| KATSE # | Lebitso la Sehlahiswa | Tlhaloso |
| CPD100501 | UNC2541 | UNC2541 ke inhibitor e matla le e khethehileng ea MerTK e bonts'ang ts'ebetso ea sub-micromolar inhibitory ho ELISA e thehiloeng liseleng. Ho phaella moo, sebopeho sa X-ray sa protheine ea MerTK e rarahaneng le 11 e ile ea rarolloa ho bontša hore li-macrocycle tsena li tlama ka mokotleng oa MerTK ATP. UNC2541 e bontšitse IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| CPD100745 | RU-302 | RU-302 ke buka e ncha ea pan-tam inhibitor, e thibelang khokahano lipakeng tsa tam ig1 ectodomain le gas6 lg domain, e thibelang mela ea lisele tsa motlalehi oa axl le mela ea lisele tsa mofets'e tsa tam. |
| CPD100744 | R916562 | |
| CPD100743 | Ningetinib-tosylate | CT-053, eo hape e tsejoang e le DE-120, ke VEGF le PDGF inhibitor e ka bang teng bakeng sa ho phekola ho senyeha ha macular ho amanang le lilemo. |
| CPD100742 | SGI-7079 | SGI-7079 ke Axl inhibitor e matla le e khethang e nang le ts'ebetso e ka bang teng ea anticancer. SGI-7079 e ile ea thibela ka katleho ts'ebetso ea Axl ka pel'a Gas6 ligand e sa tloaelehang. SGI-7079 e thibetse ho hola ha hlahala ka mokhoa o itšetlehileng ka lethal dose. Axl ke sepheo sa kalafo se ka bang teng bakeng sa ho hlola EGFR inhibitor resistance. |
| CPD100741 | 2-D08 | 2-D08 ke flavone ea maiketsetso e thibelang sumoylation. 2-D08 e bonts'itse anti-aggregatory le neuroprotective effect |
| CPD100740 | Dubermatinib | Dubermatinib, e tsejoang hape e le TP-0903, ke inhibitor e matla le e khethang ea AXL. TP-0903 e kenya apoptosis e kholo liseleng tsa CLL B tse nang le boleng ba LD50 ba mefuta ea nanomolar. Motsoako oa TP-0903 le BTK inhibitors augments CLL B-cell apoptosis AXL overexpression ke sehlooho se hlahang hape se hlokometsoeng ka mefuta e mengata ea hlahala e fumaneng ho hanyetsa mahlahana a fapaneng. Kalafo ea lisele tsa mofetše ka TP-0903 e khutlisa mesenchymal phenotype mefuteng e mengata mme e hlokomelisa lisele tsa mofetše hore li phekoloe ka li-agent tse ling tse lebisitsoeng ho tsona. Tsamaiso ea TP-0903 e le moemeli a le mong kapa hammoho le BTK inhibitors e ka sebetsa hantle ho phekola bakuli ba CLL. |
| CPD100739 | NPS-1034 | NPS-1034 ke buka e ncha ea MET inhibitor, e thibelang li-receptor tsa MET tse kentsoeng le liphetoho tsa eona tse sebetsang hantle. NPS-1034, e thibela mefuta e fapaneng e sebetsang ea MET hammoho le HGF-activated wild-type MET. NPS-1034 e thibetse ho ata ha lisele tse hlalosang MET e sebelisitsoeng mme e khothalelitse ho fokotseha ha lihlahala tse entsoeng liseleng tse joalo ka mohlala oa mouse xenograft ka liketso tse khahlanong le angiogenic le pro-apoptotic. NPS-1034 e boetse e thibela ts'ebetso e tsositsoeng ea HGF ea lipontšo tsa MET boteng kapa bosieong ba serum. Ka ho hlakileng, NPS-1034 e thibetse mefuta e meraro ea MET e hanyetsanang le MET inhibitors SU11274, NVP-BVU972, le PHA665752. |
| CPD100738 | Glesatinib | Glesatinib, eo hape e tsejoang e le MGCD-265, ke bioavailable ka molomo, molek'hule e nyenyane, e nang le mefuta e mengata ea tyrosine kinase inhibitor e nang le ts'ebetso e ka 'nang ea e-ba teng ea antineoplastic. MGCD265 e tlama le ho thibela phosphorylation ea li-receptor tyrosine kinases tse 'maloa (RTKs), ho kenyelletsa le c-Met receptor (hepatocyte growth factor receptor); mokelikeli oa Tek/Tie-2; vascular endothelial growth factor receptor (VEGFR) mefuta ea 1, 2, le 3; le macrophage-stimulating 1 receptor (MST1R kapa RON). |
| CPD100737 | CEP-40783 | CEP-40783, eo hape e tsejoang ka hore ke RXDX-106, ke inhibitor e matla, e khethang le e fumanehang ka molomo ea AXL le c-Met e nang le boleng ba IC50 ba 7 nM le 12 nM, ka ho latellana bakeng sa ts'ebeliso ea sefuba, seleng ea matšoafo e seng nyane (NSCLC) , le kankere ea pancreatic. |
| CPD1725 | Bemcentinib | BGB-324, e tsejoang hape e le R428 kapa Bemcentinib, ke inhibitor e nyane ea molek'hule ea Axl kinase, e bonts'itseng ts'ebetso ea ho thibela ho ata ha hlahala le ho lelefatsa ho phela ho mefuta ea mofetše oa matsoele oa metastatic. The receptor tyrosine kinase Axl e ka bapala karolo ea bohlokoa tsoelo-peleng ea mofetše, tlhaselo, metastasis, ho hanyetsa lithethefatsi le lefu la mokuli. R428 e thibela Axl ka ts'ebetso e tlaase ea nanomolar le liketsahalo tse thibetsoeng tse itšetlehileng ka Axl, ho akarelletsa le Akt phosphorylation, tlhaselo ea lisele tsa kankere ea matsoele, le tlhahiso ea proinflammatory cytokine. |
| CPD3545 | Gilteritinib | Gilteritinib, e tsejoang hape e le ASP2215, ke inhibitor e matla ea FLT3/AXL, e bonts'itseng ts'ebetso e matla ea antileukemic khahlano le AML ka liphetoho tsa FLT3-ITD le FLT3-D835 kapa ka bobeli. Invitro, har'a 78 tyrosine kinases e lekiloeng, ASP2215 e thibetse FLT3, LTK, ALK, le AXL kinases ka ho feta 50% ho 1 nM e nang le IC50 boleng ba 0.29 nM bakeng sa FLT3, hoo e ka bang 800-fold ho feta bakeng sa c-KIT, thibelo ea eona e amanang le kotsi e ka bang teng ea myelosuppression. ASP2215 e thibelitse ho hōla ha lisele tsa MV4-11, tse nang le FLT3-ITD, tse nang le boleng ba IC50 ba 0.92 nM, e tsamaeang le ho thibela pFLT3, pAKT, pSTAT5, pERK, le pS6. ASP2215 e ile ea fokotsa boima ba hlahala mokong oa masapo 'me ea lelefatsa bophelo ba litoeba tse kentsoeng ka methapo ka lisele tsa MV4-11. ASP2215 e kanna ea ba le ts'ebeliso e ka bang teng ho alafa AML. |
| CPD100734 | UNC2881 | UNC2881 ke Mer kinase inhibitor e matla. UNC2281 e thibela phosphorylation ea Mer kinase e tsitsitseng e nang le boleng ba IC50 ba 22 nM. Kalafo e nang le UNC2281 e boetse e lekane ho thibela EGF-mediated stimulation of chimeric receptor e nang le intracellular domain ea Mer e kopantsoeng le sebaka sa extracellular sa EGFR. Ntle le moo, UNC2881 e thibela ka matla ho kopana ha liplatelete tse hlahisoang ke collagen, e fana ka maikutlo a hore sehlopha sena sa li-inhibitors se ka ba le thuso bakeng sa thibelo le/kapa kalafo ea pathologic thrombosis. |
| CPD100733 | UNC2250 | UNC2250 ke inhibitor e matla le e khethang ea Mer Kinase. Ha e sebelisoa ho lisele tse phelang, UNC2250 e ile ea thibela phosphorylation e tsitsitseng ea Mer e sa feleng ka IC50 ea 9.8 nM le ho thibela ts'ebetso ea ligand-stimulated ea chimeric EGFR-Mer protheine. Kalafo e nang le UNC2250 e boetse e felisitse ho fokotseha ha bokhoni ba ho theha kolone liseleng tsa tumor tsa rhabdoid le NSCLC, ka hona ho bonts'a ts'ebetso e sebetsang ea antitumor. Liphetho li fana ka lebaka la lipatlisiso tse ling tsa UNC2250 bakeng sa ts'ebeliso ea kalafo ho bakuli ba nang le mofetše. |
| CPD100732 | LDC1267 | LDC1267 ke TAM kinase inhibitor e matla ebile e khetha. LDC1267 e bonts'a ts'ebetso e tlase khahlano le Met, Aurora B, Lck, Src, le CDK8. LDC1267 e fokolitse haholo kankere ea mammary ea murine le melanoma metastases e itšetlehileng ka lisele tsa NK. TAM tyrosine kinase receptors Tyro3, Axl le Mer (tse tsejoang hape e le Mertk) li ile tsa khetholloa e le li-substrates tsa ubiquitylation bakeng sa Cbl-b. Kalafo ea lisele tse hlaha tsa NK tse nang le molek'hule e nyane e sa tsoa etsoa ea TAM kinase inhibitor e fane ka matla a kalafo, e matlafatsang ts'ebetso ea lisele tsa NK tsa anti-metastatic ka har'a vivo. |
| CPD100731 | BMS-777607 | BMS-777607, e tsejoang hape e le BMS-817378 le ASLAN-002, Met tyrosine kinase inhibitor, ke inhibitor ea MET tyrosine kinase e nang le ts'ebetso e ka bang teng ea antineoplastic. MET tyrosine kinase inhibitor BMS-777607 e tlama protheine ea c-Met, kapa hepatocyte growth factor receptor (HGFR), e thibelang ho tlama ha hepatocyte growth factor (HGF) le ho senya tsela ea pontšo ea MET; moemeli enoa a ka 'na a baka lefu la sele liseleng tsa tumor tse hlalosang c-Met. c-Met, receptor tyrosine kinase e fetelletseng kapa e fetotsoeng ka mefuta e mengata ea lisele tsa tumor, e phetha karolo ea bohlokoa ho ata ha lisele tsa tumor, ho pholoha, tlhaselo, le metastasis, le ho angiogenesis ea hlahala. |
| CPD100730 | Cabozantinib | Cabozantinib, eo hape e tsejoang ka hore ke XL-184 kapa BMS-907351, ke inhibitor e fumanehang ka molomo, e nyane ea molek'hule ea tyrosine kinase (RTK) e nang le ts'ebetso e ka bang teng ea antineoplastic. Cabozantinib e tlama ka matla le ho thibela tyrosine receptor kinases tse 'maloa. Ka ho khetheha, cabozantinib e bonahala e na le kamano e matla bakeng sa hepatocyte growth factor receptor (Met) le vascular endothelial growth factor receptor 2 (VEGFR2), e ka fellang ka ho thibela ho hōla ha hlahala le angiogenesis, le ho fokotseha ha hlahala. Cabozantinib e ile ea amoheloa ke US FDA ka November 2012 bakeng sa phekolo ea kankere ea qoqotho ea medulla. |
