| CAT # | Inoa Huahana | wehewehe |
| CPD100501 | UNC2541 | ʻO UNC2541 kahi mea hoʻopaneʻe ikaika a me MerTK-specific e hōʻike ana i ka hana pale sub-micromolar i ka ELISA i hoʻokumu ʻia. Eia kekahi, ua hoʻoholo ʻia kahi hanana X-ray o MerTK protein i loko o ka paʻakikī me 11 e hōʻike i ka paʻa ʻana o kēia mau macrocycles i ka ʻeke MerTK ATP. Ua hōʻike ʻo UNC2541 iā IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| CPD100745 | RU-302 | ʻO RU-302 kahi mea hoʻopaneʻe pan-tam hou, e ālai ana i ka pilina ma waena o tam ig1 ectodomain a me gas6 lg domain, hiki ke pale i nā laina kelepona axl reporter a me nā mea hoʻokipa tam maoli. |
| CPD100744 | R916562 | |
| CPD100743 | Ningetinib-Tosylate | ʻO CT-053, ʻike ʻia hoʻi ʻo DE-120, he VEGF a me PDGF inhibitor hiki ke mālama i ka macular degeneration pili i ka makahiki. |
| CPD100742 | SGI-7079 | ʻO SGI-7079 kahi mea hoʻopaneʻe Axl ikaika a koho me ka hana anticancer. Ua pale pono ʻo SGI-7079 i ka hoʻoulu ʻana o Axl i mua o ka ligand Gas6 exogenous. Ua kāohi ʻo SGI-7079 i ka ulu ʻana o ka maʻi maʻi ma ke ʻano i hilinaʻi ʻia. ʻO Axl kahi pahuhopu lapaʻau kūpono no ka lanakila ʻana i ka pale ʻana i ka EGFR inhibitor. |
| CPD100741 | 2-D08 | ʻO 2-D08 kahi flavone synthetic e pale ai i ka sumoylation. Ua hōʻike ʻo 2-D08 i ka hopena anti-aggregatory a me ka neuroprotective |
| CPD100740 | ʻO Dubermatinib | ʻO Dubermatinib, ka mea i kapa ʻia ʻo TP-0903, he mea hoʻokae AXL ikaika a koho. Hoʻoulu ʻo TP-0903 i ka apoptosis nui i nā pūnae CLL B me nā waiwai LD50 o nā pae nanomolar. ʻO ka hui pū ʻana o TP-0903 me BTK inhibitors e hoʻonui i ka CLL B-cell apoptosis AXL overexpression kahi kumuhana reoccurring i ʻike ʻia i nā ʻano tumora he nui i loaʻa ke kū'ē i nā ʻano mea like ʻole. ʻO ka mālama ʻana i nā pūnaewele maʻi maʻi me TP-0903 e hoʻohuli i ka mesenchymal phenotype i loko o nā kumu hoʻohālike he nui a hoʻonaʻauao i nā cell cancer i ka mālama ʻana me nā mea hana ʻē aʻe. ʻO ka lawelawe ʻana o TP-0903 ma ke ʻano he mea hoʻokahi a i hui pū ʻia me nā mea hoʻopaneʻe BTK hiki ke kūpono i ka mālama ʻana i nā maʻi me CLL. |
| CPD100739 | NPS-1034 | ʻO NPS-1034 kahi mea hoʻopaneʻe MET hou, kahi e kāohi ai i ka mea hoʻokipa MET i hoʻāla ʻia a me kāna mau mutants constitutively actively actively. NPS-1034, kaohi i nā ʻano mutant constitutively active o MET a me HGF-activated wild-type MET. Ua kāohi ʻo NPS-1034 i ka hoʻonui ʻana o nā cell e hōʻike ana i ka MET i hoʻāla ʻia a hāpai i ka regression o nā maʻi koko i hoʻokumu ʻia mai ia mau cell i loko o kahi hoʻohālike xenograft mouse ma o nā hana anti-angiogenic a pro-apoptotic. ʻO NPS-1034 hoʻi i kāohi i ka hoʻoulu ʻana o ka HGF-hoʻoulu ʻia o ka hōʻailona MET i ke alo a i ʻole ka nele o ka serum. ʻO ka mea nui, ua kāohi ʻo NPS-1034 i ʻekolu mau ʻokoʻa MET e kū kūʻē i ka MET inhibitors SU11274, NVP-BVU972, a me PHA665752. |
| CPD100738 | ʻO Glesatinib | ʻO Glesatinib, ka mea i ʻike ʻia ʻo MGCD-265, he mea hiki ke hoʻohana ʻia i ka waha, liʻiliʻi-mole, multitargeted tyrosine kinase inhibitor me ka hana antineoplastic. Hoʻopili ʻo MGCD265 a hoʻopaʻa i ka phosphorylation o kekahi mau receptor tyrosine kinases (RTKs), me ka c-Met receptor (hepatocyte growth factor receptor); ka mea hoʻokipa Tek/Tie-2; vascular endothelial growth factor receptor (VEGFR) ʻano 1, 2, a me 3; a me ka macrophage-stimulating 1 receptor (MST1R a i ʻole RON). |
| CPD100737 | CEP-40783 | ʻO CEP-40783, i ʻike ʻia ʻo RXDX-106, he mea hoʻopaneʻe ikaika, koho a loaʻa i ka waha o AXL a me c-Met me nā koina IC50 o 7 nM a me 12 nM, kēlā me kēia no ka hoʻohana ʻana i ka umauma, non-small cell lung (NSCLC) , a me na ma'i ma'i pancreatic. |
| CPD1725 | ʻO Bemcentinib | ʻO ka BGB-324, ka mea i kapa ʻia ʻo R428 a i ʻole Bemcentinib, he mea hoʻopaneʻe molekele liʻiliʻi koho o Axl kinase, ka mea i hōʻike i ka hana e pale ai i ka laha ʻana a hoʻolōʻihi i ke ola ʻana i nā ʻano o ka maʻi maʻi umauma metastatic. Hiki i ka receptor tyrosine kinase Axl ke hoʻokani i kahi hana koʻikoʻi i ka piʻi ʻana o ka maʻi kanesa, ka hoʻouka ʻana, ka metastasis, ka pale ʻana i ka lāʻau, a me ka make maʻi. Hoʻopaʻa ʻo R428 iā Axl me ka haʻahaʻa nanomolar haʻahaʻa a hoʻopaʻa ʻia i nā hanana hilinaʻi Axl, me ka Akt phosphorylation, ka hoʻouka ʻana o ka maʻi maʻi umauma, a me ka hana proinflammatory cytokine. |
| CPD3545 | ʻO Gilteritinib | ʻO Gilteritinib, ka mea i ʻike ʻia ʻo ASP2215, he mea hoʻopio FLT3/AXL ikaika, i hōʻike i ka hana antileukemic ikaika e kūʻē iā AML me nā hoʻololi FLT3-ITD a me FLT3-D835. Invitro, ma waena o nā 78 tyrosine kinases i hoʻāʻo ʻia, ASP2215 inhibited FLT3, LTK, ALK, a me AXL kinases ma luna o 50% ma 1 nM me kahi waiwai IC50 o 0.29 nM no FLT3, ma kahi o 800-fold ʻoi aku ka ikaika ma mua o ka c-KIT, ʻO ka hoʻopaʻa ʻana e pili ana i kahi pilikia o ka myelosuppression. Ua kāohi ʻo ASP2215 i ka ulu ʻana o nā pūnaewele MV4-11, kahi i hoʻopaʻa ai i ka FLT3-ITD, me kahi waiwai IC50 o 0.92 nM, i hui pū ʻia me ka pale ʻana o pFLT3, pAKT, pSTAT5, pERK, a me pS6. Ua hoʻemi ʻo ASP2215 i ke kaumaha o ka maʻi maʻi ma ka iwi iwi a ua hoʻolōʻihi i ke ola o nā ʻiole i hoʻololi ʻia me ka MV4-11 cell. Hiki ke hoʻohana ʻia ka ASP2215 i ka mālama ʻana i ka AML. |
| CPD100734 | UNC2881 | ʻO UNC2881 kahi mea hoʻopaneʻe Mer kinase ikaika. ʻO UNC2281 ke kāohi i ka phosphorylation Mer kinase me ka waiwai IC50 o 22 nM. Ua lawa ka lapaʻau ʻana me UNC2281 i mea e ālai ai i ka hoʻoulu ʻia ʻana o ka EGF-mediated stimulation o kahi mea hoʻokipa chimeric i loaʻa i ka pūnaewele intracellular o Mer i hoʻohui ʻia i ka domain extracellular o EGFR. Eia kekahi, hiki i ka UNC2881 ke ho'ōki i ka hoʻohui ʻana o ka platelet collagen-induced, me ka manaʻo e loaʻa paha i kēia papa o nā mea hoʻopale no ka pale ʻana a me ka mālama ʻana i ka thrombosis pathologic. |
| CPD100733 | UNC2250 | ʻO UNC2250 kahi mea hoʻopaneʻe Mer Kinase ikaika a koho. Ke hoʻohanaʻia i nā pūnaewele ola, ua kāohiʻo UNC2250 i ka phosphorylation steady-state o ka endogenous Mer me kahi IC50 o 9.8 nM a ua kāohi i ka ligand-hoʻoulu i ka hoʻouluʻana o kahi protein chimeric EGFR-Mer. ʻO ka mālama ʻana me UNC2250 ka hopena i ka emi ʻana o ka hiki ke hoʻokumu ʻia i loko o ka rhabdoid a me ka NSCLC tumor cell, a laila e hōʻike ana i ka hana antitumor hana. Hāʻawi nā hopena i kumu no ka hoʻokolokolo hou ʻana o UNC2250 no ka noi therapeutic i nā maʻi me ka maʻi kanesa. |
| CPD100732 | LDC1267 | ʻO LDC1267 kahi mea hoʻopaneʻe TAM kinase ikaika a koho. Hōʻike ʻo LDC1267 i ka hana haʻahaʻa e kūʻē iā Met, Aurora B, Lck, Src, a me CDK8. ʻO LDC1267 ka hōʻemi nui ʻana i ka maʻi maʻi mammary murine a me nā metastases melanoma i hilinaʻi ʻia i nā cell NK. ʻO ka TAM tyrosine kinase receptors Tyro3, Axl a me Mer (ʻike ʻia ʻo Mertk) i ʻike ʻia he mau substrates ubiquitylation no Cbl-b. ʻO ka mālama ʻana i nā pūnaewele NK ʻano ʻāhiu me kahi mole liʻiliʻi liʻiliʻi hou ʻo TAM kinase inhibitor i hāʻawi ʻia i ka hiki ke lapaʻau, hoʻomaikaʻi maikaʻi i ka hana anti-metastatic NK cell in vivo. |
| CPD100731 | BMS-777607 | ʻO BMS-777607, i ʻike ʻia ʻo BMS-817378 a me ASLAN-002, he mea hoʻopaneʻe Met tyrosine kinase, he mea hoʻopale o MET tyrosine kinase me ka hana antineoplastic. Hoʻopili ʻo MET tyrosine kinase inhibitor BMS-777607 i ka c-Met protein, a i ʻole hepatocyte growth factor receptor (HGFR), e pale ana i ka hoʻopaʻa ʻana o ka hepatocyte growth factor (HGF) a hoʻopau i ke ala hōʻailona MET; hiki i kēia mea hana ke hoʻoulu i ka make cell i loko o nā pūnaʻi tumor e hōʻike ana i ka c-Met. ʻO c-Met, kahi mea hoʻokipa tyrosine kinase i hōʻike nui ʻia a i hoʻololi ʻia i nā ʻano cell tumor he nui, he hana koʻikoʻi i ka hoʻonui ʻana o ka cell tumor, ke ola, ka hoʻouka ʻana, a me ka metastasis, a me ka angiogenesis tumor. |
| CPD100730 | Cabozantinib | ʻO Cabozantinib, ka mea i ʻike ʻia ʻo XL-184 a i ʻole BMS-907351, he mea hiki ke loaʻa i ka waha, he mea hoʻopaneʻe liʻiliʻi liʻiliʻi ʻo tyrosine kinase (RTK) me ka hana antineoplastic. Hoʻopaʻa ikaika ʻo Cabozantinib i nā kinase receptor tyrosine. ʻO ka mea kikoʻī, ʻike ʻia ka cabozantinib i kahi pilina ikaika no ka hepatocyte growth factor receptor (Met) a me ka vascular endothelial growth factor receptor 2 (VEGFR2), hiki ke hopena i ka pale ʻana i ka ulu ʻana o ka tumo a me ka angiogenesis, a me ka regression tumor. Ua ʻae ʻia ʻo Cabozantinib e ka US FDA i Nowemapa 2012 no ka mālama ʻana i ka maʻi maʻi thyroid medullary. |
