| CAT # | Izina ryibicuruzwa | Ibisobanuro |
| CPD100654 | PD-169316 | PD-169316 ni inhibitori ya p38 MAPK. Irabuza p38 MAPK hamwe na IC50 ya 89 nM. PD169316, ibuza guhindura ibintu bikura beta-iterwa na Smad amarenga muri selile ya kanseri yintanga. |
| CPD100653 | LDN-193189 | LDN193189 ni molekile ntoya cyane ya BMP inhibitor hamwe na IC50 ya 5 na 30 nM kuri ALK2 na ALK3. LDN193189 irabuza kandi ubwoko bwa BMP kwakirwa ALK6 (ibimenyetso bya TGFβ1 / BMP) hamwe na fosifori ya SMAD ikurikira. |
| CPD100652 | K02288 | K02288 ninzitizi ikomeye yerekana ibimenyetso bya BMP. K02288 ifite ibikorwa bya vitro irwanya ALK2 kumurongo wa nanomolar nkeya isa nubu LDN-193189. K02288 yabujije byumwihariko inzira ya BMP iterwa na Smad inzira itagize ingaruka ku kimenyetso cya TGF-β kandi itera dorsalisation ya insoro zebrafish; |
| CPD100650 | SB-431542 | SB-431542 nigitabo gishya cya molekile inhibitor yubwoko bwa I TGF-beta reseptor, kumurongo wumurongo wa selile mbi ya glioma. SB-431542 yahagaritse fosifora noguhinduranya nucleaire ya SMADs, abahuza hagati yimitsi ya TGF-beta yerekana, hamwe no kugabanuka kwa TGF-beta-mediated. Byongeye kandi, SB-431542 yabujije imvugo yingirakamaro zibiri za TGF-beta-vascular endothelial growth factor na plasminogen activator inhibitor-1. |
| CPD100649 | GW788388 | GW788388 nuburyo bushya bwa TGF-beta ubwoko bwa I reseptor inhibitor hamwe numwirondoro wa farumasi wateye imbere ugereranije na SB431542. Twize ku ngaruka zayo muri vitro dusanga byabujije ibikorwa bya TGF-beta ubwoko bwa I ndetse nubwoko bwa II reseptor kinase, ariko ntabwo aribyo byerekeranye na magufa ya poroteyine yo mu bwoko bwa II yakira. Byongeye kandi, yahagaritse TGF-beta-iterwa na Smad gukora no kwerekana imiterere ya gene, mugihe igabanya inzibacyuho-mesenchymal inzibacyuho na fibrogenez. |
| CPD100648 | SB-525334 | SB525334 ninzitizi ikomeye kandi itoranya ihindura ibintu bikura-beta1 (TGF-beta1) reseptor, reseptor ya enterin imeze nka kinase (ALK5). SB525334 yahagaritse ibikorwa bya ALK5 kinase hamwe na IC (50) ya 14.3 nM kandi yari ifite imbaraga zigera kuri 4 nkeya nkimbaraga za ALK4 (IC (50) = 58.5 nM). SB-525334 ntiyakoraga nka inhibitor ya ALK2, ALK3, na ALK6 (IC (50)> 10,000 nM). Mu bushakashatsi bushingiye ku ngirabuzimafatizo, SB-525334 (1 microM) yahagaritse TGF-beta1 iterwa na fosifora iterwa no guhinduranya nucleaire ya Smad2 / 3 mu ngirabuzimafatizo ya tubule yimpyiko kandi ibuza TGF-beta1 iterwa no kwiyongera kwa plasminogen ukora inhibitor-1 (PAI-1) ) na protollagen alpha1 (I) mRNA imvugo muri A498 impyiko epithelial kanseri. |
| CPD100647 | BIBF0775 | BIBF0775 ni inhibitori yimpinduka zikura β reseptor I (TGFβRI). Isesengura rya X-ray ryerekanye ko BIBF0775 yinjiye muri domaine ya kinase ya TGFβRI |
| CPD100646 | LY3023414 | LY3023414 ni molekile ntoya yerekanwe muri vitro kugirango ibe ihitamo ATP irwanya irwanya PI3Kα na mTOR, ADN-PK, hamwe nabandi bagize umuryango I PI3K. Muri vitro, LY3023414 yerekanye ibikorwa byo kubuza kurwanya PI3K na mTOR mu ngirabuzimafatizo, ndetse n'ibikorwa bya antiproliferative n'ingaruka z'ingirabuzimafatizo. Mubyongeyeho, muri vitro, LY3023414 ibuza ubushobozi bwa PI3K na mTOR kuri substrate ya fosifori mu nzira ya PI3K / mTOR. LY3023414 iri gukorwaho iperereza mugice cya mbere cyamavuriro. |
| CPD100645 | Onatasertib | CC-223 ni umunwa ubuza umunwa inyamaswa z’inyamabere za rapamycine (mTOR) hamwe nibikorwa bya antineoplastique. mTOR kinase inhibitor CC-223 ibuza ibikorwa bya mTOR, bishobora kuvamo kwinjiza kanseri yibibyimba apoptose no kugabanuka kwikwirakwizwa rya selile. mTOR, serine / threonine kinase igengwa nibibyimba bitandukanye, igira uruhare runini kumanuka mumihanda ya PI3K / AKT / mTOR yerekana inzira, ikunze kugabanywa kanseri yabantu. |
| CPD100644 | Bimiralisib | Bimiralisib, izwi kandi ku izina rya PQR309, ni umunwa wa bioavailable pan inhibitor ya fosifinositide-3-kinase (PI3K) kandi ikabuza inyamaswa z’inyamabere kwibasira rapamycine (mTOR), hamwe nibikorwa bya antineoplastique. PI3K / mTOR kinase inhibitor PQR309 ibuza PI3K kinase isoforms alpha, beta, gamma na delta kandi, ku rugero ruto, mTOR kinase, ishobora kuvamo apoptose yibibyimba no kubuza gukura muri selile bikabije PI3K / mTOR. Gukora inzira ya PI3K / mTOR itera gukura kwingirabuzimafatizo, kubaho, no kurwanya imiti ya chimiotherapie na radiotherapi. |
| CPD100643 | CZ415 | C. Imiti ya Pharmacokinetic yuburyo bugaragara hamwe na bioavailability yo mu kanwa yerekanaga ko CZ415 ikwiye kugirango itere imbere mubushakashatsi bwa vivo. CZ415 yerekana molekile nziza yo gukora iperereza rya farumasi uruhare rwa mTOR pathophysiologique muri vivo. |
| CPD100642 | GDC-0084 | GDC-0084, izwi kandi nka RG7666 na Paxalisib, ni fosifatiidilinositol 3-kinase (PI3K) inhibitor ifite ibikorwa bya antineoplastique. PI3K inhibitor GDC-0084 irabuza cyane PI3K mumuhanda wa PI3K / AKT kinase (cyangwa protein kinase B) yerekana inzira, bityo bikabuza gukora inzira ya signal ya PI3K. Ibi birashobora kuvamo kubuza gukura kwakagari no kubaho mubantu bafite ibibyimba byoroshye. Gukora inzira ya PI3K yerekana inzira ikunze guhuzwa na tumorigenez. |
| CPD100641 | CC-115 | CC-115 ni inzitizi zibiri za ADN ziterwa na poroteyine kinase (ADN-PK) hamwe n’inyamabere yibasira rapamycine (mTOR), hamwe nibikorwa bya antineoplastique. CC-115 ihuza kandi ikabuza ibikorwa bya ADN-PK hamwe na raptor-mTOR (TOR complex 1 cyangwa TORC1) hamwe na rictor-mTOR (TOR complex 2 cyangwa TORC2), bishobora gutuma igabanuka ryiyongera rya selile ya kanseri yerekana. ADN-PK na TOR. ADN-PK, serine / threonine kinase akaba n'umwe mu bagize kinase ifitanye isano na PI3K ifitanye isano na poroteyine ya kinase, ikora nyuma yo kwangirika kwa ADN kandi ikagira uruhare runini mu gusana ibice bibiri bya ADN ikoresheje inzira ya ADN idahwitse ihuza (NHEJ). . |
| CPD100640 | XL388 | X. XL388 yabujije fosifora ya selile ya mTOR complex 1 (p-p70S6K, pS6, na p-4E-BP1) hamwe na mTOR complex 2 (pAKT (S473)). XL388 yerekanye imiti myiza ya farumasi no kwerekana umunwa mubwoko bwinshi hamwe na bioavailable igereranije. Ubuyobozi bwo mu kanwa bwa XL388 kugeza imbeba zambaye ubusa zatewe hamwe n’ibibyimba byabantu byatanze ibikorwa byingenzi kandi biterwa na antitumor. |
| CPD100639 | GDC-0349 | GDC-0349 numukandida muto wa molekile anticaner, ikorwa na Genentech. Kuva muri Nyakanga 2012, Genentech yatanze ikizamini cya mbere cya GDC-0349 kugirango isuzume umutekano n’ubworoherane bwa GDC-0349 mu barwayi bafite ibibyimba byateye imbere cyangwa Metastatike ikomeye cyangwa Lymphoma ya Non Hodgkin. |
| CPD100638 | ETP-46464 | ETP46464 ni inzitizi ya ADN yangiza ibyangiritse kinase Ataxia-telangiectasia yahinduwe (ATM) - na Rad3 ifitanye isano (ATR). |
| CPD100637 | INZIRA-600 | INZIRA-600 ni imbaraga, ATP-irushanwa kandi ihitamo inhibitor ya mTOR hamwe na IC50 ya 9 nM |
| CPD100636 | WYE-687 | WYE-687 nimbaraga zikomeye na ATP-irushanwa kandi ihitamo inhibitor ya mTOR hamwe na IC50 ya 7 nM. |
| CPD100635 | Palomid-529 | Palomid 529, izwi kandi nka P529, ni igitabo PI3K / Akt / mTOR inhibitor. Palomid 529 (P529) ibuza ibigo bya TORC1 na TORC2 kandi ikerekana uburyo bwo kubuza ibimenyetso bya Akt na mTOR byerekana kimwe mubyimba na vasculature. Byerekanwe ko P529 yabujije imikurire yikibyimba, angiogenez, hamwe nu mitsi yinjira. Yagumanye ibintu byingirakamaro byikibyimba cyimitsi isanzwe rapamycin yirata. Ariko, P529 yerekanye inyungu zinyongera zo guhagarika ibimenyetso bya pAktS473 bihuye no guhagarika TORC2 mungirangingo zose bityo ukirengagiza ibice byisubiramo bigatuma ibimenyetso bya Akt byiyongera muri selile zimwe na zimwe. (Inkomoko: Kanseri Res 008; 68 (22): 9551? –7). |
| CPD100634 | BGT226-umugabo | BGT226 ni fosifatiidilinositol 3-kinase (PI3K) inhibitor hamwe nibikorwa bya antineoplastique. PI3K inhibitor BGT226 irabuza cyane PIK3 muri PI3K / AKT kinase (cyangwa protein kinase B) inzira yerekana inzira, ishobora gutera guhinduranya Bax ya cytosolike kuri membrane yo hanze ya mitochondial, bikongerera ubwonko bwa mitochondrial membrane; apoptotic selile ishobora gupfa. Bax ni umwe mu bagize umuryango wa poropoptotike Bcl2 ya poroteyine. |
| CPD100633 | WYE-125132 | WYE-125132, izwi kandi ku izina rya WYE-132, ni imbaraga zikomeye, irushanwa rya ATP, kandi yihariye ya mTOR kinase inhibitor (IC (50): 0.19 +/- 0.07 nmol / L;> inshuro 5000 zatoranijwe na PI3Ks). WYE-132 yabujije mTORC1 na mTORC2 muburyo butandukanye bwa kanseri muri vitro no muri vivo. Icy'ingenzi, kijyanye no gukuraho genetike ya mTORC2, WYE-132 yibasiye imikorere ya P-AKT (S473) na AKT bitagabanije cyane urwego ruhamye rwibikorwa bya PI3K / PDK1 biomarker P-AKT (T308), byerekana amabwiriza akomeye kandi ataziguye. ya AKT na mTORC2 muri selile kanseri. |
| CPD100632 | Vistusertib | Vistusertib, izwi kandi nka AZD2014, ni bioavailable yo mu kanwa ibuza inyamaswa z’inyamabere kwibasirwa na rapamycine (mTOR) ishobora gukora antineoplastique. mTOR kinase inhibitor AZD2014 ibuza ibikorwa bya mTOR, bishobora kuvamo kwinjiza kanseri yibibyimba apoptose no kugabanuka kwikwirakwizwa rya selile. mTOR, serine / threonine kinase igenzurwa mubyimba bitandukanye, igira uruhare runini epfo na ruguru muri PI3K / Akt / mTOR yerekana inzira. |
| CPD100631 | WYE-354 | WYE-354 ni ingirabuzimafatizo ikomeye ya mTOR (IC50 = 4.3 nM) ihagarika ibimenyetso binyuze muri mTOR complex 1 (mTORC1) na mTORC2. |
| CPD100630 | Gedatolisib | Gedatolisib, izwi kandi ku izina rya PKI-587 na PF-05212384, ni umukozi wibasiye fosifatiidilinositol 3 kinase (PI3K) hamwe n’inyamabere yibasira rapamycine (mTOR) mu nzira yerekana ibimenyetso bya PI3K / mTOR, hamwe n’ibikorwa bya antineoplastique. Iyo imiyoborere yimitsi, PI3K / mTOR kinase inhibitor PKI-587 ibuza kinase ya PI3K na mTOR, ibyo bikaba bishobora kuviramo apoptose no gukura kwingirangingo za kanseri bikabije PI3K / mTOR. Gukora inzira ya PI3K / mTOR iteza imbere ingirabuzimafatizo, kubaho, no kurwanya chimiotherapie na radiotherapi; mTOR, serine / threonine kinase hepfo ya PI3K, irashobora kandi gukora idashingiye kuri PI3K. |
