| CAT # | Product Name | Tsanangudzo |
| CPD100654 | PD-169316 | PD-169316 is selective inhibitor ye p38 MAPK. Iyo inhibisa p38 MAPK ine IC50 ye89 nM. PD169316, inhibits kushandura kukura chinhu beta-induced Smad siginecha mumasero egomarara remunhu. |
| CPD100653 | LDN-193189 | LDN193189 imorekuru diki rine simba zvakanyanya BMP inhibitor ine IC50 ye5 uye 30 nM yeALK2 neALK3, zvichiteerana. LDN193189 inodzivisawo BMP mhando I receptors ALK6 (TGFβ1 / BMP chiratidzo) uye inotevera SMAD phosphorylation. |
| CPD100652 | K02288 | K02288 inhibitor ine simba yeBMP kusaina. K02288 ine in vitro chiitiko inopesana neALK2 pane yakaderera nanomolar concentrations yakafanana neyazvino inotungamira kombi LDN-193189. K02288 yakanyatso kuvharira BMP-induced Smad nzira isina kukanganisa TGF-β kusaina uye kukonzeresa dorsalization ye zebrafish embryos. |
| CPD100650 | SB-431542 | SB-431542 inhibitor diki molecule inhibitor yemhando I TGF-beta receptor, pane panhizha yeakaipa glioma cell mitsara. SB-431542 yakavharira phosphorylation uye nyukireya translocation yeSMADs, intracellular mediators yeTGF-beta siginecha, nekuderera kweTGF-beta-mediated transcription. Uyezve, SB-431542 yakadzivisa kutaura kwezvinhu zviviri zvakakosha zvinokonzerwa neTGF-beta-vascular endothelial growth factor uye plasminogen activator inhibitor-1. |
| CPD100649 | GW788388 | GW788388 itsva TGF-beta yerudzi rweI receptor inhibitor ine yakavandudzwa pharmacokinetic profile kana ichienzaniswa neSB431542. Takadzidza kushanda kwayo mu vitro uye takaona kuti yakadzivisa zvose TGF-beta mhando I uye mhando II receptor kinase zviitiko, asi kwete iyo yakabatana bone morphogenic protein type II receptor. Kupfuurirazve, yakavharira TGF-beta-induced Smad activation uye chinangwa chejini kutaura, ichideredza epithelial-mesenchymal shanduko uye fibrogenesis. |
| CPD100648 | SB-525334 | SB525334 inhibitor ine simba uye inosarudza yekushandura kukura factor-beta1 (TGF-beta1) receptor, activin receptor-like kinase (ALK5). SB525334 yakavharira ALK5 kinase chiitiko neIC(50) ye14.3 nM uye yaive ingangoita 4-yakapetwa isina simba seinhibitor yeALK4 (IC(50) = 58.5 nM). SB-525334 yakanga isingashande se inhibitor yeALK2, ALK3, uye ALK6 (IC(50)> 10,000 nM). Mune cell-based assays, SB-525334 (1 microM) yakavharira TGF-beta1-induced phosphorylation uye nyukireya translocation yeSmad2/3 mu renal proximal tubule masero uye inhibited TGF-beta1-induced kuwedzera mu plasminogen activator inhibitor-1 (PAI-1). ) uye procollagen alpha1 (I) mRNA kutaura muA498 renal epithelial carcinoma masero. |
| CPD100647 | BIBF0775 | BIBF0775 inhibitor yekushandura kukura factor β receptor I (TGFβRI). X-ray chimiro chekuongorora chakaratidza kuti BIBF0775 yakanyura mune kinase domain yeTGFβRI. |
| CPD100646 | LY3023414 | LY3023414 iduku duku rakaratidzwa mu vitro kuva sarudzo yeATP-competitive inhibitor yePI3Kα uye mTOR, DNA-PK, uye imwe kirasi I PI3K nhengo dzemhuri. In vitro, LY3023414 yakaratidza inhibitory chiitiko ichipokana nePI3K uye mTOR mumamota maseru, pamwe neantiproliferative chiitiko uye sero cycle mhedzisiro. Mukuwedzera, in vitro, LY3023414 inodzivisa kukwanisa kwePI3K uye mTOR kune phosphorylate substrates muPI3K / mTOR nzira. LY3023414 iri kuongororwa muchikamu chekutanga chekiriniki yekuedza. |
| CPD100645 | Onatasertib | CC-223 inhibitor inowanikwa nemuromo ye mammalian target ye rapamycin (mTOR) ine inogona kuita antineoplastic chiitiko. mTOR kinase inhibitor CC-223 inhibits basa reMTOR, izvo zvinogona kuguma nekuiswa kwebundu cell apoptosis uye kuderera kwebundu cell proliferation. mTOR, serine/threonine kinase iyo inokwidziridzwa mumhando dzakasiyana-siyana dzemamota, inoita basa rakakosha kudzika pasi munzira yePI3K/AKT/mTOR yechiratidzo, iyo inowanzo gadziriswa mumakenza evanhu. |
| CPD100644 | Bimiralisib | Bimiralisib, inozivikanwawo sePQR309, inonzi orally bioavailable pan inhibitor ye phosphoinositide-3-kinases (PI3K) uye inhibitor yemammalian target yerapamycin (mTOR), ine inogona kuita antineoplastic chiitiko. PI3K/mTOR kinase inhibitor PQR309 inhibits PI3K kinase isoforms alpha, beta, gamma uye delta uye, zvishoma, mTOR kinase, izvo zvinogona kukonzera bundu cell apoptosis uye kukura inhibition mumasero overexpressing PI3K/mTOR. Kuita kwePI3K/mTOR nzira inosimudzira kukura kwesero, kurarama, uye kuramba kune zvese chemotherapy uye radiotherapy. |
| CPD100643 | CZ415 | CZ415 ine simba ATP-yemakwikwi mTOR inhibitor ine kusarudzwa kusati kwamboitika pane chero imwe kinase (IC50 = 14.5 nM IC50 ye pS6RP uye 14.8 nM ye pAKT) ine yakanaka kwazvo sero permeability (Kd app = 6.9 nM). Pharmacokinetic zvimiro zvepakati pemvumo uye yakanaka yemuromo bioavailability yakaratidza kukodzera kweCZ415 yekufambira mberi kune mu vivo zvidzidzo. CZ415 inomiririra molekuru yakanakira yekuferefeta kwemishonga yemTOR pathophysiological basa mu vivo. |
| CPD100642 | GDC-0084 | GDC-0084, inozivikanwawo seRG7666 uye Paxalisib, inonzi phosphatidylinositol 3-kinase (PI3K) inhibitor ine inogona kuita antineoplastic. PI3K inhibitor GDC-0084 inonyanya kuvharidzira PI3K muPI3K/AKT kinase (kana protein kinase B) nzira yechiratidzo, nokudaro ichidzivisa kushandiswa kwePI3K nzira yechiratidzo. Izvi zvinogona kuguma nekudzivirirwa kweese kukura kwesero uye kurarama mune anotarisika bundu cell populations. Kuita kwePI3K nzira yekusaina kunowanzo kubatanidzwa ne tumorigenesis. |
| CPD100641 | CC-115 | CC-115 inonzi dual inhibitor yeDNA-inotsamira protein kinase (DNA-PK) uye mammalian chinangwa cherapamycin (mTOR), ine inogona kuita antineoplastic. CC-115 inosunga uye inhibits kuita kweDNA-PK uye zvese zviri zviviri raptor-mTOR (TOR complex 1 kana TORC1) uye rictor-mTOR (TOR complex 2 kana TORC2), izvo zvinogona kutungamirira mukuderedza kupararira kwemasero ekenza masero anoratidza. DNA-PK uye TOR. DNA-PK, serine / threonine kinase uye nhengo yePI3K-inoenderana kinase subfamily yeprotein kinases, inoshandiswa pane DNA kukuvara uye inoita basa rakakosha mukugadzirisa kuputika kweDNA kwakapetwa kaviri kuburikidza neDNA nonhomologous end joining (NHEJ) nzira. . |
| CPD100640 | XL388 | XL388 iNovel Kirasi yeYakanyanya Kusimba, Inosarudza, ATP-Kukwikwidza, uye Nemuromo Bioavailable Inhibitors yeMammalian Target yeRapamycin (mTOR). XL388 inhibited cellular phosphorylation ye mTOR complex 1 (p-p70S6K, pS6, uye p-4E-BP1) uye mTOR yakaoma 2 (pAKT (S473)) substrates. XL388 yakaratidza yakanaka pharmacokinetics uye kuratidzwa kwemuromo mumarudzi akawanda ane pakati nepakati bioavailability. Oral management yeXL388 kune athymic nude mbeva dzakasimwa nebundu remunhu xenografts yakapa yakakosha uye inotsamira-dosi-inotsamira antitumor chiitiko. |
| CPD100639 | GDC-0349 | GDC-0349 idiki molecule anticaner drug candidate, iri kugadzirwa neGenentech. Kubva muna Chikunguru 2012, Genentech yakaisa chirongwa chechikamu chekutanga cheGDC-0349 chekuongorora Kuchengetedzeka uye Kushivirira kweGDC-0349 muVarwere Vane Nzvimbo Yakakura Kana Metastatic Solid Tumors kana Non Hodgkin's Lymphoma. |
| CPD100638 | ETP-46464 | ETP46464 inhibitor yeDNA damage response kinase Ataxia-telangiectasia mutated (ATM)- uye Rad3-inoenderana (ATR). |
| CPD100637 | NZIRA-600 | NZIRA-600 ine simba, ATP-inokwikwidza uye inosarudza inhibitor ye mTOR ine IC50 ye9 nM. |
| CPD100636 | WYE-687 | WYE-687 ine simba uye ATP-inokwikwidza uye inosarudza inhibitor ye mTOR ine IC50 ye7 nM. |
| CPD100635 | Palomid-529 | Palomid 529, inozivikanwawo seP529, ibhuku PI3K/Akt/mTOR inhibitor. Palomid 529 (P529) inhibits iyo TORC1 uye TORC2 complexes uye inoratidza zvose inhibition yeAkt kusaina uye mTOR kusaina zvakafanana mubundu uye vasculature. Zvakaratidzwa kuti P529 inhibited bundu kukura, angiogenesis, uye vascular permeability. Yakachengeta izvo zvinobatsira zve tumor vascular normalization iyo rapamycin inodada. Nekudaro, P529 yakaratidza imwe bhenefiti yekuvharisa pAktS473 siginecha inoenderana nekuvharira TORC2 mumaseru ese uye nekudaro ichipfuura mhinduro zvishwe zvinotungamira kuwedzera kweAkt kusaina mune mamwe masero bundu. (Kwakabva: Cancer Res 008;68(22):9551?–7). |
| CPD100634 | BGT226-murume | BGT226 ndeye phosphatidylinositol 3-kinase (PI3K) inhibitor ine inogona kuita antineoplastic chiitiko. PI3K inhibitor BGT226 inonyanya kuvharidzira PIK3 muPI3K / AKT kinase (kana protein kinase B) nzira yechiratidzo, iyo inogona kukonzera kuendeswa kwe cytosolic Bax kune mitochondrial kunze membrane, kuwedzera mitochondrial membrane permeability; Kufa kweapoptotic cell kunogona kuitika. Bax inhengo yeproapoptotic Bcl2 mhuri yemapuroteni. |
| CPD100633 | WYE-125132 | WYE-125132, inozivikanwawo seWYE-132, ine simba zvakanyanya, ATP-inokwikwidza, uye yakananga mTOR kinase inhibitor (IC(50): 0.19 +/- 0.07 nmol/L; > 5,000-yakapetwa inosarudza maringe nePI3Ks). WYE-132 inhibited mTORC1 uye mTORC2 mumhando dzakasiyana dzekenza mu vitro uye mu vivo. Zvinonyanya kukosha, zvinoenderana neiyo genetic ablation ye mTORC2, WYE-132 yakanangwa P-AKT (S473) uye AKT basa pasina zvakanyanya kudzikisa yakadzikama-yero nhanho yePI3K/PDK1 chiitiko biomarker P-AKT (T308), ichiratidzira yakakurumbira uye yakananga mutemo. yeAKT nemTORC2 mumasero ekenza. |
| CPD100632 | Vistusertib | Vistusertib, inozivikanwawo se AZD2014, inhibitor yemuromo yemhuka yerapamycin (mTOR) inogona kuita antiineoplastic. mTOR kinase inhibitor AZD2014 inhibits basa reMTOR, izvo zvinogona kuguma nekuiswa kwebundu cell apoptosis uye kuderera kwebundu cell proliferation. mTOR, serine/threonine kinase iyo inokwidziridzwa mumhando dzakasiyana-siyana dzemamota, inoita basa rakakosha kudzika pasi munzira yePI3K/Akt/mTOR yekusaina. |
| CPD100631 | WYE-354 | WYE-354 ine simba cell-permeable inhibitor ye mTOR (IC50 = 4.3 nM) inovharira kusaina kuburikidza nezvose zviri zviviri mTOR complex 1 (mTORC1) uye mTORC2. |
| CPD100630 | Gedatolisib | Gedatolisib, inozivikanwawo sePKI-587 uye PF-05212384, mumiririri akananga kune phosphatidylinositol 3 kinase (PI3K) uye mammalian chinangwa cherapamycin (mTOR) muPI3K/mTOR yekusaina nzira, ine inogona kuita antineoplastic chiitiko. Pamusoro pe intravenous administration, PI3K/mTOR kinase inhibitor PKI-587 inhibits zvose PI3K uye mTOR kinases, izvo zvinogona kukonzera apoptosis uye kukura kwekudzivirira kwemasero ekenza overexpressing PI3K/mTOR. Kuita kwePI3K/mTOR nzira inosimudzira kukura kwesero, kurarama, uye kuramba chemotherapy uye radiotherapy; mTOR, serine/threonine kinase kuzasi kwePI3K, inogona zvakare kuvhurwa yakazvimirira yePI3K. |
