| CAT # | Khoom npe | Kev piav qhia |
| PIB 100501 | UNC2541 | UNC2541 yog ib qho muaj zog thiab MerTK tshwj xeeb inhibitor uas nthuav tawm cov kev ua haujlwm ntawm cov micromolar inhibitory hauv cell-based ELISA. Tsis tas li ntawd, X-ray qauv ntawm MerTK protein nyob rau hauv complex nrog 11 tau txiav txim siab los qhia tias cov macrocycles khi hauv MerTK ATP hnab ris. UNC2541 qhia IC50 MerTH = 4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| PIB 100745 | UA-302 | RU-302 yog ib qho tshiab pan-tam inhibitor, thaiv qhov sib cuam tshuam ntawm tam ig1 ectodomain thiab gas6 lg domain, muaj zog inhibiting axl reporter cell kab thiab haiv neeg tam receptors kab mob qog noj ntshav. |
| PIB 100744 | r91656 2 | |
| PIB 100743 | Ningetinib-Tosylate | CT-053, tseem hu ua DE-120, yog VEGF thiab PDGF inhibitor muaj peev xwm los kho cov hnub nyoog ntub dej ntsig txog macular degeneration. |
| PIB 100742 | TSI-7079 | SGI-7079 yog ib qho muaj zog thiab xaiv Axl inhibitor uas muaj peev xwm tiv thaiv qog noj ntshav. SGI-7079 zoo inhibited Axl activation nyob rau hauv lub xub ntiag ntawm exogenous Gas6 ligand. SGI-7079 inhibited qog loj hlob nyob rau hauv ib koob tshuaj raws li. Axl yog lub hom phiaj kho mob rau kev kov yeej EGFR inhibitor tsis kam. |
| PIB 100741 | 2-D 08 | 2-D08 yog ib qho hluavtaws flavone uas inhibits suoylation. 2-D08 tau pom tias muaj cov nyhuv anti-aggregatory thiab neuroprotective |
| PIB 100740 | Dubermatinib | Dubermatinib, tseem hu ua TP-0903, yog lub zog thiab xaiv AXL inhibitor. TP-0903 induces loj apoptosis hauv CLL B hlwb nrog LD50 qhov tseem ceeb ntawm nanomolar ranges. Kev sib xyaw ntawm TP-0903 nrog BTK inhibitors augments CLL B-cell apoptosis AXL overexpression yog lub ntsiab lus rov tshwm sim pom nyob rau hauv ntau hom qog uas tau txais kev tiv thaiv rau ntau tus neeg ua haujlwm. Kev kho mob qog noj ntshav nrog TP-0903 thim rov qab cov tshuaj mesenchymal phenotype hauv ntau cov qauv thiab ua rau mob qog noj ntshav rau kev kho mob nrog rau lwm cov tshuaj tiv thaiv. Kev tswj hwm ntawm TP-0903 yog ib tus neeg sawv cev lossis ua ke nrog BTK inhibitors tuaj yeem ua tau zoo hauv kev kho cov neeg mob nrog CLL. |
| PAB 100739 | NPE-1034 | NPS-1034 yog ib qho tshiab MET inhibitor, uas inhibits MET receptor activated thiab nws constitutively active mutants. NPS-1034, inhibits ntau yam kev hloov pauv hloov pauv ntawm MET nrog rau HGF-activated wild-type MET. NPS-1034 inhibited qhov kev loj hlob ntawm cov hlwb uas nthuav tawm MET thiab txhawb kev rov ua haujlwm ntawm cov qog tsim los ntawm cov hlwb hauv cov qauv nas xenograft los ntawm kev ua haujlwm anti-angiogenic thiab pro-apoptotic. NPS-1034 kuj inhibited HGF-stimulated activation ntawm MET signaling nyob rau hauv lub xub ntiag los yog tsis muaj ntshav. Qhov tseem ceeb, NPS-1034 inhibited peb MET variants uas tiv taus MET inhibitors SU11274, NVP-BVU972, thiab PHA665752. |
| PAB 100738 | Glesatinib | Glesatinib, tseem hu ua MGCD-265, yog ib qho kev hais lus bioavailable, me me-molecule, multitargeted tyrosine kinase inhibitor uas muaj peev xwm ua haujlwm antineoplastic. MGCD265 khi rau thiab inhibits phosphorylation ntawm ob peb receptor tyrosine kinases (RTKs), nrog rau cov c-Met receptor (hepatocyte loj hlob receptor receptor); Tek/Tie-2 receptor; vascular endothelial growth factor receptor (VEGFR) hom 1, 2, thiab 3; thiab macrophage-stimulating 1 receptor (MST1R lossis RON). |
| PAB 100737 | PEB-40783 | CEP-40783, tseem hu ua RXDX-106, yog ib qho muaj zog, xaiv thiab hais lus muaj inhibitor ntawm AXL thiab c-Met nrog IC50 qhov tseem ceeb ntawm 7 nM thiab 12 nM, raws li kev siv hauv lub mis, tsis yog lub ntsws me me (NSCLC) , thiab mob qog noj ntshav pancreatic. |
| PEB 1725 | Bemcentinib | BGB-324, tseem hu ua R428 los yog Bemcentinib, yog ib qho kev xaiv me me molecule inhibitor ntawm Axl kinase, uas qhia txog kev ua haujlwm los thaiv cov qog nqaij hlav thiab ua kom muaj sia nyob ntev hauv cov qauv ntawm cov qog nqaij hlav cancer mis. Lub receptor tyrosine kinase Axl tuaj yeem ua lub luag haujlwm tseem ceeb hauv kev mob qog noj ntshav, ntxeem tau, metastasis, tshuaj tiv thaiv, thiab cov neeg mob tuag. R428 inhibits Axl nrog kev ua haujlwm tsawg nanomolar thiab thaiv cov xwm txheej ntawm Axl-dependent, suav nrog Akt phosphorylation, mob qog noj ntshav ntawm lub mis, thiab kev tsim cov cytokine proinflammatory. |
| PIB 3545 | Gilteritinib | Gilteritinib, tseem hu ua ASP2215, yog ib qho muaj zog FLT3 / AXL inhibitor, uas pom muaj zog tiv thaiv kab mob tiv thaiv AML nrog ob lossis ob qho tib si FLT3-ITD thiab FLT3-D835 kev hloov pauv. Hauv invitro, ntawm 78 tyrosine kinases kuaj, ASP2215 inhibited FLT3, LTK, ALK, thiab AXL kinases los ntawm ntau dua 50% ntawm 1 nM nrog IC50 tus nqi ntawm 0.29 nM rau FLT3, kwv yees li 800-fold muaj zog dua li c-KIT, qhov inhibition ntawm uas yog txuas mus rau ib qho kev pheej hmoo ntawm myelosuppression. ASP2215 inhibited kev loj hlob ntawm MV4-11 hlwb, uas harbor FLT3-ITD, nrog IC50 tus nqi ntawm 0.92 nM, nrog rau inhibition ntawm pFLT3, pAKT, pSTAT5, pERK, thiab pS6. ASP2215 txo cov qog nqaij hlav hauv cov pob txha pob txha thiab ua rau cov nas muaj sia nyob ntev dua nrog cov tshuaj MV4-11. ASP2215 tuaj yeem siv tau los kho AML. |
| PIB 100734 | UNC2881 | UNC2881 yog tus muaj zog Mer kinase inhibitor. UNC2281 inhibits khov kho-xeev Mer kinase phosphorylation nrog IC50 tus nqi ntawm 22 nM. Kev kho mob nrog UNC2281 kuj tseem txaus los thaiv EGF-mediated stimulation ntawm chimeric receptor uas muaj cov intracellular domain ntawm Mer fused mus rau extracellular domain ntawm EGFR. Tsis tas li ntawd, UNC2881 muaj zog inhibits collagen-induced platelet aggregation, qhia tias cov chav kawm ntawm inhibitors no yuav muaj txiaj ntsig rau kev tiv thaiv thiab / lossis kev kho mob ntawm cov kab mob thrombosis. |
| PIB 100733 | UNC 2250 | UNC2250 yog lub zog thiab xaiv Mer Kinase inhibitor. Thaum ua ntawv thov rau cov hlwb nyob, UNC2250 inhibited khov kho-state phosphorylation ntawm endogenous Mer nrog IC50 ntawm 9.8 nM thiab thaiv ligand-stimulated activation ntawm chimeric EGFR-Mer protein. Kev kho mob nrog UNC2250 kuj tau ua rau txo qis hauv colony-forming peev xwm hauv rhabdoid thiab NSCLC qog hlwb, yog li ua kom pom cov haujlwm ua haujlwm antitumor. Cov txiaj ntsig tau muab qhov laj thawj rau kev tshawb nrhiav ntxiv ntawm UNC2250 rau kev siv tshuaj kho mob rau cov neeg mob qog noj ntshav. |
| PIB 100732 | TSI 1267 | LDC1267 yog ib qho muaj zog thiab xaiv TAM kinase inhibitor. LDC1267 qhia cov haujlwm qis dua rau Met, Aurora B, Lck, Src, thiab CDK8. LDC1267 txo qis murine mammary cancer thiab melanoma metastases nyob ntawm NK hlwb. Lub TAM tyrosine kinase receptors Tyro3, Axl thiab Mer (tseem hu ua Mertk) tau txheeb xyuas raws li ubiquitylation substrates rau Cbl-b. Kev kho mob ntawm cov tsiaj qus NK hlwb nrog ib qho tshiab tsim me me molecule TAM kinase inhibitor tau muab kev kho mob muaj peev xwm, ua kom muaj txiaj ntsig zoo los tiv thaiv metastatic NK cell ua haujlwm hauv vivo. |
| PIB 100731 | BMS-777607 Kev | BMS-777607, tseem hu ua BMS-817378 thiab ASLAN-002, Met tyrosine kinase inhibitor, yog ib qho inhibitor ntawm MET tyrosine kinase uas muaj peev xwm ua haujlwm antineoplastic. MET tyrosine kinase inhibitor BMS-777607 khi rau c-Met protein, lossis hepatocyte growth factor receptor (HGFR), tiv thaiv kev khi ntawm hepatocyte growth factor (HGF) thiab cuam tshuam rau MET signaling pathway; Tus neeg sawv cev no tuaj yeem ua rau cov cell tuag hauv cov qog hlwb uas qhia txog c-Met. c-Met, receptor tyrosine kinase overexpressed lossis hloov pauv hauv ntau hom qog cell, ua lub luag haujlwm tseem ceeb hauv qog cell proliferation, ciaj sia taus, ntxeem tau, thiab metastasis, thiab hauv cov qog angiogenesis. |
| PIB 100730 | Cabozantinib | Cabozantinib, tseem hu ua XL-184 los yog BMS-907351, yog qhov ncauj bioavailable, me me molecule receptor tyrosine kinase (RTK) inhibitor uas muaj peev xwm ua haujlwm antineoplastic. Cabozantinib khi rau thiab inhibits ntau tyrosine receptor kinases. Tshwj xeeb, cabozantinib zoo li muaj kev sib raug zoo rau cov kab mob hepatocyte loj hlob receptor (Met) thiab vascular endothelial kev loj hlob yam receptor 2 (VEGFR2), uas yuav ua rau inhibition ntawm qog loj hlob thiab angiogenesis, thiab qog regression. Cabozantinib tau pom zoo los ntawm US FDA nyob rau lub Kaum Ib Hlis 2012 rau kev kho mob ntawm medullary thyroid cancer. |
