| CAT # | Sunan samfur | Bayani |
| Saukewa: CPD100654 | Saukewa: PD-169316 | PD-169316 mai zaɓin mai hanawa na p38 MAPK. Yana hana p38 MAPK tare da IC50 na 89 nM. PD169316, yana hana canza yanayin haɓakar beta-induced siginar Smad a cikin ƙwayoyin kansar ovarian ɗan adam. |
| Saukewa: CPD100653 | LDN-193189 | LDN193189 shine mai hana ƙananan ƙwayoyin ƙwayoyin BMP mai ƙarfi tare da IC50 na 5 da 30 nM don ALK2 da ALK3, bi da bi. LDN193189 kuma yana hana nau'in BMP nau'in I masu karɓa ALK6 (TGFβ1 / BMP siginar) da kuma SMAD phosphorylation na gaba. |
| Saukewa: CPD100652 | K02288 | K02288 babban mai hana siginar BMP ne. K02288 yana da in vitro aiki a kan ALK2 a ƙananan ƙididdiga na nanomolar kama da na yanzu gubar fili LDN-193189. K02288 musamman ya hana hanyar Smad da BMP ta haifar ba tare da shafar siginar TGF-β ba da kuma haifar da dorsalization na embryos na zebrafish. |
| Saukewa: CPD100650 | Saukewa: SB-431542 | SB-431542 sabon labari ne mai hana ƙwayoyin ƙwayoyin cuta na nau'in I TGF-beta receptor, akan rukunin layukan ƙwayoyin glioma na ɗan adam. SB-431542 ya toshe phosphorylation da makaman nukiliya na SMADs, masu shiga tsakani na siginar TGF-beta, tare da raguwar fassarar TGF-beta. Bugu da ƙari kuma, SB-431542 ya hana maganganun biyu masu tasiri masu mahimmanci na TGF-beta-vascular endothelial growth factor da plasminogen activator inhibitor-1. |
| Saukewa: CPD100649 | GW788388 | GW788388 sabon TGF-beta nau'in I mai hana mai karɓa ne tare da ingantaccen bayanin martabar harhada magunguna idan aka kwatanta da SB431542. Mun yi nazarin tasirin sa a cikin vitro kuma mun gano cewa ya hana duka nau'in TGF-beta I da nau'in ayyukan kinase mai karɓa na II, amma ba na nau'in nau'in furotin na nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'in nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i nau'i-nau'i). Bugu da ari, ya toshe TGF-beta-induced Smad kunnawa da kuma maƙasudin gene magana, yayin da rage epithelial-mesenchymal mika mulki da fibrogenesis. |
| Saukewa: CPD100648 | Saukewa: SB-525334 | SB525334 shine mai hanawa mai ƙarfi da zaɓi na mai karɓar haɓakar girma-beta1 (TGF-beta1), mai karɓar mai karɓar activin kamar kinase (ALK5). SB525334 ya hana ALK5 kinase aiki tare da IC (50) na 14.3 nM kuma ya kasance kusan 4-ninka ƙasa da ƙarfi a matsayin mai hana ALK4 (IC (50) = 58.5 nM). SB-525334 baya aiki azaman mai hana ALK2, ALK3, da ALK6 (IC(50)> 10,000 nM). A cikin gwaje-gwaje na tushen tantanin halitta, SB-525334 (1 microM) ya toshe TGF-beta1-induced phosphorylation da makaman nukiliya na Smad2/3 a cikin sel proximal tubule na koda da kuma hana TGF-beta1-induced karuwa a cikin plasminogen activator inhibitor-1 (PAI-1). ) da procollagen alpha1(I) mRNA magana a cikin A498 renal epithelial carcinoma cell. |
| Saukewa: CPD100647 | BIBF0775 | BIBF0775 mai hanawa ne na mai canza girma factor β receptor I (TGFβRI). Binciken tsarin X-ray ya nuna cewa BIBF0775 ya jike cikin yankin kinase na TGFβRI |
| Saukewa: CPD100646 | Saukewa: LY3023414 | LY3023414 ƙaramin kwayoyin halitta ne wanda aka nuna a cikin vitro don zama zaɓi na ATP-gasar inhibitor na PI3KA da mTOR, DNA-PK, da sauran dangin I PI3K na aji. A cikin vitro, LY3023414 ya nuna aikin hanawa akan PI3K da mTOR a cikin ƙwayoyin tumor, da kuma aikin antiproliferative da tasirin sake zagayowar tantanin halitta. Bugu da ƙari, in vitro, LY3023414 yana hana ikon PI3K da mTOR zuwa phosphorylate substrates a cikin hanyar PI3K/mTOR. Ana binciken LY3023414 a cikin gwaji na asibiti na lokaci na. |
| Saukewa: CPD100645 | Onatasertib | CC-223 shine mai hanawa ta baki na mammalian hari na rapamycin (mTOR) tare da yuwuwar aikin antineoplastic. mTOR kinase inhibitor CC-223 ya hana aikin mTOR, wanda zai iya haifar da ƙaddamar da ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar kuma kuma ta haifar da apoptosis na ciwon daji. mTOR, serine / threonine kinase wanda aka haɓaka a cikin nau'in ciwace-ciwacen ƙwayoyi, yana taka muhimmiyar rawa a cikin hanyar siginar PI3K / AKT / mTOR, wanda akai-akai dysregulated a cikin ciwon daji na mutum. |
| Saukewa: CPD100644 | Bimiralisib | Bimiralisib, wanda kuma aka sani da PQR309, shine mai hana kwanon rufi na baki na phosphoinotide-3-kinases (PI3K) kuma mai hana mammalian hari na rapamycin (mTOR), tare da yuwuwar aikin antineoplastic. PI3K/mTOR kinase inhibitor PQR309 yana hana PI3K kinase isoforms alpha, beta, gamma da delta kuma, zuwa ƙarami, mTOR kinase, wanda zai iya haifar da ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar cuta PI3K/mTOR. Kunna hanyar PI3K/mTOR yana haɓaka haɓakar tantanin halitta, rayuwa, da juriya ga duka chemotherapy da radiotherapy. |
| Saukewa: CPD100643 | CZ415 | CZ415 shine mai hanawa na ATP-gasar mTOR tare da zaɓin da ba a taɓa gani ba akan kowane kinase (IC50 = 14.5 nM IC50 don pS6RP da 14.8 nM don pAKT) tare da ingantaccen iyawar salula (Kd app = 6.9 nM). Pharmacokinetic kaddarorin na matsakaiciyar sharewa da kyakkyawan yanayin rayuwa na baka sun nuna dacewa da CZ415 don ci gaba zuwa karatun vivo. CZ415 yana wakiltar ingantaccen kwayoyin halitta don binciken harhada magunguna na mTOR pathophysiological rawar a cikin vivo. |
| Saukewa: CPD100642 | Saukewa: GDC-0084 | GDC-0084, kuma aka sani da RG7666 da Paxalisib, mai hana phosphatidylinositol 3-kinase (PI3K) tare da yuwuwar aikin antineoplastic. Mai hana PI3K GDC-0084 musamman yana hana PI3K a cikin hanyar siginar PI3K/AKT kinase (ko protein kinase B), ta haka yana hana kunna hanyar siginar PI3K. Wannan na iya haifar da hana ci gaban tantanin halitta biyu da kuma rayuwa a cikin yawan ƙwayar ƙwayar cuta mai rauni. Kunna hanyar siginar PI3K ana danganta shi akai-akai tare da tumarigenesis. |
| Saukewa: CPD100641 | Saukewa: CC-115 | CC-115 mai hanawa dual inhibitor na DNA-dependant protein kinase (DNA-PK) da mammalian hari na rapamycin (mTOR), tare da yuwuwar aikin antineoplastic. CC-115 yana ɗaure da kuma hana ayyukan DNA-PK da duka raptor-mTOR (TOR complex 1 ko TORC1) da rictor-mTOR (TOR complex 2 ko TORC2), wanda zai iya haifar da raguwar haɓakar salula na ƙwayoyin kansa. DNA-PK da TOR. DNA-PK, serine/threonine kinase kuma memba na dangin kinase mai alaƙa da PI3K na furotin kinases, ana kunna shi akan lalacewar DNA kuma yana taka muhimmiyar rawa wajen gyara ɓarnawar DNA guda biyu ta hanyar DNA nonhomologous end joining (NHEJ) hanya. . |
| Saukewa: CPD100640 | XL388 | XL388 Novel Class of Highly Power, Selective, ATP-Competitive, and Oally Bioavailable Inhibitors na Mammalian Target of Rapamycin (mTOR). XL388 ya hana phosphorylation salon salula na mTOR hadaddun 1 (p-p70S6K, pS6, da p-4E-BP1) da mTOR hadaddun 2 (pAKT (S473)) substrates. XL388 ya nuna kyawawan magunguna na magunguna da baka a cikin nau'ikan da yawa tare da daidaitaccen bioavaibability. Gudanar da baka na XL388 zuwa berayen tsiraicin athymic da aka dasa tare da xenografts na ƙwayar cuta na ɗan adam sun ba da gagarumin aiki mai dogaro da ƙwayar cuta. |
| Saukewa: CPD100639 | Saukewa: GDC-0349 | GDC-0349 ƙaramin ɗan takarar maganin ƙwayar cuta ne, wanda Genentech ke haɓakawa. Tun daga watan Yuli 2012, Genentech ya shigar da gwaji na lokaci I na GDC-0349 don kimanta Tsaro da Haƙuri na GDC-0349 a cikin Marasa lafiya Tare da Ci gaba na Gida ko Metastatic Solid Tumors ko Non Hodgkin's Lymphoma. |
| Saukewa: CPD100638 | Saukewa: ETP-46464 | ETP46464 mai hanawa ne na amsawar lalacewar DNA kinase Ataxia-telangiectasia mutated (ATM) da Rad3 mai alaƙa (ATR). |
| Saukewa: CPD100637 | HANYA-600 | WAY-600 mai ƙarfi ne, mai gasa ATP da mai hanawa na mTOR tare da IC50 na 9 nM |
| Saukewa: CPD100636 | WYE-687 | WYE-687 mai ƙarfi ne kuma mai gasa na ATP da mai hanawa na mTOR tare da IC50 na 7 nM. |
| Saukewa: CPD100635 | Palomid-529 | Palomid 529, wanda kuma aka sani da P529, sabon labari ne mai hanawa PI3K/Akt/mTOR. Palomid 529 (P529) yana hana TORC1 da TORC2 hadaddun kuma yana nuna duka hana siginar Akt da siginar mTOR iri ɗaya a cikin ƙari da vasculature. An nuna cewa P529 ya hana ci gaban ƙwayar cuta, angiogenesis, da kuma ƙwayar cuta. Ya riƙe fa'idodi masu fa'ida na daidaitawar jijiyoyin bugun jini wanda rapamycin ke alfahari. Koyaya, P529 ya nuna ƙarin fa'idar toshe siginar pAktS473 daidai da toshe TORC2 a cikin duk sel kuma don haka ketare madaukai na amsawa wanda ke haifar da ƙarar siginar Akt a cikin wasu ƙwayoyin ƙari. (Madogararsa: Ciwon daji Res 008;68(22):9551?–7). |
| Saukewa: CPD100634 | Saukewa: BGT226 | BGT226 shine mai hana phosphatidylinositol 3-kinase (PI3K) tare da yuwuwar aikin antineoplastic. PI3K inhibitor BGT226 musamman yana hana PIK3 a cikin hanyar siginar PI3K/AKT kinase (ko protein kinase B), wanda zai iya haifar da jujjuyawar cytosolic Bax zuwa membrane na mitochondrial na mitochondrial, yana haɓaka haɓakar mitochondrial; Mutuwar sel apoptotic na iya faruwa. Bax memba ne na dangin sunadaran Bcl2 proapoptotic. |
| Saukewa: CPD100633 | Saukewa: 125132 | WYE-125132, wanda kuma aka sani da WYE-132, yana da ƙarfi sosai, ATP-gasa, kuma takamaiman mTOR kinase inhibitor (IC(50): 0.19 +/- 0.07 nmol / L;> 5,000-ninka zaɓi tare da PI3Ks). WYE-132 ya hana mTORC1 da mTORC2 a cikin nau'ikan ciwon daji iri-iri a cikin vitro da in vivo. Mahimmanci, daidai da ƙayyadaddun kwayoyin halitta na mTORC2, WYE-132 da aka yi niyya P-AKT (S473) da aikin AKT ba tare da rage girman matakin matakin PI3K/PDK1 biomarker biomarker P-AKT (T308), yana nuna sanannen tsari kai tsaye. na AKT ta mTORC2 a cikin kwayoyin cutar kansa. |
| Saukewa: CPD100632 | Vistusertib | Vistusertib, wanda kuma aka sani da AZD2014, shine mai hanawa ta baka na bioavailable mai hana mammalian hari na rapamycin (mTOR) tare da yuwuwar aikin antineoplastic. mTOR kinase inhibitor AZD2014 yana hana aikin mTOR, wanda zai iya haifar da ƙaddamar da ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar cuta. mTOR, serine / threonine kinase wanda aka haɓaka a cikin nau'ikan ciwace-ciwacen daji, yana taka muhimmiyar rawa a cikin hanyar siginar PI3K/Akt/mTOR. |
| Saukewa: CPD100631 | WYE-354 | WYE-354 shine mai hanawa mai ƙarfi ta cell-permeable na mTOR (IC50 = 4.3 nM) wanda ke toshe sigina ta hanyar hadaddun mTOR 1 (mTORC1) da mTORC2. |
| Saukewa: CPD100630 | Gedatolisib | Gedatolisib, wanda kuma aka sani da PKI-587 da PF-05212384, wakili ne da ke yin niyya ga phosphatidylinositol 3 kinase (PI3K) da mammalian manufa na rapamycin (mTOR) a cikin hanyar siginar PI3K/mTOR, tare da yuwuwar aikin antineoplastic. Bayan gudanar da intravenous, PI3K/mTOR kinase inhibitor PKI-587 yana hana duka PI3K da mTOR kinases, wanda zai iya haifar da apoptosis da haɓaka haɓakar ƙwayoyin ciwon daji da ke nuna PI3K/mTOR. Kunna hanyar PI3K/mTOR yana haɓaka haɓakar tantanin halitta, rayuwa, da juriya ga chemotherapy da radiotherapy; mTOR, serine/threonine kinase na PI3K, kuma ana iya kunna shi ba tare da PI3K ba. |
