| CAT # | Igama lemveliso | Inkcazo |
| CPD100501 | UNC2541 | I-UNC2541 inamandla kunye ne-MerTK-specific inhibitor ebonisa umsebenzi we-sub-micromolar inhibitory kwi-cell-based ELISA. Ukongezelela, isakhiwo se-X-ray seprotheni ye-MerTK kwi-complex kunye ne-11 yasombululwa ukubonisa ukuba ezi macrocycles zibophe kwi-pocket ye-MerTK ATP. I-UNC2541 ibonise i-IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| CPD100745 | RU-302 | I-RU-302 iyinoveli ye-pan-tam inhibitor, ivalela ujongano phakathi kwe-tam ig1 ectodomain kunye ne-gas6 lg domain, inqanda ngokunamandla imigca yeeseli ze-axl kunye nemigca yeeseli zomhlaza ze-tam receptors. |
| CPD100744 | R916562 | |
| CPD100743 | I-Ningetinib-Tosylate | I-CT-053, ekwabizwa ngokuba yi-DE-120, yi-VEGF kunye ne-PDGF inhibitor enokubakho kunyango lwe-macular degeneration emanzi enxulumene nobudala. |
| CPD100742 | SGI-7079 | I-SGI-7079 yinto enamandla kunye ne-Axl inhibitor ekhethiweyo kunye nomsebenzi onokuthi ube ne-anticancer. I-SGI-7079 ithintele ngokufanelekileyo ukusebenza kwe-Axl phambi kobukho be-Gas6 ligand yangaphandle. I-SGI-7079 ithintele ukukhula kwethumba ngendlela exhomekeke kwithamo. I-Axl yinto ekujoliswe kuyo yonyango enokuthi iphumelele ukuxhatshazwa kwe-EGFR inhibitor. |
| CPD100741 | 2-D08 | I-2-D08 yi-flavone yokwenziwa evimbela ukuxutywa kwe-sumoylation. I-2-D08 ibonise i-anti-aggregatory kunye ne-neuroprotective effect |
| CPD100740 | I-Dubermatinib | I-Dubermatinib, eyaziwa ngokuba yi-TP-0903, inamandla kwaye i-AXL inhibitor ekhethiweyo. I-TP-0903 yenza i-apoptosis enkulu kwiiseli ze-CLL B ezinexabiso le-LD50 le-nanomolar ranges. Ukudityaniswa kwe-TP-0903 kunye ne-BTK inhibitors augments CLL B-cell apoptosis AXL overexpression ngumxholo oqhubekayo obonwa kwiintlobo ezininzi zamathumba eziye zafumana ukuxhathisa kwii-arhente ezahlukeneyo. Unyango lweeseli zomhlaza nge-TP-0903 ibuyisela umva i-mesenchymal phenotype kwiimodeli ezininzi kwaye ivuselele iiseli zomhlaza kunyango kunye nezinye iiarhente ezichongiweyo. Ulawulo lwe-TP-0903 mhlawumbi njenge-arhente enye okanye ngokudibanisa ne-BTK inhibitors inokusebenza ekunyangeni izigulane ezine-CLL. |
| CPD100739 | NPS-1034 | I-NPS-1034 iyinoveli ye-MET inhibitor, evimbela i-MET receptor esebenzayo kunye ne-constitutively active mutants. I-NPS-1034, inqanda iindlela ezahlukeneyo eziguqukayo ezisebenzayo ze-MET kunye ne-HGF-activated wild-type MET. I-NPS-1034 ithintele ukwanda kweeseli ezibonisa i-MET esebenzayo kwaye yakhuthaza ukuhlehla kwamathumba akhiwe kwiiseli ezinjalo kwimodeli ye-mouse xenograft ngokusebenzisa izenzo ezichasene ne-angiogenic kunye ne-pro-apoptotic. I-NPS-1034 iphinde ivimbele ukusetyenziswa kwe-HGF-ivuselelwe ukubonakaliswa kwe-MET kubukho okanye ukungabikho kwe-serum. Ngokucacileyo, i-NPS-1034 inqanda iintlobo ezintathu ze-MET ezichasene ne-MET inhibitors SU11274, NVP-BVU972, kunye ne-PHA665752. |
| CPD100738 | Glesatinib | I-Glesatinib, eyaziwa ngokuba yi-MGCD-265, i-bioavailable yomlomo, i-molecule encinci, i-multitargeted tyrosine kinase inhibitor enokuthi isebenze i-antineoplastic. I-MGCD265 ibophelela kwaye inqanda i-phosphorylation ye-receptor tyrosine kinases (RTKs) ezininzi, kuquka i-c-Met receptor (i-hepatocyte ukukhula factor receptor); i-Tek/Tie-2 receptor; i-vascular endothelial growth factor receptor (VEGFR) iindidi ze-1, i-2, kunye ne-3; kunye ne-macrophage-stimulating 1 receptor (MST1R okanye RON). |
| CPD100737 | CEP-40783 | I-CEP-40783, eyaziwa ngokuba yi-RXDX-106, i-inhibitor enamandla, ekhethiweyo kwaye efumaneka ngomlomo ye-AXL kunye ne-c-Met kunye nexabiso le-IC50 le-7 nM kunye ne-12 nM, ngokulandelanayo ukusetyenziswa kwebele, i-cell cell lung engeyincinci (NSCLC) , kunye nomhlaza we-pancreatic. |
| CPD1725 | Bemcentinib | I-BGB-324, ekwabizwa ngokuba yi-R428 okanye i-Bemcentinib, sisithinteli esincinci se-molecule ye-Axl kinase, ebonise umsebenzi wokuthintela ukusasazeka kwethumba kunye nokwandisa ukusinda kwiimodeli zomhlaza webele we-metastatic. I-receptor tyrosine kinase Axl inokudlala indima ebalulekileyo ekuqhubekeni komhlaza, ukuhlasela, i-metastasis, ukunganyangeki kweziyobisi, kunye nokufa kwesigulane. I-R428 inqanda i-Axl kunye nomsebenzi ophantsi we-nanomolar kwaye ivalwe iziganeko ezixhomekeke kwi-Axl, kuquka i-Akt phosphorylation, i-cell cancer invasion cell, kunye ne-proinflammatory cytokine production. |
| CPD3545 | Gilteritinib | I-Gilteritinib, eyaziwa ngokuba yi-ASP2215, i-FLT3 / AXL inhibitor enamandla, ebonise umsebenzi onamandla we-antileukemic ngokuchasene ne-AML kunye nokuba okanye zombini i-FLT3-ITD kunye ne-FLT3-D835 utshintsho. I-invitro, phakathi kwe-78 tyrosine kinases evavanyiweyo, i-ASP2215 inhibited FLT3, LTK, ALK, kunye ne-AXL kinases ngaphezu kwe-50% kwi-1 nM enexabiso le-IC50 le-0.29 nM ye-FLT3, malunga ne-800-fold more than c-KIT, uthintelo oludityaniswe nobungozi obunokubakho be-myelosuppression. I-ASP2215 inqanda ukukhula kweeseli ze-MV4-11, ezigcina i-FLT3-ITD, enexabiso le-IC50 le-0.92 nM, ihamba kunye nokuvinjelwa kwe-pFLT3, pAKT, pSTAT5, pERK, kunye ne-pS6. I-ASP2215 yehlise umthwalo wethumba kumongo wethambo kwaye yandisa ukusinda kweempuku ezifakwe emithanjeni ngeeseli ze-MV4-11. I-ASP2215 inokuba nokusetyenziswa okunokubakho ekunyangeni i-AML. |
| CPD100734 | UNC2881 | I-UNC2881 yi-Mer kinase inhibitor enamandla. I-UNC2281 inqanda i-phosphorylation ye-Mer kinase ezinzileyo enexabiso le-IC50 le-22 nM. Unyango kunye ne-UNC2281 lukwanele ukuvimba i-EGF-mediated stimulation ye-chimeric receptor equkethe i-intracellular domain ye-Mer edibeneyo kwi-domain ye-extracellular ye-EGFR. Ukongeza, i-UNC2881 inhibits ngokunamandla i-collagen-induced platelet aggregation, icebisa ukuba olu didi lwe-inhibitors lunokuba luncedo lokuthintela kunye/okanye unyango lwe-pathologic thrombosis. |
| CPD100733 | UNC2250 | I-UNC2250 inamandla kwaye ikhetha i-Mer Kinase inhibitor. Xa isetyenziswe kwiiseli eziphilayo, i-UNC2250 inhibited steady-state phosphorylation ye-endogenous Mer kunye ne-IC50 ye-9.8 nM kunye ne-blocked ligand-stimulated activation ye-chimeric EGFR-Mer protein. Unyango nge-UNC2250 lukhokelele ekuncipheni kokukwazi ukwenza ikholoni kwiiseli zethumba le-rhabdoid kunye ne-NSCLC, ngaloo ndlela kuboniswa umsebenzi wokulwa nethumba. Iziphumo zibonelela ngengqiqo yophando oluthe kratya lwe-UNC2250 yesicelo sonyango kwizigulana ezinomhlaza. |
| CPD100732 | I-LDC1267 | I-LDC1267 yi-TAM kinase inhibitor enamandla kwaye ekhethiweyo. I-LDC1267 ibonisa umsebenzi ophantsi ngokuchasene ne-Met, i-Aurora B, i-Lck, i-Src, kunye ne-CDK8. I-LDC1267 yanciphisa ngokuphawulekayo umhlaza webele we-murine kunye ne-melanoma metastases exhomekeke kwiiseli ze-NK. I-TAM ye-tyrosine kinase receptors iTyro3, i-Axl kunye ne-Mer (eyaziwa nangokuthi i-Mertk) ichongiwe njenge-ubiquitylation substrates ye-Cbl-b. Unyango lweeseli ze-NK zasendle ezinemolekyuli encinci esanda kuphuhliswa i-TAM kinase inhibitor enikezela amandla onyango, ngokufanelekileyo iphucula umsebenzi weseli we-NK we-anti-metastatic kwi-vivo. |
| CPD100731 | BMS-777607 | I-BMS-777607, eyaziwa ngokuba yi-BMS-817378 kunye ne-ASLAN-002, i-Met tyrosine kinase inhibitor, i-inhibitor ye-MET tyrosine kinase enokuthi ibe nomsebenzi we-antineoplastic. I-MET tyrosine kinase inhibitor BMS-777607 ibophelela kwiprotheni ye-c-Met, okanye i-hepatocyte ukukhula factor receptor (HGFR), ukuthintela ukubophelela kwe-hepatocyte factor factor (HGF) kunye nokuphazamisa indlela yokubonakalisa i-MET; le arhente inokubangela ukufa kweeseli kwiiseli zethumba ezibonisa i-c-Met. I-c-Met, i-receptor tyrosine kinase igqithise okanye iguqulwe kwiintlobo ezininzi zeeseli zethumba, idlala indima ebalulekileyo ekwandeni kweseli yethumba, ukusinda, ukuhlasela, kunye ne-metastasis, kunye ne-tumor angiogenesis. |
| CPD100730 | Cabozantinib | I-Cabozantinib, eyaziwa ngokuba yi-XL-184 okanye i-BMS-907351, i-bioavailable ngomlomo, i-molecule encinci ye-receptor tyrosine kinase (RTK) inhibitor enokuthi isebenze i-antineoplastic. I-Cabozantinib ibophelela kakhulu kwaye inqanda i-tyrosine receptor kinases ezininzi. Ngokukodwa, i-cabozantinib ibonakala inobudlelwane obuqinileyo kwi-hepatocyte growth factor receptor (Met) kunye ne-vascular endothelial growth factor receptor 2 (VEGFR2), enokubangela ukuvinjelwa kokukhula kwe-tumor kunye ne-angiogenesis, kunye ne-tumor regression. I-Cabozantinib yamkelwa yi-US FDA ngoNovemba 2012 kunyango lwe-medullary thyroid cancer. |
