| CAT # | Ingoa Hua | Whakaahuatanga |
| CPD100501 | UNC2541 | Ko te UNC2541 he kaiwawao kaha me te MerTK-motuhake e whakaatu ana i nga mahi aukati iti-micromolar i roto i te ELISA e pa ana ki te pūtau. I tua atu, he hanga X-ray o te pūmua MerTK i roto i te matatini me te 11 i whakatauhia hei whakaatu ka herea enei macrocycles i roto i te putea MerTK ATP. I whakaatu a UNC2541 i te IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| CPD100745 | RU-302 | Ko te RU-302 he kaitao pan-tam hou, e aukati ana i te atanga i waenga i te tam ig1 ectodomain me te rohe gas6 lg, he kaha te aukati i nga raina axl kairipoata me nga kaiwhakawhiwhi tam taketake nga raina pūtau mate pukupuku. |
| CPD100744 | R916562 | |
| CPD100743 | Ningetinib-Tosylate | Ko te CT-053, e mohiotia ana ko DE-120, he aukati VEGF me te PDGF pea mo te maimoatanga o te whakahekenga o te maaka e pa ana ki te tau. |
| CPD100742 | SGI-7079 | Ko te SGI-7079 he aukati Axl kaha me te whiriwhiri me te mahi anticancer pea. Ko te SGI-7079 i kaha te aukati i te whakahohenga a Axl i te aroaro o te herenga Gas6 o waho. Ko te SGI-7079 i aukati i te tipu o te puku i runga i te tikanga o te horopeta. Ko te Axl he kaupapa rongoa mo te aukati i te aukati aukati EGFR. |
| CPD100741 | 2-D08 | Ko te 2-D08 he flavone waihanga e aukati ana i te whakahiatotanga. I whakaatu a 2-D08 i te hua anti-agregatory me te neuroprotective |
| CPD100740 | Dubermatinib | Ko Dubermatinib, e mohiotia ana ko TP-0903, he kaha me te whiriwhiri i te aukati AXL. Ko te TP-0903 e whakaawe ana i te apoptosis nui i roto i nga ruma CLL B me nga uara LD50 o nga awhe nanomolar. Ko te whakakotahitanga o te TP-0903 me te aukati BTK hei whakanui ake i te CLL B-cell apoptosis AXL overexpression he kaupapa hou ka kitea i roto i nga momo pukupuku maha kua mau i te aukati ki nga momo apiha. Ko te maimoatanga o nga pūtau mate pukupuku me te TP-0903 ka huri i te tohu tohu mesenchymal i roto i nga tauira maha, me te whakamohio i nga pūtau mate pukupuku ki te maimoatanga me etahi atu matū kua tohua. Ko te whakahaeretanga o te TP-0903 hei kaihoko kotahi, ma te whakakotahi ranei me nga aukati BTK ka whai hua ki te rongoa i nga turoro whai CLL. |
| CPD100739 | NPS-1034 | Ko te NPS-1034 he aukati MET hou, e aukati ana i te kaiwhakawhiwhi MET kua whakahohehia me ona mutants kaha. NPS-1034, ka aukati i nga momo mutant kaha kaha o te MET tae atu ki te MET momo mohoao kua whakahohehia e te HGF. Ko te NPS-1034 i aukati i te tipu o nga pūtau e whakaatu ana i te MET kua whakahohehia, me te whakatairanga i te whakahekenga o nga pukupuku i puta mai i aua pūtau i roto i te tauira xenograft kiore na roto i nga mahi anti-angiogenic me te pro-apoptotic. Ko te NPS-1034 hoki i aukati i te whakahoahoatanga o te HGF-whakaongaonga o te tohu MET i te aroaro o te kore ranei o te serum. Ko te mea nui, ko te NPS-1034 i aukati i nga momo MET e toru e aukati ana ki nga aukati MET SU11274, NVP-BVU972, me PHA665752. |
| CPD100738 | Glesatinib | Ko te Glesatinib, e mohiotia ana ko MGCD-265, he kaiao-a-waha, he iti-ngota ngota, he aukati tyrosine kinase multitargeted me te mahi antineoplastic pea. Ko te MGCD265 te here me te aukati i te phosphorylation o te maha o nga kinases tyrosine (RTKs), tae atu ki te c-Met receptor (hepatocyte growth factor receptor); te Tek/Tie-2 receptor; vascular endothelial growth factor receptor (VEGFR) momo 1, 2, me te 3; me te kaiwhiwhi 1 whakaihiihi macrophage (MST1R, RON ranei). |
| CPD100737 | CEP-40783 | Ko te CEP-40783, e mohiotia ana ko RXDX-106, he aukati kaha, whiriwhiri me te waatea o te AXL me te c-Met me nga uara IC50 o te 7 nM me te 12 nM, mo te whakamahi i roto i te u, i te ngutu iti-iti (NSCLC) , me nga mate pukupuku pancreatic. |
| CPD1725 | Bemcentinib | Ko te BGB-324, e mohiotia ana ko R428, Bemcentinib ranei, he aukati ngota ngota iti o Axl kinase, i whakaatu i te mahi ki te aukati i te horapa puku me te whakaroa i te oranga o nga tauira o te mate pukupuku uma metastatic. Ka whai waahi nui pea te kaiwhakawhiwhi tyrosine kinase Axl ki te haere whakamua o te mate pukupuku, te whakaekenga, te metastasis, te aukati i te tarukino, me te mate turoro. Ko te R428 te aukati i te Axl me te iti o te mahi nanomolar me te aukati i nga kaupapa e whakawhirinaki ana ki a Axl, tae atu ki te Akt phosphorylation, te whakaekenga o nga pūtau mate pukupuku uma, me te hanga cytokine proinflammatory. |
| CPD3545 | Gilteritinib | Ko Gilteritinib, e mohiotia ana ko ASP2215, he aukati FLT3/AXL kaha, i whakaatu i nga mahi antileukemic kaha ki te AML me nga huringa FLT3-ITD me FLT3-D835 ranei. I roto i te invitro, i roto i te 78 tyrosine kinases i whakamatauria, ASP2215 inhibited FLT3, LTK, ALK, me AXL kinases i runga i te 50% i te 1 nM me te uara IC50 o 0.29 nM mo te FLT3, tata ki te 800-nui ake te kaha atu i te c-KIT, ko te aukati e hono ana ki te tupono o te myelosuppression. I whakakorehia e te ASP2215 te tipu o nga pūtau MV4-11, e whanga ana i te FLT3-ITD, me te uara IC50 o 0.92 nM, me te aukati i te pFLT3, pAKT, pSTAT5, pERK, me te pS6. I whakaitihia e te ASP2215 te taumahatanga o te puku i roto i te hinu wheua me te whakaroa i te oranga o nga kiore i whakawhitia ki roto i nga ruma MV4-11. Ka taea pea te ASP2215 ki te rongoa i te AML. |
| CPD100734 | UNC2881 | Ko te UNC2881 he aukati Mer kinase kaha. Ka whakakorehia e te UNC2281 te phosphorylation Mer kinase u tonu me te uara IC50 o te 22 nM. Ko te maimoatanga me te UNC2281 e ranea ana ki te aukati i te whakaihiihi a EGF-takawaenga o te kaikawe chimeric kei roto te rohe intracellular o Mer kua honoa ki te rohe extracellular o EGFR. I tua atu, ka kaha te aukati a UNC2881 i te whakahiato pereti na te collagen-induced platelet, e kii ana tera pea he whaipainga tenei momo aukati mo te aukati me te maimoatanga o te thrombosis pathologic. |
| CPD100733 | UNC2250 | Ko te UNC2250 he aukati Mer Kinase kaha me te whiriwhiri. I te tono ki nga pūtau ora, ka aukati te UNC2250 i te phosphorylation o te Mer endogenous me te IC50 o te 9.8 nM me te aukati i te whakahoahoatanga o te ligand-stimulated o te pūmua EGFR-Mer chimeric. Ko te maimoatanga me te UNC2250 i heke iho te kaha o te hanga koroni i roto i te rhabdoid me te NSCLC pūtau puku, na reira ka whakaatu te mahi antitumor mahi. Ko nga hua ka puta he take mo te tirotiro ano mo te UNC2250 mo te tono rongoa mo nga turoro mate pukupuku. |
| CPD100732 | LDC1267 | Ko te LDC1267 he kaha me te whiriwhiri i te TAM kinase inhibitor. Ko te LDC1267 e whakaatu ana i nga mahi iti ki a Met, Aurora B, Lck, Src, me CDK8. LDC1267 i tino whakahekehia te mate pukupuku mammary murine me nga metastases melanoma e whakawhirinaki ana ki nga pūtau NK. Ko te TAM tyrosine kinase receptors Tyro3, Axl me Mer (e mohiotia ana ko Mertk) i tohuhia hei taputapu ubiquitylation mo Cbl-b. Ko te maimoatanga o nga pūtau NK momo mohoao me te ngota ngota iti katahi ano ka whanakehia te aukati TAM kinase i whakawhiwhia ki te kaha whakaora, e pai ana te whakarei ake i nga mahi pūtau NK anti-metastatic i roto i te vivo. |
| CPD100731 | BMS-777607 | Ko te BMS-777607, e mohiotia ana ko BMS-817378 me te ASLAN-002, he aukati Met tyrosine kinase, he aukati o te MET tyrosine kinase me te mahi antineoplastic pea. MET tyrosine kinase inhibitor BMS-777607 herea ki c-Met pūmua, hepatocyte growth factor receptor (HGFR) ranei, te aukati i te herenga o te tauwehe tipu hepatocyte (HGF) me te whakakore i te huarahi tohu MET; ka mate pea tenei kaihoko i te mate o te pūtau i roto i nga pūtau puku e whakaatu ana i te c-Met. Ko te c-Met, he kaikawe tyrosine kinase kua whakahiatohia, kua whakarereketia ranei i roto i te maha o nga momo pūtau puku, ka whai waahi nui ki te tipu o te pūtau puku, te oranga, te whakaekenga, me te metastasis, me te angiogenesis puku. |
| CPD100730 | Cabozantinib | Ko te Cabozantinib, e mohiotia ana ko XL-184, BMS-907351 ranei, he kaiao-a-waha e waatea ana ki te waha, he iti nei te whakangao i te ngota whakangao ngota tyrosine kinase (RTK) me te mahi antineoplastic pea. He kaha te here a Cabozantinib me te aukati i te maha o nga kinases kaikawe tyrosine. Ko te mea nui, ko te cabozantinib te ahua o te hononga kaha mo te kaitautoko o te tipu o te hepatocyte (Met) me te vascular endothelial growth factor receptor 2 (VEGFR2), ka taea te whakakore i te tipu o te pukupuku me te angiogenesis, me te whakahekenga o te pukupuku. I whakaaetia a Cabozantinib e te US FDA i te marama o Whiringa-a-rangi 2012 mo te maimoatanga o te mate pukupuku thyroid medullary. |
