| CAT # | Magaca Alaabta | Sharaxaada |
| CPD100501 | UNC2541 | UNC2541 waa horjooge awood leh oo MerTK-gaar ah oo muujiya waxqabadyo ka-hortagga-yar-yar ee ELISA-ku-saleysan unugga. Intaa waxaa dheer, qaab-dhismeedka raajada ee borotiinka MerTK ee kakan oo leh 11 ayaa la xalliyey si loo muujiyo in makroskooladani ay ku xidhan yihiin jeebka MerTK ATP. UNC2541 waxay muujisay IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| CPD100745 | RU-302 | RU-302 waa sheeko cusub oo pan-tam inhibitor ah, oo xannibaysa is-dhexgalka u dhexeeya tam ig1 ectodomain iyo gaaska 6 lg domain, oo si xooggan u xannibaya khadadka unugyada axl ee saxafiyiinta iyo kuwa asaliga ah ee tam receptors khadadka unugyada kansarka |
| CPD100744 | R916562 | |
| CPD100743 | Ningetinib-Tosylate | CT-053, oo sidoo kale loo yaqaan DE-120, waa VEGF iyo PDGF inhibitor oo awood u leh daaweynta da'da qoyan ee hoos u dhaca maskaxda. |
| CPD100742 | SGI-7079 | SGI-7079 waa Axl inhibitor awood leh oo la xushay oo leh firfircoonida ka hortagga kansarka. SGI-7079 waxay si wax ku ool ah u joojisay firfircoonida Axl iyada oo ay jirto ligand Gas6 exogenous. SGI-7079 waxay joojisay korriinka burada ee qiyaasta qiyaasta. Axl waa bartilmaameed daweyn oo suurtagal ah si looga gudbo iska caabbinta EGFR. |
| CPD100741 | 2-D08 | 2-D08 waa flavone synthetic oo joojisa sumoylation. 2-D08 waxay muujisay saameyn lid ku ah isku-darka iyo neuroprotective |
| CPD100740 | Dubermatinib | Dubermatinib, oo sidoo kale loo yaqaan TP-0903, waa xakameyn awood leh oo xulashada AXL. TP-0903 waxay keentaa apoptosis weyn oo ku jira unugyada CLL B oo leh LD50 qiyam ah oo kala duwan oo nanomolar ah. Isku darka TP-0903 oo leh BTK inhibitors waxay kordhisaa CLL B-unugyada apoptosis AXL xad dhaafka ah waa mawduuc soo noqnoqda oo lagu arkay noocyo badan oo burooyin ah kuwaas oo helay caabbinta wakiilada kala duwan. Daawaynta unugyada kansarka ee leh TP-0903 waxay beddeshaa phenotype mesenchymal ee noocyo badan waxayna dareensiisaa unugyada kansarka inay ku daaweeyaan wakiilada kale ee la beegsaday. Maamulka TP-0903 ha ahaato hal wakiil ama marka lagu daro BTK inhibitors waxay waxtar u yeelan kartaa daaweynta bukaanada qaba CLL. |
| CPD100739 | NPS-1034 | NPS-1034 waa hor-jooge cusub oo MET ah, kaas oo xannibaya soo-dhoweynta MET ee firfircoon iyo mutant-keeda firfircoon. NPS-1034, waxay joojisaa noocyo kala duwan oo mutant ah oo firfircoon ee MET iyo sidoo kale HGF-firfircoon ee nooca duurjoogta ah ee MET. NPS-1034 waxay joojisay faafinta unugyada muujinaya MET firfircoon waxayna kor u qaadday dib u soo noqoshada burooyinka laga sameeyay unugyadaas oo ku jira qaabka xenograft jiirka iyada oo loo marayo ficillada anti-angiogenic iyo pro-apoptotic. NPS-1034 waxay kaloo joojisay firfircoonida HGF-kicinta ee calaamadaynta MET ee joogitaanka ama maqnaanshaha serum. Si gaar ah, NPS-1034 waxay joojisay saddex nooc oo MET ah kuwaas oo u adkeysanaya MET inhibitors SU11274, NVP-BVU972, iyo PHA665752. |
| CPD100738 | Glesatinib | Glesatinib, oo sidoo kale loo yaqaan MGCD-265, waa noole afka laga heli karo, unug yar-yar, tyrosine kinase inhibitor oo badan oo bartilmaameed leh oo leh firfircoonida antineoplastic ee suurtagalka ah. MGCD265 waxay ku xidhan tahay oo joojisaa fosforyaalka dhowr tayroosin kinases (RTKs), oo ay ku jiraan soo-dhoweeyaha c-Met (receptor factor factor koritaanka hepatocyte); receptor Tek / Tie-2; Noocyada kobaca xuubka xuubka xuubka (VEGFR) ee 1, 2, iyo 3; iyo macrophage-kicinta 1 reseptor (MST1R ama RON). |
| CPD100737 | CEP-40783 | CEP-40783, oo sidoo kale loo yaqaan RXDX-106, waa mid awood leh, xulashada iyo afka laga heli karo xannibaadaha AXL iyo c-Met oo leh IC50 qiyamka 7 nM iyo 12 nM, siday u kala horreeyaan loogu isticmaalo naaska, sambabada unugyada yaryar (NSCLC) , iyo kansarrada ganaca. |
| CPD1725 | Bemcentinib | BGB-324, oo sidoo kale loo yaqaan R428 ama Bemcentinib, waa molecule yar oo la xushay ee Axl kinase, kaas oo muujiyay waxqabad si loo xakameeyo faafitaanka burada oo sii dheeraysa badbaadada moodooyinka kansarka naasaha ee metastatic. Reseptor tyrosine kinase Axl ayaa laga yaabaa inay door muhiim ah ka ciyaarto horumarka kansarka, duulaanka, metastasis, caabbinta daroogada, iyo dhimashada bukaanka. R428 waxay joojisaa Axl oo leh hawl yar oo nanomolar ah waxayna xannibtay dhacdooyinka Axl-ku-tiirsanaanta, oo ay ku jiraan Akt phosphorylation, soo-galitaanka unugyada kansarka naasaha, iyo soosaarka cytokine proinflammatory. |
| CPD3545 | Gilteritinib | Gilteritinib, oo sidoo kale loo yaqaan ASP2215, waa FLT3 / AXL inhibitor awood leh, kaas oo muujiyay firfircoonida antileukemic ee ka dhanka ah AML midkood ama labadaba FLT3-ITD iyo FLT3-D835 isbeddellada. Invitro, oo ka mid ah 78 tyrosine kinases ee la tijaabiyay, ASP2215 waxay joojisay FLT3, LTK, ALK, iyo AXL kinases in ka badan 50% at 1 nM oo leh IC50 qiimaha 0.29 nM ee FLT3, qiyaastii 800-laab ka awood badan c-KIT, Ka-hortagga kaas oo ku xiran khatarta suurtagalka ah ee myelosuppression. ASP2215 waxay joojisay korriinka unugyada MV4-11, kuwaas oo xareeya FLT3-ITD, oo leh IC50 qiimaha 0.92 nM, oo ay la socoto xannibaadda pFLT3, pAKT, pSTAT5, PERK, iyo pS6. ASP2215 waxay hoos u dhigtay culeeska buro ee dhuuxa lafta waxayna sii dheeraatay badbaadada jiirarka xididada lagu beeray unugyada MV4-11. ASP2215 waxa laga yaabaa in loo isticmaalo daawaynta AML. |
| CPD100734 | UNC2881 | UNC2881 waa ka hortag awood leh oo Mer kinase ah. UNC2281 waxay joojisaa fosforyaalka Mer kinase ee joogtada ah oo leh IC50 oo qiimaheedu yahay 22 nM. Daawaynta UNC2281 sidoo kale waa ku filan tahay in la joojiyo kicinta dhexdhexaadinta EGF ee reseptor chimeric ka kooban qaybta unugyada unugyada ee Mer oo ku xidhan qaybta ka baxsan unugga ee EGFR. Intaa waxaa dheer, UNC2881 waxay si xoog leh u joojisaa isu-ururinta platelet-ka kollagen-ku keeno, iyadoo soo jeedinaysa in fasalkan ka-hortaggayaashu ay yeelan karaan faa'iidooyin ka-hortagga iyo/ama daaweynta xinjirowga dhiigga. |
| CPD100733 | UNC2250 | UNC2250 waa ka hortagta Mer Kinase oo awood leh oo door ah. Marka lagu dabaqo unugyada nool, UNC2250 waxay joojisay fosforyaalka joogtada ah ee endogenous Mer oo leh IC50 ee 9.8 nM iyo kicinta kicinta ligand ee borotiinka chimeric EGFR-Mer. Daawaynta UNC2250 waxay sidoo kale keentay hoos u dhac ku yimaada samaynta gumaysigu ee unugyada burooyinka rhabdoid iyo NSCLC, taas oo muujinaysa waxqabadka antitumor functional. Natiijooyinku waxay bixiyaan sabab baadhis dheeraad ah oo UNC2250 ah oo loogu talagalay codsiga daweynta bukaanka qaba kansarka. |
| CPD100732 | LDC1267 | LDC1267 waa TAM kinase inhibitor awood leh oo door ah. LDC1267 waxay soo bandhigaysaa waxqabad hoose oo ka dhan ah Met, Aurora B, Lck, Src, iyo CDK8. LDC1267 waxay si muuqata hoos ugu dhacday kansarka naasaha naasaha iyo melanoma metastases ku tiirsan unugyada NK. Reseptors-ka TAM tyrosine kinase Tyro3, Axl iyo Mer (sidoo kale loo yaqaan Mertk) ayaa loo aqoonsaday inay yihiin substrates-ka meelaynta ee Cbl-b. Daawaynta unugyada NK-duur-joogta ah oo leh unug cusub oo cusub oo TAM kinase inhibitor ah ayaa siisay awood daweyn, si wax ku ool ah u wanaajisay dhaqdhaqaaqa unugyada NK-ka-hortagga-mastastatic ee vivo. |
| CPD100731 | BMS-777607 | BMS-777607, oo sidoo kale loo yaqaan BMS-817378 iyo ASLAN-002, Met tyrosine kinase inhibitor, waa horjoogaha MET tyrosine kinase oo leh firfircoonida antineoplastic ee suurtagalka ah. MET tyrosine kinase inhibitor BMS-777607 waxay ku xidhan tahay borotiinka c-Met, ama hepatocyte factor reseptor (HGFR), ka hortagga xidhitaanka factor koritaanka hepatocyte (HGF) iyo carqaladaynta jidka calaamadaynta MET; Wakiilkan ayaa laga yaabaa inuu keeno dhimashada unugyada unugyada burooyinka ee muujinaya c-Met. c-Met, reseptor tyrosine kinase xad-dhaaf ah ama beddelmay noocyo badan oo unugyada burooyinka, ayaa door muhiim ah ka ciyaara kororka unugyada burooyinka, badbaadada, duulaanka, iyo metastasis, iyo buro angiogenesis. |
| CPD100730 | Cabozantinib | Cabozantinib, oo sidoo kale loo yaqaan XL-184 ama BMS-907351, waa noole afka laga heli karo, tyrosine kinase (RTK) receptor molecule yar oo leh firfircoonida antineoplastic. Cabozantinib wuxuu si adag ugu xidhaa oo uu joojiyaa dhowr kinases tyrosine reseptor ah. Gaar ahaan, cabozantinib wuxuu u muuqdaa inuu leeyahay xiriir xooggan oo loogu talagalay hepatocyte factor factor receptor (Met) iyo vascular endothelial factor factor receptor 2 (VEGFR2), taas oo keeni karta in la joojiyo koritaanka burooyinka iyo angiogenesis, iyo dib u soo noqoshada buro. Cabozantinib waxaa ansixiyay FDA-da Mareykanka bishii Nofembar 2012 si loogu daweeyo kansarka qanjirka 'thyroid'. |
