| CAT # | Izina ryibicuruzwa | Ibisobanuro |
| CPD100501 | UNC2541 | UNC2541 nigikoresho gikomeye kandi cyihariye cya MerTK cyerekana ibikorwa byo guhagarika sub-micromolar muri ELISA. Byongeye kandi, imiterere ya X-ray ya poroteyine ya MerTK muri complexe hamwe na 11 yiyemeje kwerekana ko izo macrocycle zihuza mu mufuka wa MerTK ATP. UNC2541 yerekanye IC50 MerTH = 4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| CPD100745 | RU-302 | RU-30. |
| CPD100744 | R916562 | |
| CPD100743 | Ningetinib-Tosylate | CT-053, izwi kandi nka DE-120, ni inhibitor ya VEGF na PDGF ishobora kuvura imiti iterwa n'imyaka. |
| CPD100742 | SGI-7079 | SGI-7079 ninzitizi ikomeye kandi ihitamo Axl inhibitor hamwe nibikorwa bishobora kurwanya antikanseri. SGI-7079 yabujije neza gukora Axl imbere ya ligand exogenous Gas6. SGI-7079 yabujije imikurire yikibyimba muburyo butandukanye. Axl ni intego yo kuvura yo gutsinda EGFR inhibitor. |
| CPD100741 | 2-D08 | 2-D08 ni flavone ya syntetique ibuza sumoylation. 2-D08 yerekanye ingaruka zo kurwanya igiteranyo na neuroprotective |
| CPD100740 | Dubermatinib | Dubermatinib, izwi kandi nka TP-0903, ni inhibitor ya AXL ikomeye kandi ihitamo. TP-0903 itera apoptose nini muri selile CLL B ifite LD50 indangagaciro za nanomolar. Guhuza TP-0903 hamwe na BTK inhibitor yongerera CLL B-selile apoptose AXL gukabya gukabije ni insanganyamatsiko yongeye kugaruka igaragara mubwoko butandukanye bwibibyimba byabonye kurwanya imiti itandukanye. Kuvura ingirangingo za kanseri hamwe na TP-0903 bihindura fenotype ya mesenchymal muburyo bwinshi kandi ikangurira kanseri kanseri kwivuza hamwe nibindi bikoresho bigamije. Ubuyobozi bwa TP-0903 haba nkumukozi umwe cyangwa bufatanije na BTK inhibitor irashobora kuba ingirakamaro mukuvura abarwayi bafite CLL. |
| CPD100739 | NPS-1034 | NPS-1034 nigitabo gishya cya MET inhibitor, kibuza MET reseptor ikora hamwe na mutant ikora. NPS-1034, irabuza uburyo butandukanye bwimikorere ya mutant ya MET kimwe na HGF ikora-ubwoko bwa MET. NPS-1034 yabujije ikwirakwizwa ry'utugingo ngengabuzima tugaragaza MET ikora kandi iteza imbere gusubira inyuma kw'ibibyimba biva muri selile nk'icyitegererezo cy'imbeba xenograft binyuze mu bikorwa byo kurwanya angiogenic na pro-apoptotic. NPS-1034 kandi yabujije HGF-iterwa no gukora MET yerekana ibimenyetso bya serumu ihari cyangwa idahari. Ikigaragara ni uko NPS-1034 yabujije ibintu bitatu MET irwanya MET inhibitor SU11274, NVP-BVU972, na PHA665752. |
| CPD100738 | Glesatinib | Glesatinib, izwi kandi ku izina rya MGCD-265, ni bioavailable yo mu kanwa, molekile nto, intego ya tyrosine kinase inhibitor hamwe nibikorwa bya antineoplastique. MGCD265 ihuza kandi ikabuza fosifora ya reseptor tyrosine kinase nyinshi (RTKs), harimo na c-Met reseptor (reseptor yo gukura kwa hepatocyte); reseptor ya Tek / Ikariso-2; imiyoboro y'amaraso ikura (VEGFR) ubwoko bwa 1, 2, na 3; na macrophage-itera 1 reseptor (MST1R cyangwa RON). |
| CPD100737 | CEP-40783 | CEP-40. , na kanseri yandura. |
| CPD1725 | Bemcentinib | BGB-324, izwi kandi ku izina rya R428 cyangwa Bemcentinib, ni molekile ntoya yatoranijwe ya Axl kinase, yerekanaga ibikorwa byo guhagarika ikibyimba ikwirakwira kandi ikomeza kubaho mu buryo bwa kanseri y'ibere. Reseptor tyrosine kinase Axl irashobora kugira uruhare runini mugutera kanseri, gutera, metastasis, kurwanya ibiyobyabwenge, no gupfa kwabarwayi. R428 ibuza Axl ibikorwa bya nanomolar nkeya kandi ikabuza ibintu biterwa na Axl, harimo nka fosifora ya Akt, gutera kanseri y'ibere, hamwe na sitokine ya protinflammatory. |
| CPD3545 | Gilteritinib | Gilteritinib, izwi kandi nka ASP2215, ni inhibitor ikomeye ya FLT3 / AXL, yerekanaga ibikorwa bikomeye bya antileukemic kurwanya AML hamwe na FLT3-ITD na FLT3-D835 ihinduka. Muri invitro, muri kinase 78 za tirozine zapimwe, ASP2215 yabujije FLT3, LTK, ALK, na AXL kinase hejuru ya 50% kuri 1 nM hamwe na IC50 ifite agaciro ka 0.29 nM kuri FLT3, hafi inshuro 800 zikomeye kuruta c-KIT, kubuzwa bifitanye isano ningaruka zishobora guterwa na myelosuppression. ASP2215 yabujije imikurire ya selile MV4-11, ibika FLT3-ITD, ifite IC50 ifite agaciro ka 0,92 nM, iherekejwe no kubuza pFLT3, pAKT, pSTAT5, pERK, na pS6. ASP2215 yagabanije umutwaro wibibyimba mumagufwa kandi bimara igihe kinini cyo kubaho kwimbeba zatewe mumitsi hamwe na selile MV4-11. ASP2215 irashobora kuba ifite ubushobozi bwo kuvura AML. |
| CPD100734 | UNC2881 | UNC2881 ninzitizi ikomeye ya Mer kinase. UNC2281 irabuza leta ya Mer kinase fosifora ihagaze hamwe na IC50 ifite agaciro ka 22 nM. Umuti hamwe na UNC2281 urahagije kandi kugirango uhagarike imbaraga za EGF ziterwa no gukurura chimeric reseptor irimo indangagitsina ya Mer yahujwe na domaine idasanzwe ya EGFR. Byongeye kandi, UNC2881 ibuza cyane gukusanya platine iterwa na kolagen, byerekana ko iki cyiciro cya inhibitor gishobora kugira akamaro mu gukumira no / cyangwa kuvura indwara ya trombose. |
| CPD100733 | UNC2250 | UNC2250 ninzitizi ikomeye ya Mer Kinase. Iyo ikoreshwa kuri selile nzima, UNC2250 yabujije fosifora ihamye ya endogenous Mer hamwe na IC50 ya 9.8 nM kandi ikabuza gukora ligand-iterwa na poroteyine ya chimeric EGFR-Mer. Kuvura hamwe na UNC2250 byanatumye ubushobozi bwo gukora ubukoroni bugabanuka muri selile ya rhabdoid na NSCLC, bityo bikerekana ibikorwa bya antitumor ikora. Ibisubizo biratanga impamvu zifatika zo gukora iperereza kuri UNC2250 mugukoresha imiti ivura abarwayi ba kanseri. |
| CPD100732 | LDC1267 | LDC1267 nimbaraga zikomeye kandi zitoranya TAM kinase inhibitor. LDC1267 yerekana ibikorwa byo hasi kurwanya Met, Aurora B, Lck, Src, na CDK8. LDC1267 yagabanije cyane kanseri y’inyamabere ya murine na metanase ya melanoma biterwa na selile NK. TAM tyrosine kinase yakira Tyro3, Axl na Mer (izwi kandi nka Mertk) byagaragaye ko ari insimburangingo ya Cbl-b. Kuvura ingirabuzimafatizo zo mu bwoko bwa NK hamwe na molekile ntoya ya TAM kinase inhibitor yatanze ubushobozi bwo kuvura, byongera imikorere yibikorwa bya selile NK muri vivo. |
| CPD100731 | BMS-777607 | BMS-777607, izwi kandi nka BMS-817378 na ASLAN-002, Met tyrosine kinase inhibitor, ni inzitizi ya MET tyrosine kinase ifite ibikorwa bya antineoplastique. MET tyrosine kinase inhibitor BMS-777607 ihuza na c-Met proteine, cyangwa reseptor yo gukura kwa hepatocyte (HGFR), ikumira guhuza ibintu bikura hepatocyte (HGF) no guhagarika inzira ya MET yerekana inzira; iyi agent irashobora gutera urupfu mungirangingo yibibyimba byerekana c-Met. C. |
| CPD100730 | Cabozantinib | Cabozantinib, izwi kandi ku izina rya XL-184 cyangwa BMS-907351, ni bioavailable yo mu kanwa, ntoya ya molekile reseptor tyrosine kinase (RTK) inhibitor ifite ibikorwa bya antineoplastique. Cabozantinib irahuza cyane kandi ikabuza tinosine reseptor kinase nyinshi. By'umwihariko, cabozantinib isa nkaho ifitanye isano ikomeye na reseptor yo gukura kwa hepatocyte (Met) hamwe na endoteliyale ikura yibintu byakira 2 (VEGFR2), bishobora kuviramo kubuza gukura kwikibyimba na angiogenezi, no gusubira inyuma kubyimba. Cabozantinib yemejwe na FDA yo muri Amerika mu Gushyingo 2012 kugira ngo ivure kanseri ya tiroyide ya medullary. |
