| IKATI # | Igama Lomkhiqizo | Incazelo |
| I-CPD2809 | I-AMG-510 | I-AMG-510 iyisivimbeli esinamandla se-KRAS G12C. I-AMG-510 iqondise ngokukhetha inguquko ye-KRAS p.G12C, ezingeni le-DNA, i-RNA noma iphrotheni, futhi ivimbela, ngendlela engakacaciswanga, ukubonakaliswa kanye/noma noma ukusayina kweseli lesimila nge-KRAS p.G12C mutant. Lokhu kungase kuvimbele ukukhula kumaseli e-KRAS p.G12C-eveza isimila |
| I-CPD100230 | JBJ-04-125-02 R-isomer | |
| I-CPD102300 | S-55746 | |
| I-CPD101235 | I-diABZI STING agonist-1 trihydrochloride | I-diABZI STING agonist-1 (trihydrochloride) iyisikhuthazi esikhethiwe sezakhi zofuzo ze-interferon (STING) receptor agonist, nama-EC50s angu-130, 186 nM womuntu negundane, ngokulandelana. |
| I-CPD101234 | I-diABZI STING agonist-1 (Tautomerism) | I-diABZI STING agonist-1 Tautomerism (inhlanganisela 3) iyisikhuthazi esikhethiwe sezakhi zofuzo ze-interferon (STING) receptor agonist, nama-EC50s angu-130, 186 nM womuntu negundane, ngokulandelana. |
| I-CPD101233 | i-diABZI STING agonist-1 | I-diABZI STING agonist-1 iyisikhuthazi esikhethiwe sezakhi zofuzo ze-interferon (STING) receptor agonist, nama-EC50s angu-130, 186 nM womuntu negundane, ngokulandelana. |
| I-CPD101232 | I-STING agonist-4 | I-STING agonist-4 iyisikhuthazi se-Interferon Genes (STING) receptor agonist ene-apparent inhibitory constant (IC50) yama-20 nM. I-STING agonist-4 iyinhlanganisela esekelwe ku-symmetry ehlobene ne-amidobenzimidazole (ABZI) ukuze idale ama-ABZI axhunyiwe (diABZIs) abophezelekile ku-STING kanye nomsebenzi weselula. |
| I-CPD101231 | I-STING agonist-3 | I-STING agonist-3, ekhishwe ku-patent WO2017175147A1 (isibonelo 10), iyi-agonist ekhethiwe futhi engeyona i-nucleotide ye-molecule encane ye-STING ene-pEC50 ne-pIC50 ye-7.5 kanye ne-9.5, ngokulandelanayo. I-STING agonist-3 inomphumela oqinile wokulwa nesimila namandla amakhulu okuthuthukisa ukwelashwa komdlavuza |
| I-CPD100904 | I-Voruciclib | I-Voruciclib, eyaziwa nangokuthi i-P1446A-05, iyi-protein kinase inhibitor eqondene ngqo ne-cyclin-dependent kinase 4 (CDK4) enekhono lomsebenzi we-antineoplastic. I-CDK4 inhibitor P1446A-05 ivimbela ngokuqondile ukuguqulwa kwesigaba se-CDK4-mediated G1-S, ukubopha ukujikeleza kwamaseli kanye nokuvimbela ukukhula kwamangqamuzana omdlavuza. I-serine/threonine kinase CDK4 itholakala kunkimbinkimbi enamabhayisikili ohlobo lwe-D-G1 futhi iyi-kinase yokuqala ukwenziwa isebenze phezu kokukhuthazwa kwe-mitogenic, ikhipha amaseli ukusuka esigabeni esithule ukuya esigabeni sokukhula samabhayisikili se-G1/S; Ama-CDK-cyclin complexes aboniswe njenge-phosphorylate the retinoblastoma (Rb) transcription factor ekuqaleni kwe-G1, asusa i-histone deacetylase (HDAC) futhi avimbe ukucindezelwa kokubhaliwe. |
| I-CPD100905 | I-Alvocidib | I-Alvocidib iyinhlanganisela ye-N-methylpiperidinyl chlorophenyl flavone yokwenziwa. Njenge-inhibitor ye-cyclin-dependent kinase, i-alvocidib inxusa ukuboshwa komjikelezo weseli ngokuvimbela i-phosphorylation ye-cyclin-dependent kinases (CDKs) kanye nenkulumo elawula phansi ye-cyclin D1 kanye ne-D3, okuholela ekuboshweni komjikelezo weseli ye-G1 kanye ne-apoptosis. Le ejenti iphinde ibe inhibitor yokuncintisana yomsebenzi we-adenosine triphosphate. Hlola izivivinyo zomtholampilo ezisebenzayo noma izivivinyo zomtholampilo ezivaliwe usebenzisa lesi sisebenzeli. |
| I-CPD100906 | BS-181 | I-BS-181 iyi-CDK inhibitor ekhetha kakhulu ye-CDK7 ene-IC(50) engu-21 nmol/L. Ukuhlolwa kwamanye ama-CDK kanye namanye ama-kinase angu-69 kubonise ukuthi i-BS-181 ivimbele i-CDK2 kuphela ekugxilweni okungaphansi kuka-1 micromol/L, i-CDK2 ivinjwe ngokuphindwe izikhathi ezingu-35 ngokunamandla (IC(50) 880 nmol/L) kune-CDK7. Kumaseli e-MCF-7, i-BS-181 ivimbele i-phosphorylation yama-CDK7 substrates, yakhuthaza ukuboshwa komjikelezo wamaseli kanye ne-apoptosis ukuvimbela ukukhula kwemigqa yamangqamuzana omdlavuza, futhi yabonisa imiphumela ye-antitumor ku-vivo. |
| I-CPD100907 | I-Rivicclib | I-Riviciclib, eyaziwa nangokuthi i-P276-00, iyi-flavone ne-cyclin encike kinase (CDK) inhibitor enomsebenzi ongaba khona we-antineoplastic. I-P276-00 ibopha ngokukhetha futhi ivimbele i-Cdk4/cyclin D1, i-Cdk1/cyclin B ne-Cdk9/cyclin T1, i-serine/threonine kinases edlala izindima ezibalulekile ekulawuleni umjikelezo weseli nokwanda kwamaselula. Ukuvinjelwa kwalawa ma-kinase kuholela ekuboshweni komjikelezo weseli ngesikhathi soguquko lwe-G1/S, ngaleyo ndlela kuholele ekungenweni kwe-apoptosis, kanye nokuvinjwa kokwanda kwamaseli wesimila. |
| I-CPD100908 | I-MC180295 | I-MC180295 iyi-CDK9 inhibitor ekhetha kakhulu (IC50 = 5 nM). (I-MC180295 inomsebenzi obanzi wokulwa nomdlavuza ku-vitro futhi iyasebenza kumamodeli womdlavuza we-vivo. Ukwengeza, i-CDK9 inhibition izwela i-immune checkpoint inhibitor α-PD-1 ku-vivo, ikwenze kube okuhlosiwe okuhle kakhulu kwe-epigenetic therapy yomdlavuza. |
| 1073485-20-7 | LDC000067 | I-LDC000067 iyi-CDK9 inhibitor enamandla futhi ekhethayo. I-LDC000067 ivinjwe ukulotshwa kwe-in vitro ngendlela yokuncintisana ne-ATP futhi encike kumthamo. Ukuchazwa kwephrofayili ye-Gene yamaseli aphathwe nge-LDC000067 kubonise ukuncishiswa okukhethiwe kwama-mRNA ahlala isikhathi esifushane, okuhlanganisa nabalawuli ababalulekile bokwanda kanye ne-apoptosis. Ukuhlaziywa kwe-de novo RNA synthesis kuphakamise indima enhle ehlukahlukene ye-CDK9. Ezingeni lamangqamuzana namaselula, i-LDC000067 iphinde yakhiqiza imiphumela yesici sokuvinjwa kwe-CDK9 njengokumisa isikhashana okuthuthukisiwe kwe-RNA polymerase II ezakhini zofuzo futhi, okubaluleke kakhulu, ukufakwa kwe-apoptosis kumaseli omdlavuza. I-LDC000067 ivimbela ukuloba kwe-in vitro okuncike ku-P-TEFb. Idala i-apoptosis ku-vitro kanye ne-vivo ihlanganiswe ne-BI 894999. |
| I-CPD100910 | I-SEL120-34A | I-SEL120-34A iyi-CDK8 inhibitor enamandla futhi ekhethayo esebenza kumaseli e-AML anamazinga aphezulu e-serine phosphorylation ye-STAT1 kanye ne-STAT5 transactivation domain. I-EL120-34A ivimbela i-phosphorylation ye-STAT1 S727 ne-STAT5 S726 kumaseli omdlavuza ku-vitro. Ngokuqhubekayo, ukulawulwa kwe-STATs- kanye nokuloba okuncike ku-NUP98-HOXA9- kuye kwaqashelwa njengendlela ehamba phambili yokusebenza ku-vivo. |
| I-CPD100501 | UNC2541 | I-UNC2541 iyisivimbeli esinamandla futhi esiqondene ne-MerTK esibonisa umsebenzi we-sub-micromolar inhibitory ku-ELISA esekelwe kuseli. Ukwengeza, isakhiwo se-X-ray seprotheni ye-MerTK eyinkimbinkimbi ene-11 yaxazululwa ukuze kuboniswe ukuthi lawa ma-macrocycle abophezela ephaketheni le-MerTK ATP. I-UNC2541 ibonise i-IC50 MerTH=4.4 nM; I-IC50 AXL = 120 nM; I-IC50 TYRO3 = 220 nM; I-IC50 FLT3 = 320 nM. |
| I-CPD100745 | I-RU-302 | I-RU-302 iyinoveli ye-pan-tam inhibitor, evimba ukuxhumana phakathi kwe-tam ig1 ectodomain kanye nesizinda se-gas6 lg, evimbela ngokunamandla imigqa yamaseli e-axl yezintatheli kanye nemigqa yamaseli omdlavuza wama-tam receptors. |
| I-CPD100744 | R916562 | |
| I-CPD100743 | I-Ningetinib-Tosylate | I-CT-053, eyaziwa nangokuthi i-DE-120, iyi-VEGF kanye ne-PDGF inhibitor engase ibe ukwelashwa kokuwohloka kwe-macular okuhlobene neminyaka emanzi. |
| I-CPD100742 | I-SGI-7079 | I-SGI-7079 iyi-Axl inhibitor enamandla futhi ekhethayo enomsebenzi ongase ube khona wokulwa nomdlavuza. I-SGI-7079 ivimbe ngempumelelo ukusebenzisa i-Axl phambi kwe-Gas6 ligand yangaphandle. I-SGI-7079 ivimbele ukukhula kwesimila ngendlela encike kumthamo. I-Axl iyithagethi yokwelapha enamandla yokunqoba ukumelana ne-EGFR inhibitor. |
| I-CPD100741 | 2-D08 | I-2-D08 iyi-flavone yokwenziwa evimbela i-sumoylation. I-2-D08 ibonise umphumela we-anti-aggregatory kanye neuroprotective |
| I-CPD100740 | I-Dubermatinib | I-Dubermatinib, eyaziwa nangokuthi i-TP-0903, iyi-AXL inhibitor enamandla futhi ekhethayo. I-TP-0903 idala i-apoptosis enkulu kumaseli e-CLL B ngamavelu e-LD50 obubanzi be-nanomolar. Inhlanganisela ye-TP-0903 ne-BTK inhibitors augments CLL B-cell apoptosis AXL overexpression itimu eyenzeka kabusha ebonwa ezinhlotsheni eziningi zesimila esithole ukumelana nama-ejenti ahlukahlukene. Ukwelashwa kwamaseli omdlavuza nge-TP-0903 kubuyisela emuva i-mesenchymal phenotype kumamodeli amaningi futhi kuqwashise amangqamuzana omdlavuza ekwelapheni namanye ama-ejenti ahlosiwe. Ukuphathwa kwe-TP-0903 njenge-ejenti eyodwa noma kuhlanganiswe ne-BTK inhibitors kungase kusebenze ekwelapheni iziguli nge-CLL. |
| I-CPD100739 | I-NPS-1034 | I-NPS-1034 iyinoveli ye-MET inhibitor, evimbela i-MET receptor ecushiwe kanye nezinguquko zayo ezisebenzayo. I-NPS-1034, ivimbela izinhlobo ezihlukahlukene eziguqukayo ezisebenzayo ze-MET kanye ne-HGF-activated wild-type MET. I-NPS-1034 ivimbele ukwanda kwamaseli aveza i-MET ecushiwe futhi yakhuthaza ukuhlehla kwezimila ezakhiwe kusukela kumaseli anjalo kumodeli ye-mouse xenograft ngokusebenzisa izenzo zokulwa ne-angiogenic kanye ne-pro-apoptotic. I-NPS-1034 iphinde yavimbela ukusebenza okuvuselelwe kwe-HGF kokusayina kwe-MET lapho kukhona noma kungekho serum. Ngokuphawulekayo, i-NPS-1034 ivimbele okuhlukile kwe-MET okuthathu okumelana nama-MET inhibitors SU11274, NVP-BVU972, kanye ne-PHA665752. |
| I-CPD100738 | I-Glesatinib | I-Glesatinib, eyaziwa nangokuthi i-MGCD-265, i-oral bioavailable, i-molecule encane, i-multitargeted tyrosine kinase inhibitor enomsebenzi ongase ube khona we-antineoplastic. I-MGCD265 ibophezela futhi ivimbele i-phosphorylation ye-receptor tyrosine kinases (RTKs) eminingana, kuhlanganise ne-c-Met receptor (i-hepatocyte growth factor receptor); i-Tek/Tie-2 receptor; i-vascular endothelial growth factor receptor (VEGFR) izinhlobo ze-1, i-2, ne-3; kanye ne-macrophage-stimulating 1 receptor (MST1R noma RON). |
