| IKATI # | Igama Lomkhiqizo | Incazelo |
| I-CPD100501 | UNC2541 | I-UNC2541 iyisivimbeli esinamandla futhi esiqondene ne-MerTK esibonisa umsebenzi we-sub-micromolar inhibitory ku-ELISA esekelwe kuseli. Ukwengeza, isakhiwo se-X-ray seprotheni ye-MerTK eyinkimbinkimbi ene-11 yaxazululwa ukuze kuboniswe ukuthi lawa ma-macrocycle abophezela ephaketheni le-MerTK ATP. I-UNC2541 ibonise i-IC50 MerTH=4.4 nM; I-IC50 AXL = 120 nM; I-IC50 TYRO3 = 220 nM; I-IC50 FLT3 = 320 nM. |
| I-CPD100745 | I-RU-302 | I-RU-302 iyinoveli ye-pan-tam inhibitor, evimba ukuxhumana phakathi kwe-tam ig1 ectodomain kanye nesizinda se-gas6 lg, evimbela ngokunamandla imigqa yamaseli e-axl yezintatheli kanye nemigqa yamaseli omdlavuza wama-tam receptors. |
| I-CPD100744 | R916562 | |
| I-CPD100743 | I-Ningetinib-Tosylate | I-CT-053, eyaziwa nangokuthi i-DE-120, iyi-VEGF kanye ne-PDGF inhibitor engase ibe ukwelashwa kokuwohloka kwe-macular okuhlobene neminyaka emanzi. |
| I-CPD100742 | I-SGI-7079 | I-SGI-7079 iyi-Axl inhibitor enamandla futhi ekhethayo enomsebenzi ongase ube khona wokulwa nomdlavuza. I-SGI-7079 ivimbe ngempumelelo ukusebenzisa i-Axl phambi kwe-Gas6 ligand yangaphandle. I-SGI-7079 ivimbele ukukhula kwesimila ngendlela encike kumthamo. I-Axl iyithagethi yokwelapha enamandla yokunqoba ukumelana ne-EGFR inhibitor. |
| I-CPD100741 | 2-D08 | I-2-D08 iyi-flavone yokwenziwa evimbela i-sumoylation. I-2-D08 ibonise umphumela we-anti-aggregatory kanye neuroprotective |
| I-CPD100740 | I-Dubermatinib | I-Dubermatinib, eyaziwa nangokuthi i-TP-0903, iyi-AXL inhibitor enamandla futhi ekhethayo. I-TP-0903 idala i-apoptosis enkulu kumaseli e-CLL B ngamavelu e-LD50 obubanzi be-nanomolar. Inhlanganisela ye-TP-0903 ne-BTK inhibitors augments CLL B-cell apoptosis AXL overexpression itimu eyenzeka kabusha ebonwa ezinhlotsheni eziningi zesimila esithole ukumelana nama-ejenti ahlukahlukene. Ukwelashwa kwamaseli omdlavuza nge-TP-0903 kubuyisela emuva i-mesenchymal phenotype kumamodeli amaningi futhi kuqwashise amangqamuzana omdlavuza ekwelapheni namanye ama-ejenti ahlosiwe. Ukuphathwa kwe-TP-0903 njenge-ejenti eyodwa noma kuhlanganiswe ne-BTK inhibitors kungase kusebenze ekwelapheni iziguli nge-CLL. |
| I-CPD100739 | I-NPS-1034 | I-NPS-1034 iyinoveli ye-MET inhibitor, evimbela i-MET receptor ecushiwe kanye nezinguquko zayo ezisebenzayo. I-NPS-1034, ivimbela izinhlobo ezihlukahlukene eziguqukayo ezisebenzayo ze-MET kanye ne-HGF-activated wild-type MET. I-NPS-1034 ivimbele ukwanda kwamaseli aveza i-MET ecushiwe futhi yakhuthaza ukuhlehla kwezimila ezakhiwe kusukela kumaseli anjalo kumodeli ye-mouse xenograft ngokusebenzisa izenzo zokulwa ne-angiogenic kanye ne-pro-apoptotic. I-NPS-1034 iphinde yavimbela ukusebenza okuvuselelwe kwe-HGF kokusayina kwe-MET lapho kukhona noma kungekho serum. Ngokuphawulekayo, i-NPS-1034 ivimbele okuhlukile kwe-MET okuthathu okumelana nama-MET inhibitors SU11274, NVP-BVU972, kanye ne-PHA665752. |
| I-CPD100738 | I-Glesatinib | I-Glesatinib, eyaziwa nangokuthi i-MGCD-265, i-oral bioavailable, i-molecule encane, i-multitargeted tyrosine kinase inhibitor enomsebenzi ongase ube khona we-antineoplastic. I-MGCD265 ibophezela futhi ivimbele i-phosphorylation ye-receptor tyrosine kinases (RTKs) eminingana, kuhlanganise ne-c-Met receptor (i-hepatocyte growth factor receptor); i-Tek/Tie-2 receptor; i-vascular endothelial growth factor receptor (VEGFR) izinhlobo ze-1, i-2, ne-3; kanye ne-macrophage-stimulating 1 receptor (MST1R noma RON). |
| I-CPD100737 | I-CEP-40783 | I-CEP-40783, eyaziwa nangokuthi i-RXDX-106, iyi-inhibitor enamandla, ekhethayo futhi etholakala ngomlomo ye-AXL kanye ne-c-Met enamanani e-IC50 angu-7 nM no-12 nM, ngokulandelanayo ukuze isetshenziswe ebeleni, iseli yamaphaphu angewona amancane (NSCLC) , kanye nomdlavuza we-pancreatic. |
| I-CPD1725 | Bemcentinib | I-BGB-324, eyaziwa nangokuthi i-R428 noma i-Bemcentinib, iyisivimbeli se-molecule encane ekhethiwe ye-Axl kinase, ebonise umsebenzi wokuvimba ukusakazeka kwesimila futhi yandise ukusinda kumamodeli omdlavuza webele we-metastatic. I-receptor tyrosine kinase Axl ingase idlale indima ebalulekile ekuqhubekeleni phambili komdlavuza, ukuhlasela, i-metastasis, ukumelana nezidakamizwa, nokufa kwesiguli. I-R428 ivimbela i-Axl ngomsebenzi ophansi we-nanomolar kanye nemicimbi evinjiwe encike ku-Axl, okuhlanganisa i-Akt phosphorylation, ukuhlasela kweseli lomdlavuza webele, nokukhiqizwa kwe-cytokine ye-proinflammatory. |
| I-CPD3545 | I-Gilteritinib | I-Gilteritinib, eyaziwa nangokuthi i-ASP2215, iyisivimbeli esinamandla se-FLT3/AXL, esibonise umsebenzi onamandla we-antileukemic ngokumelene ne-AML ngokushintsha noma kokubili kwe-FLT3-ITD kanye ne-FLT3-D835. I-invitro, phakathi kwama-78 tyrosine kinases ahloliwe, i-ASP2215 ivimbe i-FLT3, LTK, ALK, ne-AXL kinases ngaphezu kuka-50% ku-1 nM enenani le-IC50 elingu-0.29 nM le-FLT3, cishe izikhathi ezingu-800 ezinamandla kune-c-KIT, ukuvimbela okuxhumene nobungozi obungaba khona be-myelosuppression. I-ASP2215 ivimbele ukukhula kwamaseli e-MV4-11, aphethe i-FLT3-ITD, enenani le-IC50 elingu-0.92 nM, ehambisana nokuvinjwa kwe-pFLT3, pAKT, pSTAT5, pERK, ne-pS6. I-ASP2215 yehlisa umthwalo wesimila emnkantsheni wethambo futhi yandisa ukuphila kwamagundane afakwe emithanjeni ngamaseli e-MV4-11. I-ASP2215 ingaba nokusetshenziswa okunamandla ekwelapheni i-AML. |
| I-CPD100734 | UNC2881 | I-UNC2881 iyi-Mer kinase inhibitor enamandla. I-UNC2281 ivimbela i-Mer kinase phosphorylation enenani le-IC50 elingu-22 nM. Ukwelashwa nge-UNC2281 nakho kwanele ukuvimba ukugqugquzelwa kwe-EGF-mediated kwe-chimeric receptor equkethe isizinda se-intracellular se-Mer esihlanganiswe kusizinda se-extracellular se-EGFR. Ngaphezu kwalokho, i-UNC2881 ivimbela ngokunamandla ukuhlangana kweplatelet eyenziwe nge-collagen, iphakamisa ukuthi leli klasi lama-inhibitors lingase libe nensizakalo yokuvimbela kanye/noma yokwelapha i-pathologic thrombosis. |
| I-CPD100733 | UNC2250 | I-UNC2250 iyisivimbi esinamandla futhi esikhethiwe se-Mer Kinase. Uma isetshenziswa kumaseli aphilayo, i-UNC2250 ivimbele i-phosphorylation yesimo esizinzile ye-Endogenous Mer nge-IC50 ye-9.8 nM futhi yavimba ukwenziwa kusebenze okuvuselelwe i-ligand kwephrotheni ye-chimeric EGFR-Mer. Ukwelashwa nge-UNC2250 kuphinde kwaholela ekwehleni kwamandla okwenza ikholoni kumaseli e-rhabdoid kanye ne-NSCLC yesimila, ngaleyo ndlela kubonise umsebenzi osebenzayo we-antitumor. Imiphumela ihlinzeka ngesizathu sokuqhubeka nophenyo lwe-UNC2250 yokusetshenziswa kokwelapha ezigulini ezinomdlavuza. |
| I-CPD100732 | I-LDC1267 | I-LDC1267 iyi-TAM kinase inhibitor enamandla futhi ekhethayo. I-LDC1267 ibonisa umsebenzi ophansi ngokumelene ne-Met, i-Aurora B, i-Lck, i-Src, ne-CDK8. I-LDC1267 inciphise ngokuphawulekayo umdlavuza webele we-murine kanye nama-metastase e-melanoma ancike kumaseli e-NK. Ama-TAM tyrosine kinase receptors i-Tyro3, i-Axl ne-Mer (eyaziwa nangokuthi i-Mertk) ikhonjwe njengama-substrates e-ubiquitylation ye-Cbl-b. Ukwelashwa kwamaseli e-NK ohlobo lwasendle nge-molecule encane esanda kwakhiwa ye-TAM kinase inhibitor kunikeza amandla okwelapha, okuthuthukisa ngempumelelo umsebenzi wamaseli e-NK e-anti-metastatic ku-vivo. |
| I-CPD100731 | I-BMS-777607 | I-BMS-777607, eyaziwa nangokuthi i-BMS-817378 ne-ASLAN-002, i-Met tyrosine kinase inhibitor, iyisivimbeli se-MET tyrosine kinase esinomsebenzi we-antineoplastic ongaba khona. I-MET tyrosine kinase inhibitor BMS-777607 ibophezela ku-c-Met protein, noma i-hepatocyte growth factor receptor (HGFR), ivimbela ukubopha kwe-hepatocyte growth factor (HGF) nokuphazamisa indlela yokubonisa i-MET; le ejenti ingase ibangele ukufa kweseli kumaseli wesimila aveza i-c-Met. I-c-Met, i-receptor tyrosine kinase evezwe ngokweqile noma eshintshiwe ezinhlotsheni eziningi zamangqamuzana e-tumor, idlala indima ebalulekile ekwandeni kweseli yesimila, ukusinda, ukuhlasela, kanye ne-metastasis, kanye naku-angiogenesis yesimila. |
| I-CPD100730 | I-Cabozantinib | I-Cabozantinib, eyaziwa nangokuthi i-XL-184 noma i-BMS-907351, iyi-inhibitor etholakala ngomlomo, i-molecule encane ye-receptor tyrosine kinase (RTK) enomsebenzi ongaba khona we-antineoplastic. I-Cabozantinib ibophezela ngokuqinile futhi ivimbele ama-tyrosine receptor kinases ambalwa. Ngokukhethekile, i-cabozantinib ibonakala inobudlelwane obuqinile be-hepatocyte growth factor receptor (Met) kanye ne-vascular endothelial growth factor receptor 2 (VEGFR2), okungase kubangele ukuvinjelwa kokukhula kwesimila kanye ne-angiogenesis, kanye nokuhlehla kwesimila. I-Cabozantinib yagunyazwa yi-FDA yase-US ngoNovemba 2012 yokwelapha umdlavuza we-medullary thyroid. |
