551?–7). |
| CPD100634 | BGT226-maleate | BGT226 ke phosphatidylinositol 3-kinase (PI3K) inhibitor e nang le ts'ebetso e ka bang teng ea antineoplastic. PI3K inhibitor BGT226 e thibela ka ho khetheha PIK3 ho PI3K/AKT kinase (kapa protheine kinase B) tsela ea pontšo, e ka 'nang ea etsa hore ho fetisetsoe cytosolic Bax ho lera la ka ntle la mitochondrial, ho eketsa ho khoneha ha membrane ea mitochondrial; Ho ka 'na ha hlaha lefu la aptotic cell. Bax ke setho sa lelapa la proapoptotic Bcl2 la protheine. |
| CPD100633 | WYE-125132 | WYE-125132, eo hape e tsejoang e le WYE-132, e matla haholo, e na le tlhōlisano ea ATP, le e tobileng mTOR kinase inhibitor (IC(50): 0.19 +/- 0.07 nmol/L; > 5,000-fold selective against PI3Ks). WYE-132 e thibetse mTORC1 le mTORC2 mefuteng e fapaneng ea mofetše in vitro le in vivo. Habohlokoa, ho tsamaellana le phallo ea liphatsa tsa lefutso tsa mTORC2, WYE-132 e lebisitsoeng P-AKT(S473) le ts'ebetso ea AKT ntle le ho fokotsa haholo boemo bo tsitsitseng ba PI3K/PDK1 biomarker P-AKT(T308), e totobatsang taolo e hlahelletseng le e tobileng. AKT ka mTORC2 liseleng tsa mofetše. |
| CPD100632 | Vistusertib | Vistusertib, eo hape e tsejoang e le AZD2014, ke inhibitor e ka sebelisoang ka molomo ea mammalian target ea rapamycin (mTOR) e nang le ts'ebetso e ka 'nang ea e-ba khahlanong le antineoplastic. mTOR kinase inhibitor AZD2014 e thibela mosebetsi oa mTOR, e ka 'nang ea fella ka ho kenngoa ha tumor cell apoptosis le ho fokotseha ha ho ata ha lisele tsa tumor. mTOR, serine / threonine kinase e laoloang ka mefuta e sa tšoaneng ea lihlahala, e phetha karolo ea bohlokoa ka tlaase ho tsela ea pontšo ea PI3K/Akt/mTOR. |
| CPD100631 | WYE-354 | WYE-354 ke inhibitor e matla ea cell-permeable ea mTOR (IC50 = 4.3 nM) e thibelang pontšo ka bobeli ba mTOR complex 1 (mTORC1) le mTORC2. |
| CPD100630 | Gedatolisib | Gedatolisib, eo hape e tsejoang e le PKI-587 le PF-05212384, ke moemeli ea shebileng phosphatidylinositol 3 kinase (PI3K) le sepheo sa mammalian sa rapamycin (mTOR) tseleng ea pontšo ea PI3K/mTOR, e nang le ts'ebetso e ka bang teng ea antineoplastic. Ka tsamaiso ea methapo, PI3K/mTOR kinase inhibitor PKI-587 e thibela bobeli PI3K le mTOR kinases, e leng se ka fellang ka apoptosis le ho thibela kholo ea lisele tsa mofetše ho feta tekano PI3K/mTOR. Ts'ebetso ea tsela ea PI3K / mTOR e khothalletsa kholo ea lisele, ho phela, le ho hanyetsa chemotherapy le radiotherapy; mTOR, serine/threonine kinase e tlase ho PI3K, e kanna ea kengoa tšebetsong ntle le PI3K. |
