| MPAKA # | Dzina lazogulitsa | Kufotokozera |
| CPD100501 | UNC2541 | UNC2541 ndi choletsa champhamvu komanso cha MerTK-specific chomwe chimawonetsa zochitika zoletsa ma micromolar mu cell-based ELISA. Kuphatikiza apo, mawonekedwe a X-ray a mapuloteni a MerTK muzovuta ndi 11 adatsimikiza kuti ma macrocycles awa amamanga m'thumba la MerTK ATP. UNC2541 inawonetsa IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| Chithunzi cha CPD100745 | Mtengo wa RU-302 | RU-302 ndi buku la pan-tam inhibitor, kutsekereza mawonekedwe pakati pa tam ig1 ectodomain ndi gas6 lg domain, kuletsa mwamphamvu ma cell a axl atolankhani ndi mizere yama cell a tam receptors. |
| CPD100744 | Mtengo wa 916562 | |
| CPD100743 | Ningetinib-tosylate | CT-053, yomwe imadziwikanso kuti DE-120, ndi VEGF ndi PDGF inhibitor yomwe ingathe kuchiza kunyowa kwa macular chifukwa cha ukalamba. |
| Chithunzi cha CPD100742 | SGI-7079 | SGI-7079 ndi Axl inhibitor yamphamvu komanso yosankha yokhala ndi zochita zolimbana ndi khansa. SGI-7079 inaletsa bwino Axl kutsegula pamaso pa exogenous Gas6 ligand. SGI-7079 inaletsa kukula kwa chotupa m'njira yodalira mlingo. Axl ndi chandamale chothandizira kuthana ndi EGFR inhibitor resistance. |
| CPD100741 | 2-D08 | 2-D08 ndi flavone yopanga yomwe imalepheretsa sumoylation. 2-D08 inawonetsa anti-aggregatory ndi neuroprotective effect |
| CPD100740 | Dubematinib | Dubermatinib, yomwe imadziwikanso kuti TP-0903, ndi yamphamvu komanso yosankha AXL inhibitor. TP-0903 imapangitsa apoptosis yayikulu m'maselo a CLL B okhala ndi ma LD50 amitundu ya nanomolar. Kuphatikiza kwa TP-0903 ndi BTK inhibitors augments CLL B-cell apoptosis AXL overexpression ndi mutu wobwerezabwereza womwe umawonedwa mumitundu ingapo ya chotupa yomwe yayamba kukana othandizira osiyanasiyana. Kuchiza kwa ma cell a khansa ndi TP-0903 kumabweza mesenchymal phenotype m'mitundu ingapo ndikulimbikitsa ma cell a khansa kuti alandire chithandizo ndi othandizira ena omwe akuwaganizira. Ulamuliro wa TP-0903 mwina ngati wothandizira m'modzi kapena kuphatikiza ndi BTK inhibitors zitha kukhala zothandiza pochiza odwala omwe ali ndi CLL. |
| CPD100739 | NPS-1034 | NPS-1034 ndi buku la MET inhibitor, lomwe limalepheretsa cholandilira cha MET chokhazikitsidwa ndi zosinthika zake zosinthika. NPS-1034, imalepheretsa mitundu yosiyanasiyana yosinthika ya MET komanso HGF-activated wild-type MET. NPS-1034 inaletsa kuchuluka kwa maselo omwe akuwonetsa MET yoyendetsedwa ndikulimbikitsa kuyambiranso kwa zotupa zomwe zimapangidwa kuchokera ku maselo oterowo mumtundu wa mbewa wa xenograft kudzera muzochita zotsutsa-angiogenic ndi pro-apoptotic. NPS-1034 idaletsanso kuyambitsa kwa HGF-kukondoweza kwa siginecha ya MET pamaso kapena kusakhalapo kwa seramu. Makamaka, NPS-1034 idaletsa mitundu itatu ya MET yomwe imalimbana ndi MET inhibitors SU11274, NVP-BVU972, ndi PHA665752. |
| CPD100738 | Glesatinib | Glesatinib, yomwe imadziwikanso kuti MGCD-265, ndi bioavailable pamlomo, yaing'ono-molecule, multitargeted tyrosine kinase inhibitor yomwe ingathe kuchitapo kanthu. MGCD265 imamangiriza ndi kulepheretsa phosphorylation ya angapo receptor tyrosine kinases (RTKs), kuphatikizapo c-Met receptor (hepatocyte kukula factor receptor); cholandilira cha Tek/Tie-2; vascular endothelial growth factor receptor (VEGFR) mitundu 1, 2, ndi 3; ndi macrophage-stimulating 1 receptor (MST1R kapena RON). |
| CPD100737 | CEP-40783 | CEP-40783, yomwe imadziwikanso kuti RXDX-106, ndi inhibitor yamphamvu, yosankha komanso yopezeka pakamwa ya AXL ndi c-Met yokhala ndi IC50 milingo ya 7 nM ndi 12 nM, motsatana kuti igwiritsidwe ntchito m'mawere, mapapo osang'onoting'ono (NSCLC) , ndi khansa ya kapamba. |
| Chithunzi cha CPD1725 | Bemcentinib | BGB-324, yomwe imadziwikanso kuti R428 kapena Bemcentinib, ndiyomwe inhibitor yaying'ono ya Axl kinase, yomwe imawonetsa ntchito yoletsa kufalikira kwa chotupa ndikutalikitsa kupulumuka kwamitundu ya khansa ya m'mawere ya metastatic. The receptor tyrosine kinase Axl ikhoza kukhala ndi gawo lofunikira pakukula kwa khansa, kuwukira, metastasis, kukana mankhwala, komanso kufa kwa odwala. R428 imalepheretsa Axl yokhala ndi ntchito yotsika ya nanomolar ndikuletsa zochitika zodalira Axl, kuphatikizapo Akt phosphorylation, kuukira kwa khansa ya m'mawere, ndi proinflammatory cytokine kupanga. |
| Chithunzi cha CPD3545 | Gilteritinib | Gilteritinib, yomwe imadziwikanso kuti ASP2215, ndi inhibitor yamphamvu ya FLT3/AXL, yomwe imasonyeza zochita zamphamvu za antileukemic motsutsana ndi AML ndi kusintha kwa FLT3-ITD ndi FLT3-D835. Invitro, pakati pa 78 tyrosine kinases yoyesedwa, ASP2215 inhibited FLT3, LTK, ALK, ndi AXL kinases ndi oposa 50% pa 1 nM ndi IC50 mtengo wa 0.29 nM wa FLT3, pafupifupi 800-fold more than c-KIT, kuletsa kwake komwe kumalumikizidwa ndi chiopsezo cha myelosuppression. ASP2215 inalepheretsa kukula kwa maselo a MV4-11, omwe amakhala ndi FLT3-ITD, ndi IC50 mtengo wa 0.92 nM, limodzi ndi kuletsa pFLT3, pAKT, pSTAT5, pERK, ndi pS6. ASP2215 idachepetsa kuchuluka kwa chotupa m'mafupa ndikutalikitsa moyo wa mbewa zomwe zidayikidwa m'mitsempha ndi ma cell a MV4-11. ASP2215 ikhoza kugwiritsidwa ntchito pochiza AML. |
| CPD100734 | UNC2881 | UNC2881 ndi Mer kinase inhibitor yamphamvu. UNC2281 imalepheretsa kukhazikika kwa Mer kinase phosphorylation yokhala ndi mtengo wa IC50 wa 22 nM. Kuchiza ndi UNC2281 ndikokwaniranso kuletsa kukondoweza kwa EGF-mediated ya chimeric receptor yomwe ili ndi intracellular domain ya Mer yosakanikirana ndi domain extracellular ya EGFR. Kuphatikiza apo, UNC2881 imalepheretsa kuphatikizika kwa mapulateleti opangidwa ndi collagen, kutanthauza kuti zoletsa izi zitha kukhala zothandiza popewa komanso/kapena kuchiza matenda a thrombosis. |
| CPD100733 | UNC2250 | UNC2250 ndi choletsa champhamvu komanso chosankha cha Mer Kinase. Ikagwiritsidwa ntchito m'maselo amoyo, UNC2250 inhibited steady-state phosphorylation ya endogenous Mer ndi IC50 ya 9.8 nM ndipo inatseka ligand-stimulated activation ya chimeric EGFR-Mer mapuloteni. Kuchiza ndi UNC2250 kudapangitsanso kuchepa kwa kuthekera kopanga koloni m'maselo a chotupa a rhabdoid ndi NSCLC, potero kuwonetsa magwiridwe antchito a antitumor. Zotsatirazi zimapereka chifukwa chofufuzira mopitilira UNC2250 pakugwiritsa ntchito achire kwa odwala omwe ali ndi khansa. |
| CPD100732 | Chithunzi cha LDC1267 | LDC1267 ndi yamphamvu komanso yosankha TAM kinase inhibitor. LDC1267 ikuwonetsa zochitika zochepa motsutsana ndi Met, Aurora B, Lck, Src, ndi CDK8. LDC1267 yachepetsa kwambiri khansa ya m'mawere ya murine ndi metastases ya melanoma yodalira ma NK cell. Ma receptor a TAM tyrosine kinase Tyro3, Axl ndi Mer (omwe amadziwikanso kuti Mertk) adazindikirika ngati magawo a ubiquitylation a Cbl-b. Kuchiza kwa ma cell akuthengo amtundu wa NK okhala ndi kamolekyu kakang'ono kamene kamapangidwa kumene ka TAM kinase inhibitor kunapatsa mphamvu zochizira, kupititsa patsogolo magwiridwe antchito a anti-metastatic NK cell mu vivo. |
| CPD100731 | BMS-777607 | BMS-777607, yomwe imadziwikanso kuti BMS-817378 ndi ASLAN-002, Met tyrosine kinase inhibitor, ndi inhibitor ya MET tyrosine kinase yomwe ingathe kuchitapo kanthu. MET tyrosine kinase inhibitor BMS-777607 imamangiriza ku c-Met mapuloteni, kapena hepatocyte growth factor receptor (HGFR), kuteteza kumanga kwa hepatocyte kukula factor (HGF) ndi kusokoneza njira yowonetsera MET; wothandizira uyu angayambitse kufa kwa maselo m'maselo otupa omwe akuwonetsa c-Met. c-Met, cholandilira tyrosine kinase chodziwikiratu kapena chosinthika mumitundu yambiri yama cell chotupa, chimakhala ndi gawo lofunikira pakuchulukira kwa maselo a chotupa, kupulumuka, kuwukira, ndi metastasis, komanso mu chotupa angiogenesis. |
| CPD100730 | Kabozantinib | Cabozantinib, yomwe imadziwikanso kuti XL-184 kapena BMS-907351, ndi inhibitor yapakamwa ya bioavailable, yaing'ono ya molekyulu ya receptor tyrosine kinase (RTK) yokhala ndi zochita za antineoplastic. Cabozantinib imamangiriza mwamphamvu ndikuletsa ma tyrosine receptor kinases angapo. Mwachindunji, cabozantinib ikuwoneka kuti ili ndi chiyanjano cholimba cha hepatocyte growth factor receptor (Met) ndi vascular endothelial growth factor receptor 2 (VEGFR2), zomwe zingayambitse kulepheretsa kukula kwa chotupa ndi angiogenesis, ndi kuchepa kwa chotupa. Cabozantinib idavomerezedwa ndi US FDA mu Novembala 2012 pochiza khansa ya medullary chithokomiro. |
