| nwamba # | Aha ngwaahịa | Nkọwa |
| CPD100501 | UNC2541 | UNC2541 bụ onye nwere ike na ihe mgbochi MerTK akọwapụtara nke na-egosipụta ọrụ inhibitory sub-micromolar na ELISA dabere na cell. Na mgbakwunye, a na-ekpebi usoro X-ray nke protein MerTK dị mgbagwoju anya yana 11 iji gosi na macrocycles ndị a na-ejikọta na akpa MerTK ATP. UNC2541 gosiri IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| CPD100745 | RU-302 | RU-302 bụ pan-tam inhibitor akwụkwọ akụkọ, na-egbochi interface dị n'etiti tam ig1 ectodomain na gas6 lg ngalaba, na-egbochi ahịrị sel ndị nta akụkọ axl na ahịrị mkpụrụ ndụ kansa tam na-anabata ya. |
| CPD100744 | R916562 | |
| CPD100743 | Ningetinib-Tosylate | CT-053, nke a makwaara dị ka DE-120, bụ VEGF na PDGF inhibitor nwere ike maka ọgwụgwọ nke macular degeneration metụtara afọ mmiri. |
| CPD100742 | SGI-7079 | SGI-7079 bụ onye na-egbochi Axl dị ike ma họrọ nke nwere ọrụ mgbochi ọrịa kansa. SGI-7079 gbochiri ọrụ Axl nke ọma n'ihu Gas6 ligand exogenous. SGI-7079 gbochiri uto tumor na usoro dabere na dose. Axl bụ ebumnuche ọgwụgwọ nwere ike imeri nguzogide ihe mgbochi EGFR. |
| CPD100741 | 2-D08 | 2-D08 bụ flavone sịntetik nke na-egbochi sumoylation. 2-D08 gosipụtara mmetụta mgbochi mkpokọta na neuroprotective |
| CPD100740 | Dubermatinib | Dubermatinib, nke a makwaara dị ka TP-0903, bụ onye na-emechi AXL nwere ike na nhọrọ. TP-0903 na-ebute oke apoptosis na sel CLL B nwere ụkpụrụ LD50 nke oke nanomolar. Nchikota nke TP-0903 na BTK inhibitors na-abawanye CLL B-cell apoptosis AXL overexpression bụ isiokwu na-emegharị ugboro ugboro n'ọtụtụ ụdị tumo nke nwetara nguzogide dị iche iche. Ọgwụgwọ mkpụrụ ndụ kansa na TP-0903 na-atụgharị mesenchymal phenotype n'ọtụtụ ụdị ma mee ka mkpụrụ ndụ kansa nwee ike ịgwọ ya na ndị ọrụ ndị ọzọ ezubere iche. Nlekọta nke TP-0903 ma ọ bụ dịka otu onye ọrụ ma ọ bụ jikọtara ya na ndị na-egbochi BTK nwere ike ịdị irè n'ịgwọ ndị ọrịa nwere CLL. |
| CPD100739 | NPS-1034 | NPS-1034 bụ onye na-egbochi MET akwụkwọ akụkọ, nke na-egbochi nnabata MET na-arụ ọrụ yana mutant ya na-arụ ọrụ. NPS-1034, na-egbochi ụdị mutant dị iche iche nke MET yana HGF na-arụ ọrụ ụdị anụ ọhịa MET. NPS-1034 gbochiri mmụba nke mkpụrụ ndụ na-ekwupụta MET na-arụ ọrụ ma kwalite nlọghachi nke etuto ahụ sitere na mkpụrụ ndụ ndị dị otú ahụ na ụdị xenograft òké site na omume mgbochi angiogenic na pro-apoptotic. NPS-1034 gbochiri HGF-akpali akpali nke nrịbama MET na ọnụnọ ma ọ bụ enweghị serum. N'ụzọ doro anya, NPS-1034 gbochiri ụdị MET atọ nke na-eguzogide MET inhibitors SU11274, NVP-BVU972, na PHA665752. |
| CPD100738 | Glesatinib | Glesatinib, nke a makwaara dị ka MGCD-265, bụ ihe a na-ahụ maka ọnụ, obere molecule, multitargeted tyrosine kinase inhibitor nwere ọrụ antineoplastic. MGCD265 na-ejikọta ma na-egbochi phosphorylation nke ọtụtụ tyrosine kinases (RTKs), gụnyere c-Met receptor ( hepatocyte growth factor receptor); onye na-anabata Tek / Tie-2; vascular endothelial growth factor receptor (VEGFR) ụdị 1, 2, na 3; na macrophage-na-akpali akpali 1 receptor (MST1R ma ọ bụ RON). |
| CPD100737 | CEP-40783 | CEP-40783, nke a makwaara dị ka RXDX-106, bụ onye nwere ike, nhọrọ na onye na-emechi ọnụ nke AXL na c-Met nwere ụkpụrụ IC50 nke 7 nM na 12 nM, n'otu n'otu maka iji ya na ara, ngụgụ na-abụghị obere cell (NSCLC). , na ọrịa cancer pancreatic. |
| CPD1725 | Bemcentinib | BGB-324, nke a makwaara dị ka R428 ma ọ bụ Bemcentinib, bụ obere ihe na-egbochi molecule nke Axl kinase, nke gosipụtara ọrụ na-egbochi mgbasa nke tumo ma na-agbatị ndụ n'ụdị ọrịa cancer ara metastatic. Onye na-anabata tyrosine kinase Axl nwere ike ịrụ ọrụ dị mkpa na ọganihu ọrịa kansa, mbuso agha, metastasis, nguzogide ọgwụ na ọnwụ onye ọrịa. R428 na-egbochi Axl na obere ọrụ nanomolar ma gbochie ihe omume Axl dabere, gụnyere Akt phosphorylation, mbuso agha ọrịa ara ara, na mmepụta cytokine proinflammatory. |
| CPD3545 | Gilteritinib | Gilteritinib, nke a makwaara dị ka ASP2215, bụ FLT3 / AXL inhibitor, nke gosipụtara ọrụ antileukemic dị ike megide AML ma ọ bụ ma FLT3-ITD na FLT3-D835 mutations. Na invitro, n'ime 78 tyrosine kinases nwalere, ASP2215 gbochiri FLT3, LTK, ALK, na AXL kinases site na 50% na 1 nM nwere uru IC50 nke 0.29 nM maka FLT3, ihe dịka 800-npịaji karịa nke c-KIT, Mgbochi nke jikọtara ya na ihe ize ndụ nke myelosuppression nwere ike ime. ASP2215 gbochiri uto nke mkpụrụ ndụ MV4-11, nke na-ebu FLT3-ITD, yana uru IC50 nke 0.92 nM, tinyere mgbochi nke pFLT3, pAKT, pSTAT5, PERK, na pS6. ASP2215 belatara ibu akpụ na ụmị ọkpụkpụ wee gbatịa ndụ ụmụ oke na mkpụrụ ndụ MV4-11 etinyere n'ime intravenously. ASP2215 nwere ike iji ya mee ihe n'ịgwọ AML. |
| CPD100734 | UNC2881 | UNC2881 bụ ihe mgbochi Mer kinase siri ike. UNC2281 na-egbochi steeti Mer kinase phosphorylation kwụ ọtọ yana uru IC50 nke 22 nM. Ọgwụgwọ na UNC2281 ezuola igbochi mkpali mgbasa ozi EGF nke onye nnata chimeric nwere ngalaba intracellular nke Mer jikọtara na ngalaba extracellular nke EGFR. Na mgbakwunye, UNC2881 na-egbochi mkpokọta platelet na-akpata collagen, na-atụ aro na klaasị nke inhibitors nwere ike ịba uru maka mgbochi na/ma ọ bụ ọgwụgwọ thrombosis pathologic. |
| CPD100733 | UNC2250 | UNC2250 bụ ihe mgbochi Mer Kinase nwere ike na nhọrọ. Mgbe etinyere ya na mkpụrụ ndụ dị ndụ, UNC2250 gbochiri phosphorylation steeti endogenous Mer na IC50 nke 9.8 nM ma gbochiri ligand-akpali akpali nke protein chimeric EGFR-Mer. Ọgwụgwọ na UNC2250 mekwara ka mbelata ikike imepụta colony na rhabdoid na mkpụrụ ndụ tumor NSCLC, si otú a na-egosipụta ọrụ antitumor na-arụ ọrụ. Nsonaazụ a na-enye echiche maka nyocha ọzọ nke UNC2250 maka ngwa ọgwụgwọ na ndị ọrịa nwere ọrịa kansa. |
| CPD100732 | LDC1267 | LDC1267 bụ ihe mgbochi TAM kinase dị ike ma họrọ. LDC1267 na-egosiputa mmemme dị ala megide Met, Aurora B, Lck, Src, na CDK8. LDC1267 belatara ọrịa kansa mammary murine na melanoma metastases dabere na sel NK. Achọpụtara ndị na-anabata TAM tyrosine kinase Tyro3, Axl na Mer (nke a makwaara dị ka Mertk) dị ka ihe eji eme ihe maka Cbl-b. Ọgwụgwọ ụdị mkpụrụ ndụ NK anụ ọhịa nwere obere ihe mgbochi TAM kinase emepụtara ọhụrụ nyere ikike ọgwụgwọ, na-akwalite ọrụ mgbochi metastatic NK cell na vivo. |
| CPD100731 | BMS-777607 | BMS-777607, nke a makwaara dị ka BMS-817378 na ASLAN-002, Met tyrosine kinase inhibitor, bụ onye na-egbochi MET tyrosine kinase nwere ọrụ antineoplastic. MET tyrosine kinase inhibitor BMS-777607 na-ejikọta na protein c-Met, ma ọ bụ onye na-anabata ihe na-eto eto hepatocyte (HGFR), na-egbochi njide nke ihe na-eto eto hepatocyte (HGF) na imebi ụzọ akara MET; onye ọrụ a nwere ike ịkpata ọnwụ cell na mkpụrụ ndụ tumo na-ekwupụta c-Met. c-Met, onye na-anabata tyrosine kinase nke ukwuu ma ọ bụ gbanwee n'ọtụtụ ụdị cell tumor, na-arụ ọrụ dị mkpa na mmụba cell tumor, nlanarị, mbuso agha, na metastasis, yana na angiogenesis tumor. |
| CPD100730 | Cabozantinib | Cabozantinib, nke a makwaara dị ka XL-184 ma ọ bụ BMS-907351, bụ ihe a na-ahụ maka ọnụ, obere ihe na-anabata tyrosine kinase (RTK) nke nwere ọrụ antineoplastic. Cabozantinib na-ejikọ ike ma na-egbochi ọtụtụ kinase nnabata tyrosine. Kpọmkwem, cabozantinib na-egosi na ọ nwere njikọ siri ike maka onye na-anabata ihe na-emepụta hepatocyte (Met) na vaskụla endothelial growth factor receptor 2 (VEGFR2), nke nwere ike ime ka nkwụsị nke tumor na angiogenesis, na regression tumor. Cabozantinib kwadoro site na US FDA na November 2012 maka ọgwụgwọ nke medullary thyroid cancer. |
