| CAT # | Sunan samfur | Bayani |
| Saukewa: CPD100501 | Saukewa: UNC2541 | UNC2541 mai ƙarfi ne kuma takamaiman mai hanawa MerTK wanda ke nuna ayyukan hanawa na ƙananan ƙwayoyin cuta a cikin tushen ELISA. Bugu da kari, an warware tsarin X-ray na furotin MerTK a hadaddun tare da 11 don nuna cewa waɗannan macrocycles suna ɗaure a cikin aljihun MerTK ATP. UNC2541 ya nuna IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| Saukewa: CPD100745 | Farashin RU-302 | RU-302 sabon inhibitor pan-tam ne, yana toshe mu'amala tsakanin tam ig1 ectodomain da gas6 lg yankin, da ƙarfi yana hana layin salula na axl da masu karɓar tam na asali. |
| Saukewa: CPD100744 | R916562 | |
| Saukewa: CPD100743 | Ningetinib-Tosylate | CT-053, wanda kuma aka sani da DE-120, VEGF ne da mai hana PDGF mai yuwuwa don kula da jigon macular degeneration. |
| Saukewa: CPD100742 | SGI-7079 | SGI-7079 shine mai hanawa Axl mai ƙarfi kuma mai zaɓi tare da yuwuwar aikin rigakafin ciwon daji. SGI-7079 yadda ya kamata ya hana Axl kunnawa a gaban exogenous Gas6 ligand. SGI-7079 ya hana haɓakar ƙwayar cuta ta hanyar dogaro da kashi. Axl shine yuwuwar manufa ta warkewa don shawo kan juriya mai hana EGFR. |
| Saukewa: CPD100741 | 2-D08 | 2-D08 flavone ne na roba wanda ke hana sumoylation. 2-D08 ya nuna anti-aggregatory da neuroprotective sakamako |
| Saukewa: CPD100740 | Dubermatinib | Dubermatinib, wanda kuma aka sani da TP-0903, shine mai hanawa AXL mai ƙarfi da zaɓi. TP-0903 yana haifar da babban apoptosis a cikin ƙwayoyin CLL B tare da ƙimar LD50 na jeri na nanomolar. Haɗin TP-0903 tare da masu hana BTK suna haɓaka CLL B-cell apoptosis AXL overexpression jigo ne mai sake faruwa a cikin nau'ikan ƙari da yawa waɗanda suka sami juriya ga wakilai daban-daban. Kula da sel na ciwon daji tare da tp-0903 ya juya da m phenchymal phenchympe a cikin samfura da yawa da sel sel sel mai magani tare da wasu wakilan da aka yi niyya. Gudanar da TP-0903 ko dai a matsayin wakili ɗaya ko a hade tare da masu hana BTK na iya zama tasiri a cikin kula da marasa lafiya tare da CLL. |
| Saukewa: CPD100739 | Saukewa: NPS-1034 | NPS-1034 sabon labari ne mai hanawa MET, wanda ke hana mai karɓar MET da aka kunna da mutants ɗin sa. NPS-1034. NPS-1034 ya hana yaduwar kwayoyin halitta da ke bayyana MET da aka kunna kuma ya inganta farfadowa na ciwace-ciwacen da aka samo daga irin waɗannan kwayoyin halitta a cikin samfurin xenograft na linzamin kwamfuta ta hanyar anti-angiogenic da pro-apoptotic ayyuka. NPS-1034 kuma ya hana HGF-ƙarfafa kunna siginar MET a gaban ko babu ruwan magani. Musamman, NPS-1034 ya hana bambance-bambancen MET guda uku waɗanda ke da juriya ga masu hana MET SU11274, NVP-BVU972, da PHA665752. |
| Saukewa: CPD100738 | Glesatinib | Glesatinib, wanda kuma aka sani da MGCD-265, abu ne da ake iya samu ta baki, ƙananan ƙwayoyin cuta, mai hana tyrosine kinase mai yawan niyya tare da yuwuwar aikin antineoplastic. MGCD265 yana ɗaure da kuma hana phosphorylation na tyrosine kinases masu karɓa da yawa (RTKs), ciki har da mai karɓa na c-Met (mai karɓar haɓakar haɓakar hepatocyte); mai karɓar Tek / Tie-2; Nau'in nau'in 1, 2, da 3 masu karɓa (VEGFR) na jijiyoyi na endothelial; da macrophage-stimulating 1 mai karɓa (MST1R ko RON). |
| Saukewa: CPD100737 | Saukewa: CEP-40783 | CEP-40783, wanda kuma aka sani da RXDX-106, mai ƙarfi ne, mai zaɓaɓɓe da mai hanawa na baka na AXL da c-Met tare da ƙimar IC50 na 7 nM da 12 nM, bi da bi don amfani a cikin nono, huhu mara ƙaranci (NSCLC) , da ciwon daji na pancreatic. |
| Saukewa: CPD1725 | Bemcentinib | BGB-324, wanda kuma aka sani da R428 ko Bemcentinib, wani zaɓin ƙananan ƙwayoyin ƙwayoyin cuta ne na Axl kinase, wanda ya nuna aiki don toshe yaduwar ƙwayar cuta kuma yana tsawaita rayuwa a cikin samfuran ciwon daji na nono. Mai karɓar tyrosine kinase Axl na iya taka muhimmiyar rawa a ci gaban ciwon daji, mamayewa, metastasis, juriya na miyagun ƙwayoyi, da mutuwar haƙuri. R428 yana hana Axl tare da ƙananan aikin nanomolar kuma ya toshe abubuwan da suka dogara da Axl, ciki har da Akt phosphorylation, mamayewar ƙwayar nono, da samar da cytokine na proinflammatory. |
| Saukewa: CPD3545 | Gilteritinib | Gilteritinib, wanda kuma aka sani da ASP2215, shine mai hana FLT3 / AXL mai ƙarfi, wanda ya nuna aikin antileukemic mai ƙarfi akan AML tare da ko dai ko duka FLT3-ITD da FLT3-D835 maye gurbi. A cikin invitro, daga cikin 78 tyrosine kinases da aka gwada, ASP2215 ya hana FLT3, LTK, ALK, da AXL kinases sama da 50% a 1 nM tare da ƙimar IC50 na 0.29 nM don FLT3, kusan 800-ninka mafi ƙarfi fiye da c-KIT, hanawa wanda ke da alaƙa da haɗarin haɗari na myelosuppression. ASP2215 ya hana haɓakar ƙwayoyin MV4-11, waɗanda ke ɗaukar FLT3-ITD, tare da ƙimar IC50 na 0.92 nM, tare da hana pFLT3, pAKT, pSTAT5, PERK, da pS6. ASP2215 ya rage nauyin ƙari a cikin kasusuwa kuma ya tsawaita rayuwar berayen da aka dasa ta cikin jini tare da ƙwayoyin MV4-11. ASP2215 na iya samun yuwuwar amfani wajen magance AML. |
| Saukewa: CPD100734 | Saukewa: UNC2881 | UNC2881 shine mai hanawa Mer kinase mai ƙarfi. UNC2281 yana hana tsayayyen yanayi Mer kinase phosphorylation tare da ƙimar IC50 na 22 nM. Jiyya tare da UNC2281 kuma ya wadatar don toshe EGF-matsakaici na motsa jiki na mai karɓa na chimeric mai ɗauke da yankin intracellular na Mer gauraye zuwa yankin extracellular na EGFR. Bugu da ƙari, UNC2881 da ƙarfi yana hana haɗin haɗin platelet mai haifar da collagen, yana nuna cewa wannan rukunin masu hanawa na iya samun amfani don rigakafi da/ko maganin thrombosis na pathologic. |
| Saukewa: CPD100733 | Saukewa: UNC2250 | UNC2250 mai ƙarfi ne kuma mai hanawa Mer Kinase. Lokacin da aka yi amfani da sel masu rai, UNC2250 sun hana tsayayyen yanayin fosforilation na endogenous Mer tare da IC50 na 9.8 nM da katange ligand-ƙarfafa kunna furotin EGFR-Mer na chimeric. Jiyya tare da UNC2250 kuma ya haifar da raguwar yuwuwar samar da mulkin mallaka a cikin rhabdoid da ƙwayoyin tumor NSCLC, don haka yana nuna ayyukan antitumor na aiki. Sakamakon ya ba da dalili don ƙarin bincike na UNC2250 don aikace-aikacen warkewa a cikin marasa lafiya da ciwon daji. |
| Saukewa: CPD100732 | Saukewa: LDC1267 | LDC1267 mai ƙarfi ne kuma mai hanawa TAM kinase. LDC1267 yana nuna ƙananan ayyuka akan Met, Aurora B, Lck, Src, da CDK8. LDC1267 ya rage yawan ciwon daji na mammary na murine da melanoma metastases masu dogaro da ƙwayoyin NK. Masu karɓa na TAM tyrosine kinase Tyro3, Axl da Mer (wanda aka fi sani da Mertk) an gano su azaman abubuwan haɓakawa na Cbl-b. Jiyya na nau'in sel NK na daji tare da sabon haɓakar ƙaramin ƙwayar ƙwayar ƙwayar ƙwayar ƙwayar cuta ta TAM kinase inhibitor ya ba da damar warkewa, ingantaccen haɓaka aikin ƙwayoyin ƙwayoyin ƙwayoyin cuta na NK a cikin vivo. |
| Saukewa: CPD100731 | Saukewa: BMS-777607 | BMS-777607, kuma aka sani da BMS-817378 da ASLAN-002, Met tyrosine kinase inhibitor, mai hana MET tyrosine kinase tare da yuwuwar aikin antineoplastic. MET tyrosine kinase inhibitor BMS-777607 yana ɗaure zuwa furotin na c-Met, ko mai karɓar haɓakar haɓakar hepatocyte (HGFR), yana hana haɓaka haɓakar haɓakar hepatocyte (HGF) da rushe hanyar siginar MET; wannan wakili na iya haifar da mutuwar tantanin halitta a cikin ƙwayoyin tumor da ke bayyana c-Met. c-Met, mai karɓa na tyrosine kinase wanda aka yi amfani da shi ko kuma ya canza a yawancin nau'in ƙwayar ƙwayar cuta, yana taka muhimmiyar rawa a cikin ƙwayar ƙwayar ƙwayar cuta, tsira, mamayewa, da metastasis, kuma a cikin angiogenesis na tumor. |
| Saukewa: CPD100730 | Cabozantinib | Cabozantinib, wanda kuma aka sani da XL-184 ko BMS-907351, wani abu ne na baka, mai hana tyrosine kinase (RTK) mai hanawa tare da yuwuwar aikin antineoplastic. Cabozantinib yana da ƙarfi sosai kuma yana hana kinases masu karɓar tyrosine da yawa. Musamman, cabozantinib ya bayyana yana da alaƙa mai ƙarfi ga mai karɓar haɓakar haɓakar haɓakar hepatocyte (Met) da mai karɓar haɓakar haɓakar haɓakar ƙwayar cuta ta 2 (VEGFR2), wanda zai iya haifar da hana haɓakar ƙwayar cuta da angiogenesis, da haɓakar ƙwayar cuta. Cabozantinib ya amince da FDA a watan Nuwamba 2012 don maganin ciwon daji na thyroid. |
