| nwamba # | Aha ngwaahịa | Nkọwa |
| CPD100654 | PD-169316 | PD-169316 bụ ihe mgbochi nhọrọ nke p38 MAPK. Ọ na-egbochi p38 MAPK na IC50 nke 89 nM. PD169316, na-egbochi mgbanwe uto ihe beta na-ebute akara Smad na mkpụrụ ndụ kansa ovarian mmadụ. |
| CPD100653 | LDN-193189 | LDN193189 bụ ihe mgbochi obere molekul BMP nwere IC50 nke 5 na 30 nM maka ALK2 na ALK3, n'otu n'otu. LDN193189 na-egbochikwa ụdị BMP ụdị m ndị na-anabata ALK6 (TGFβ1 / BMP na-egosi) na SMAD phosphorylation na-esote. |
| CPD100652 | K02288 | K02288 bụ ihe mgbochi siri ike nke akara BMP. K02288 nwere ọrụ in vitro megide ALK2 na obere nchịkọta nanomolar dị ka nke dị ugbu a nke LDN-193189. K02288 gbochiri ụzọ Smad nke BMP na-ebute na-enweghị emetụta akara TGF-β na ịkpata dorsalization nke embrayo zebrafish. |
| CPD100650 | SB-431542 | SB-431542 bụ obere ihe mgbochi molecule nke ụdị I TGF-beta receptor, na panel nke ahịrị glioma cell ọjọọ mmadụ. SB-431542 gbochiri phosphorylation na ntugharị nuklia nke SMAD, ndị mgbasa ozi intracellular nke akara TGF-beta, yana mbelata ntụgharị mgbasa ozi TGF-beta. Ọzọkwa, SB-431542 gbochiri okwu nke abụọ dị oke mkpa mmetụta nke TGF-beta-vascular endothelial growth factor na plasminogen activator inhibitor-1. |
| CPD100649 | GW788388 | GW788388 bụ TGF-beta ụdị I anabata ihe mgbochi nwere profaịlụ pharmacokinetic emelitere nke ukwuu ma e jiri ya tụnyere SB431542. Anyị mụrụ mmetụta ya na vitro wee chọpụta na ọ na-egbochi ma TGF-beta ụdị I na ụdị II receptor kinase omume, ma ọ bụghị nke ọkpụkpụ morphogenic protein ụdị II nnabata. Ọzọkwa, ọ gbochiri TGF-beta-induced Smad activation na mkpụrụ ndụ mkpụrụ ndụ ebumnuche, ebe ọ na-ebelata ntụgharị epithelial-mesenchymal na fibrogenesis. |
| CPD100648 | SB-525334 | SB525334 bụ onye na-egbochi ike na nhọrọ nke mgbanwe uto-beta1 (TGF-beta1) receptor, activin receptor-like kinase (ALK5). SB525334 gbochiri ALK5 kinase ọrụ na IC (50) nke 14.3 nM ma bụrụ ihe dị ka 4-fold obere ike dị ka onye na-egbochi ALK4 (IC (50) = 58.5 nM). SB-525334 adịghị arụ ọrụ dị ka onye na-egbochi ALK2, ALK3, na ALK6 (IC(50)> 10,000 nM). N'ime nyocha nke sel, SB-525334 (1 microM) gbochiri TGF-beta1-induced phosphorylation na ntughari nuklia nke Smad2/3 na sel proximal tubule na-egbochi TGF-beta1 na-ebute mmụba na plasminogen activator inhibitor-1 (PAI-1). ) na procollagen alpha1 (I) mRNA okwu na A498 renal epithelial carcinoma cell. |
| CPD100647 | BIBF0775 | BIBF0775 bụ onye na-egbochi ihe na-agbanwe uto β receptor I (TGFβRI). Nyocha nhazi usoro X-ray gosiri na BIBF0775 mikpuru n'ime ngalaba kinase nke TGFβRI. |
| CPD100646 | LY3023414 | LY3023414 bụ obere molekul nke egosiri na vitro ka ọ bụrụ onye na-egbochi asọmpi ATP nke PI3KA na mTOR, DNA-PK na ndị otu ezi na ụlọ PI3K ndị ọzọ. Na vitro, LY3023414 egosipụtawo ọrụ mgbochi megide PI3K na mTOR na mkpụrụ ndụ tumo, yana ọrụ mgbochi na mmetụta okirikiri cell. Na mgbakwunye, in vitro, LY3023414 na-egbochi ikike nke PI3K na mTOR na phosphorylate substrates na ụzọ PI3K/mTOR. A na-enyocha LY3023414 n'ime nnwale ụlọ ọgwụ na ngalaba nke mbụ. |
| CPD100645 | Onatasertib | CC-223 bụ onye na-egbochi ọnụ nke ihe anụ mammalian nke rapamycin (mTOR) nwere ọrụ antineoplastic. mTOR kinase inhibitor CC-223 na-egbochi ọrụ nke mTOR, nke nwere ike ịkpata mmalite nke apoptosis tumor cell na mbelata nke mmụba cell tumor. mTOR, serine/threonine kinase nke a na-achịkwa n'ọtụtụ etuto ahụ, na-arụ ọrụ dị mkpa na ala na ụzọ akara PI3K/AKT/mTOR, bụ nke a na-emekarị ka ọ bụrụ ọrịa cancer mmadụ. |
| CPD100644 | Bimiralisib | Bimiralisib, nke a makwaara dị ka PQR309, bụ onye na-egbochi phosphoinotide-3-kinases (PI3K) na onye na-egbochi mammalian target nke rapamycin (mTOR), nwere ọrụ antineoplastic. PI3K/mTOR kinase inhibitor PQR309 na-egbochi PI3K kinase isoforms alpha, beta, gamma na delta na, ruo n'ókè dị nta, mTOR kinase, nke nwere ike ịkpata apoptosis cell tumor na igbochi uto na mkpụrụ ndụ na-egosipụta PI3K/mTOR. Ịgbalite ụzọ PI3K/mTOR na-akwalite uto cell, nlanarị, na iguzogide ma chemotherapy na rediotherapy. |
| CPD100643 | CZ415 | CZ415 bụ onye na-egbochi mTOR asọmpi ATP na-enwetụbeghị ụdị ya karịa kinase ọ bụla (IC50 = 14.5 nM IC50 maka pS6RP na 14.8 nM maka pAKT) nwere ezigbo ikike cell (Kd app = 6.9 nM). Ngwongwo ọgwụ nke pharmacokinetic nke mkpochapụ agafeghị oke yana ezigbo bioavailability ọnụ gosipụtara dabara nke CZ415 maka ịga n'ihu na ọmụmụ vivo. CZ415 na-anọchite anya molekul dị mma maka nyocha ọgwụ gbasara ọrụ mTOR pathophysiological na vivo. |
| CPD100642 | GDC-0084 | GDC-0084, makwaara dị ka RG7666 na Paxalisib, bụ phosphatidylinositol 3-kinase (PI3K) inhibitor nwere ike antineoplastic ọrụ. PI3K inhibitor GDC-0084 na-egbochi kpọmkwem PI3K na PI3K/AKT kinase (ma ọ bụ protein kinase B) ụzọ akara, si otú ahụ na-egbochi mmalite nke ụzọ akara PI3K. Nke a nwere ike bute mgbochi nke ma uto cell na nlanarị n'ime ọnụ ọgụgụ cell tumor nwere ike ime ya. Ịgbalite ụzọ mgbama PI3K na-ejikọtakarị na tumorigenesis. |
| CPD100641 | CC-115 | CC-115 bụ onye na-egbochi DNA-based protein kinase (DNA-PK) yana ebumnuche anụ ahụ nke rapamycin (mTOR), nwere ọrụ antineoplastic nwere ike. CC-115 na-ejikọta ma na-egbochi ọrụ nke DNA-PK na ma raptor-mTOR (TOR complex 1 ma ọ bụ TORC1) na rictor-mTOR (TOR complex 2 ma ọ bụ TORC2), nke nwere ike iduga na mbelata cellular proliferation nke mkpụrụ ndụ cancer na-egosipụta. DNA-PK na TOR. DNA-PK, serine/threonine kinase na onye otu ezinụlọ kinase metụtara PI3K nke protein kinases, na-arụ ọrụ na mmebi DNA ma na-arụ ọrụ dị mkpa n'ịrụzi nkwụsịtụ DNA nwere okpukpu abụọ site na DNA nonhomologous end joining (NHEJ) ụzọ. . |
| CPD100640 | XL388 | XL388 bụ klaasị ọhụụ nke nwere ike dị ukwuu, nhọrọ, ATP-asọmpi, yana ndị na-egbochi ọnụ nke bioavailable nke Mammalian Target of Rapamycin (mTOR). XL388 gbochiri phosphorylation cellular nke mTOR complex 1 (p-p70S6K, pS6, na p-4E-BP1) na mTOR complex 2 (pAKT (S473)) substrates. XL388 gosipụtara ezigbo pharmacokinetics na mkpughe ọnụ n'ọtụtụ ụdị nwere bioavailability na-agafeghị oke. Nlekọta ọnụ nke XL388 nye ụmụ oke athymic gba ọtọ etinyere na xenografts tumor mmadụ nyere ọrụ mgbochi mgbochi na-adabere na dose. |
| CPD100639 | GDC-0349 | GDC-0349 bụ obere nwa akwụkwọ ọgwụ anticaner molecule, nke Genentech mepụtara. Dị ka nke July 2012, Genentech etinyela akwụkwọ ikpe nke mbụ nke GDC-0349 maka nyochaa Safety and Tolerability of GDC-0349 na Patients With Locally Advanced ma ọ bụ Metastatic Solid Tumors ma ọ bụ Non Hodgkin's Lymphoma. |
| CPD100638 | ETP-46464 | ETP46464 bụ onye na-egbochi mmeghachi omume DNA mebiri kinase Ataxia-telangiectasia mutated (ATM) na Rad3 metụtara (ATR). |
| CPD100637 | Ụzọ-600 | WAY-600 bụ onye nwere ike, ATP-asọmpi na onye na-egbochi mTOR nwere IC50 nke 9 nM. |
| CPD100636 | WYE-687 | WYE-687 bụ onye nwere ike na ATP-asọmpi na onye na-egbochi mTOR nwere IC50 nke 7 nM. |
| CPD100635 | Palomid-529 | Palomid 529, makwaara dị ka P529, bụ ihe mgbochi PI3K/Akt/mTOR akwụkwọ akụkọ. Palomid 529 (P529) na-egbochi ogige TORC1 na TORC2 ma gosipụta ma mgbochi nke akara Akt na mTOR n'otu aka ahụ na tumor na vasculature. E gosipụtara na P529 gbochiri uto tumor, angiogenesis, na permeability vaskụla. Ọ na-ejigide akụkụ bara uru nke tumor vaskụla normalization nke rapamycin na-anya isi. Otú ọ dị, P529 gosipụtara uru ọzọ nke igbochi pAktS473 akara na-adabere na igbochi TORC2 na sel niile ma si otú a na-agafe loops nzaghachi na-eduga n'ịba ụba Akt na ụfọdụ mkpụrụ ndụ tumo. (Isi mmalite: Ọrịa Cancer Res 008;68(22):9551?–7). |
| CPD100634 | BGT226-nwoke | BGT226 bụ ihe mgbochi phosphatidylinositol 3-kinase (PI3K) nwere ọrụ antineoplastic nwere ike. PI3K inhibitor BGT226 na-egbochi kpọmkwem PIK3 na PI3K/AKT kinase (ma ọ bụ protein kinase B) ụzọ akara, nke nwere ike ịkpalite ntụgharị nke cytosolic Bax gaa na akpụkpọ anụ mpụta nke mitochondrial, na-abawanye permeability nke mitochondrial; Ọnwụ cell apoptotic nwere ike ịmalite. Bax bụ onye otu ezinụlọ proapoptotic Bcl2 nke protein. |
| CPD100633 | WYE-125132 | WYE-125132, nke a makwaara dị ka WYE-132, bụ nnukwu ike, ATP-asọmpi, na kpọmkwem mTOR kinase inhibitor (IC(50): 0.19 +/- 0.07 nmol/L;> 5,000-fold selective vesos PI3Ks). WYE-132 gbochiri mTORC1 na mTORC2 n'ụdị ọrịa kansa dị iche iche na vitro na vivo. N'ụzọ dị mkpa, na-agbanwe agbanwe na mkpụrụ ndụ ihe nketa nke mTORC2, WYE-132 ezubere iche P-AKT (S473) na ọrụ AKT na-enweghị ibelata ọkwa kwụ ọtọ nke PI3K/PDK1 ọrụ biomarker P-AKT (T308), na-egosipụta ụkpụrụ a ma ama na kpọmkwem. nke AKT site na mTORC2 na mkpụrụ ndụ kansa. |
| CPD100632 | Vistusertib | Vistusertib, nke a makwaara dị ka AZD2014, bụ onye na-egbochi anụ ahụ nke rapamycin (mTOR) nke nwere ike ịrụ ọrụ antineoplastic. mTOR kinase inhibitor AZD2014 na-egbochi ọrụ nke mTOR, nke nwere ike ime ka ntinye nke apoptosis tumor cell na mbelata mmụba nke cell tumor. mTOR, serine/threonine kinase nke a na-edozi n'ụdị etuto dị iche iche, na-arụ ọrụ dị mkpa na ala na ụzọ akara PI3K/Akt/mTOR. |
| CPD100631 | WYE-354 | WYE-354 bụ onye na-egbochi mTOR (IC50 = 4.3 nM) nke na-egbochi mgbaàmà site na mTOR complex 1 (mTORC1) na mTORC2. |
| CPD100630 | Gedatolisib | Gedatolisib, nke a makwaara dị ka PKI-587 na PF-05212384, bụ onye nnọchi anya na-ezubere phosphatidylinositol 3 kinase (PI3K) na mammalian target nke rapamycin (mTOR) n'ụzọ akara PI3K/mTOR, yana ọrụ antineoplastic nwere ike. Mgbe nchịkwa intravenous, PI3K/mTOR kinase inhibitor PKI-587 na-egbochi ma PI3K na mTOR kinases, nke nwere ike ịkpata apoptosis na mmụba nke mkpụrụ ndụ cancer na-egosipụta PI3K/mTOR. Ịkwalite ụzọ PI3K/mTOR na-akwalite uto cell, nlanarị, na iguzogide chemotherapy na redio; mTOR, serine/threonine kinase mgbada PI3K, nwekwara ike rụọ ọrụ na-adabereghị na PI3K. |
