| PUSI # | Igoa Oloa | Fa'amatalaga |
| CPD100654 | PD-169316 | O le PD-169316 o se fa'atosina filifilia o le p38 MAPK. E taofia le p38 MAPK ma le IC50 o le 89 nM. PD169316, fa'alavelaveina le suiga o le tuputupu a'e o le fa'ailoga Smad fa'aosoina i totonu o sela o le kanesa o le tagata. |
| CPD100653 | LDN-193189 | LDN193189 o se fa'atosina BMP mole laiti sili ona malosi ma le IC50 o le 5 ma le 30 nM mo ALK2 ma le ALK3, i le faasologa. LDN193189 fa'agata fo'i le BMP ituaiga I fa'afeiloa'i ALK6 (TGFβ1/BMP fa'ailoga) ma le SMAD phosphorylation mulimuli ane. |
| CPD100652 | K02288 | K02288 o se faʻalavelave malosi ole BMP faʻailoga. K02288 ei ai in vitro gaoioiga e faasaga i le ALK2 i le maualalo nanomolar concentrations tutusa ma le taʻitaʻia o loʻo iai nei LDN-193189. K02288 fa'apitoa fa'alavelave le ala Smad fa'aosoina ole BMP e aunoa ma le a'afiaina ole TGF-β fa'ailoga ma fa'aosoina le fa'aosoina ole zebrafish embryos |
| CPD100650 | SB-431542 | O le SB-431542 o se fa'atosina mole mole laiti o le ituaiga I TGF-beta fa'afofoga, i luga o se laulau o laina sela glioma ma'i tagata. O le SB-431542 na poloka le phosphorylation ma le faʻaliliuga faaniukilia o SMADs, mediators intracellular o le TGF-beta faʻailoga, faʻatasi ai ma le faʻaitiitia o le TGF-beta-mediated transcription. E le gata i lea, o le SB-431542 na faʻalavelaveina le faʻaalia o ni mea taua se lua o le TGF-beta-vascular endothelial growth factor ma le plasminogen activator inhibitor-1. |
| CPD100649 | GW788388 | GW788388 o se TGF-beta ituaiga I le faʻaogaina o le faʻaogaina ma se faʻataʻitaʻiga faʻaleleia atili pharmacokinetic faʻatusatusa i le SB431542. Na matou suʻesuʻeina lona aʻafiaga i vitro ma maua ai na faʻalavelave uma le TGF-beta ituaiga I ma le ituaiga II receptor kinase, ae le o le ponaivi morphogenic protein type II receptor. E le gata i lea, na poloka ai le TGF-beta-induced Smad activation ma le faʻaalia o le gene, aʻo faʻaitiitia le suiga o le epithelial-mesenchymal ma le fibrogenesis. |
| CPD100648 | SB-525334 | O le SB525334 o se fa'atosina malosi ma le filifilia o le suiga o le tuputupu aʻe-beta1 (TGF-beta1) tali, activin receptor-like kinase (ALK5). SB525334 faʻasaina le gaioiga ALK5 kinase faʻatasi ma le IC (50) o le 14.3 nM ma e tusa ma le 4-faʻaitiitia le malosi e avea o se inhibitor o le ALK4 (IC (50) = 58.5 nM). SB-525334 sa le galue o se inhibitor o ALK2, ALK3, ma ALK6 (IC(50)> 10,000 nM). I suʻesuʻega faʻavae, SB-525334 (1 microM) na poloka le TGF-beta1-faʻaosoina le phosphorylation ma le faʻaliliuina faaniukilia o Smad2 / 3 i totonu o sela tubule proximal ma faʻalavelaveina le TGF-beta1-faʻateleina le faʻateleina o le plasminogen activator inhibitor-1 (PAI-1). ) ma le procollagen alpha1(I) mRNA faʻamatalaga i le A498 renal epithelial sela o le kanesa. |
| CPD100647 | BIBF0775 | O le BIBF0775 o se faʻalavelave o le suiga o le tuputupu aʻe β receptor I (TGFβRI). O suʻesuʻega o le fausaga o le X-ray na faʻaalia ai o le BIBF0775 na sosolo i totonu o le kinase domain o TGFβRI |
| CPD100646 | LY3023414 | LY3023414 o se mole laʻititi lea na faʻaalia i le vitro e avea o se ATP-faʻatauva faʻatauva filifilia o PI3Kα ma mTOR, DNA-PK, ma isi vasega I PI3K tagata o le aiga. In vitro, LY3023414 ua faʻaalia le faʻaogaina o gaioiga e faasaga i le PI3K ma le mTOR i sela tumo, faʻapea foʻi ma le antiproliferative gaioiga ma aʻafiaga o le taamilosaga. E le gata i lea, i le in vitro, LY3023414 faʻalavelaveina le gafatia o le PI3K ma le mTOR i le phosphorylate substrates i le auala PI3K / mTOR. LY3023414 o lo'o su'esu'eina ile vaega I fa'ata'ita'iga ile falema'i. |
| CPD100645 | Onatasertib | O le CC-223 o se fa'agata avanoa fa'alaua'itele o le fa'amoemoega mamame o le rapamycin (mTOR) fa'atasi ai ma gaioiga antineoplastic. mTOR kinase inhibitor CC-223 faʻalavelaveina le gaioiga a le mTOR, lea e ono mafua ai le faʻaosoina o le apoptosis cell tumo ma le faʻaitiitia o le faʻateleina o le tumo cell. mTOR, o se serine / threonine kinase o loʻo faʻatulafonoina i le tele o tumo, e iai sona sao taua i lalo i le ala faʻailoga PI3K / AKT / mTOR, lea e masani ona faʻaleagaina i gasegase o le tagata. |
| CPD100644 | Bimiralisib | O le Bimiralisib, lea e taʻua foi o le PQR309, o se mea e mafai ona tuʻuina atu i le gutu o le pan inhibitor o phosphoinositide-3-kinases (PI3K) ma le inhibitor o le faʻamoemoega mamame o le rapamycin (mTOR), faʻatasi ai ma gaioiga antineoplastic. PI3K / mTOR kinase inhibitor PQR309 faʻalavelaveina le PI3K kinase isoforms alpha, beta, gamma ma delta ma, i se tulaga laʻititi, mTOR kinase, lea e ono mafua ai le apoptosis cell tumo ma le faʻalavelaveina o le tuputupu aʻe i sela o loʻo faʻaalia le PI3K / mTOR. O le fa'agaoioia o le ala PI3K/mTOR e fa'aolaina ai le tuputupu a'e o sela, ola, ma le tete'e atu i le chemotherapy ma le radiotherapy. |
| CPD100643 | CZ415 | CZ415 o se ATP-fa'atauva mTOR inhibitor malosi ma se filifiliga e le'i tupu muamua i luga o so'o se isi kinase (IC50 = 14.5 nM IC50 mo pS6RP ma le 14.8 nM mo pAKT) fa'atasi ai ma le fa'aogaina lelei tele (Kd app = 6.9 nM). O mea tau vaila'au o le kilia feololo ma le lelei o le tautala tautala na fa'aalia ai le talafeagai o le CZ415 mo le fa'agasolo i su'esu'ega in vivo. CZ415 o loʻo faʻatusalia se mole mole mole suʻesuʻega faʻafomaʻi o le mTOR pathophysiological matafaioi i vivo. |
| CPD100642 | GDC-0084 | GDC-0084, e lauiloa foi o le RG7666 ma Paxalisib, o le phosphatidylinositol 3-kinase (PI3K) inhibitor ma gaioiga antineoplastic gafatia. PI3K inhibitor GDC-0084 faʻapitoa faʻalavelave PI3K i le PI3K / AKT kinase (poʻo le protein kinase B) ala faʻailoga, ma faʻafefe ai le faʻagaoioia o le ala faʻailoga PI3K. E ono i'u ai i le taofiofia o le tuputupu a'e o sela ma le ola i le faitau aofa'i o sela tumo. O le faʻagaoioia o le ala faʻailoga PI3K e masani ona fesoʻotaʻi ma le tumorigenesis. |
| CPD100641 | CC-115 | O le CC-115 o se fa'alavelave fa'alua ole DNA-fa'alagolago i le protein kinase (DNA-PK) ma le fa'amoemoe o le rapamycin (mTOR), fa'atasi ai ma gaioiga antineoplastic. O le CC-115 e fusifusia ma faʻalavelaveina le gaioiga a DNA-PK ma raptor-mTOR (TOR complex 1 poʻo TORC1) ma rictor-mTOR (TOR complex 2 poʻo TORC2), lea e ono mafua ai le faʻaitiitia o le faʻalauteleina o sela o le kanesa e faʻaalia. DNA-PK ma TOR. DNA-PK, o se serine/threonine kinase ma se sui ole PI3K-related kinase subfamily of protein kinases, e faʻagaoioia ile faʻaleagaina o le DNA ma e iai sona sao taua i le toe faʻaleleia o faʻamaufaʻailoga faʻalua DNA e ala i le DNA nonhomologous end joining (NHEJ) ala. . |
| CPD100640 | XL388 | XL388 ose Vasega Tala o le Mamana, Filifilia, ATP-Fa'atauva, ma Fa'aola Fa'aola Fa'atosina o le Mammalian Target of Rapamycin (mTOR). XL388 faʻasaina phosphorylation cellular o mTOR complex 1 (p-p70S6K, pS6, ma p-4E-BP1) ma mTOR complex 2 (pAKT (S473)) substrates. XL388 na fa'aalia lelei pharmacokinetics ma fa'aaliga tautala i le tele o ituaiga ma le fa'aogaina lelei o meaola. O le tu'u fofoga ole XL388 ile athymic nude isumu fa'atūina i le tumo o tagata xenografts e maua ai le tele ma le fa'alagolago i fuala'au antitumor gaioiga. |
| CPD100639 | GDC-0349 | GDC-0349 o se sui mole mole anticaner fualaau faasaina, o loʻo atiaʻe e Genentech. E oʻo mai ia Iulai 2012, ua tuʻuina atu e Genentech le vaega I le faʻataʻitaʻiga o le GDC-0349 mo le iloiloina o le Saogalemu ma le Tolerability o le GDC-0349 i Patients with Locally Advanced or Metastatic Solid Tumors poʻo Non Hodgkin's Lymphoma. |
| CPD100638 | ETP-46464 | ETP46464 o se inhibitor o le DNA faaleagaina tali kinase Ataxia-telangiectasia mutated (ATM)- ma Rad3-related (ATR). |
| CPD100637 | AUALA-600 | WAY-600 o se malosi, ATP-faatauva ma fa'aituau filifilia o le mTOR ma le IC50 o le 9 nM |
| CPD100636 | WYE-687 | WYE-687 o se malosi ma ATP-faʻatauvaʻa ma filifili le inhibitor o mTOR ma IC50 o le 7 nM. |
| CPD100635 | Palomid-529 | Palomid 529, e lauiloa foi o le P529, o se tala PI3K / Akt / mTOR inhibitor. Palomid 529 (P529) faʻalavelave faʻalavelave TORC1 ma TORC2 ma faʻaalia uma le faʻasaina o le Akt faʻailoga ma le mTOR faʻailoga tutusa i le tuma ma vasculature. Na faʻaalia o le P529 na faʻalavelaveina le tuputupu aʻe o le tumo, angiogenesis, ma le faʻaogaina o le vascular. O lo'o fa'atumauina ai vaega aoga o le fa'asa'oina o totoga o le tumo lea e fa'amaualuga e rapamycin. Ae ui i lea, o le P529 na faʻaalia ai le faʻaopoopoga o le faʻaogaina o le pAktS473 faʻailoga e ogatasi ma le polokaina o TORC2 i sela uma ma faʻapea ona faʻafefe ai faʻamatalaga faʻaalia e oʻo atu ai i le faʻateleina o le faʻailoga Akt i nisi sela tumo. (Source: Cancer Res 008;68(22):9551?–7). |
| CPD100634 | BGT226-male | BGT226 o le phosphatidylinositol 3-kinase (PI3K) inhibitor ma gaioiga antineoplastic gafatia. PI3K inhibitor BGT226 faʻapitoa faʻalavelave PIK3 i le PI3K / AKT kinase (poʻo le protein kinase B) ala faʻailoga, lea e ono faʻaosoina ai le faʻaliliuina o le cytosolic Bax i le mitochondrial membrane i fafo, faʻateleina le faʻaogaina o le membrane mitochondrial; e ono tula'i mai le oti o sela apoptotic. Bax o se sui o le proapoptotic Bcl2 aiga o polotini. |
| CPD100633 | WYE-125132 | O le WYE-125132, lea e lauiloa foi o le WYE-132, o se mea e sili ona malosi, ATP-faatauva, ma faapitoa mTOR kinase inhibitor (IC(50): 0.19 +/- 0.07 nmol/L; >5,000-filifili filifilia versus PI3Ks). WYE-132 taofia mTORC1 ma mTORC2 i faʻataʻitaʻiga kanesa eseese in vitro ma in vivo. O le mea taua, o loʻo ogatasi ma faʻamaʻi faʻamaʻi o le mTORC2, WYE-132 faʻatatau i le P-AKT (S473) ma le AKT galuega e aunoa ma le faʻaititia tele o le tulaga mautu o le PI3K / PDK1 gaoioiga biomarker P-AKT (T308), faʻamaonia ai se tulafono faʻapitoa ma tuusaʻo. o le AKT e mTORC2 i sela o le kanesa. |
| CPD100632 | Visusertib | Vistusertib, lea e taʻua foi o le AZD2014, o se iniseti o loʻo mafai ona tuʻuina atu i le gutu o le faʻamoemoega o le rapamycin (mTOR) faʻatasi ma gaioiga antineoplastic. mTOR kinase inhibitor AZD2014 faʻalavelaveina le gaioiga a le mTOR, lea e ono mafua ai le faʻaosoina o le apoptosis cell tumo ma le faʻaitiitia o le faʻateleina o le tumo cell. mTOR, o se serine / threonine kinase o loʻo faʻatonutonuina i le tele o tumo, e iai sona sao taua i lalo i le ala faʻailoga PI3K / Akt / mTOR. |
| CPD100631 | WYE-354 | O le WYE-354 o se iniseti malosi e mafai ona faʻaogaina i le sela o le mTOR (IC50 = 4.3 nM) lea e poloka ai faʻailoga e ala i le mTOR complex 1 (mTORC1) ma le mTORC2. |
| CPD100630 | Gedatolisib | Gedatolisib, e lauiloa foi o le PKI-587 ma le PF-05212384, o se sooupu e tulimataʻia le phosphatidylinositol 3 kinase (PI3K) ma le mammalian target o rapamycin (mTOR) i le PI3K / mTOR ala faʻailoga, faʻatasi ai ma gaioiga antineoplastic. I luga o le faʻaogaina o le toto, PI3K / mTOR kinase inhibitor PKI-587 faʻalavelave uma PI3K ma mTOR kinases, lea e ono mafua ai le apoptosis ma le tuputupu aʻe o le kanesa o loʻo faʻaalia le PI3K / mTOR. Fa'agaoioia o le ala PI3K/mTOR e fa'aolaina ai le tuputupu a'e o le sela, ola, ma le tetee atu i le chemotherapy ma le radiotherapy; mTOR, se serine / threonine kinase i lalo ifo o le PI3K, e mafai foi ona faʻagaoioia tutoatasi mai le PI3K. |
