| CAT # | Igama lemveliso | Inkcazo |
| CPD2809 | I-AMG-510 | I-AMG-510 yi-KRAS G12C i-covalent inhibitor enamandla. I-AMG-510 ijolise ngokukhethekileyo kwi-KRAS p.G12C eguqukileyo, nokuba yi-DNA, i-RNA okanye inqanaba leprotheyini, kwaye inqanda, ngendlela engekacaciswanga, ukubonakaliswa kunye/okanye ukubonakaliswa kweseli yethumba nge-KRAS p.G12C eguqukileyo. Oku kunokuthintela ukukhula kwi-KRAS p.G12C-ebonisa iiseli zethumba |
| CPD100230 | JBJ-04-125-02 R-isomer | |
| CPD102300 | S-55746 | |
| CPD101235 | i-diABZI STING agonist-1 trihydrochloride | I-diABZI STING i-agonist-1 (i-trihydrochloride) i-stimulator ekhethiweyo ye-interferon genes (STING) i-receptor agonist, kunye ne-EC50 ye-130, i-186 nM yomntu kunye nemouse, ngokulandelanayo. |
| CPD101234 | i-diABZI STING agonist-1 (Tautomerism) | I-diABZI STING i-agonist-1 I-Tautomerism (i-compound 3) i-stimulator ekhethiweyo ye-interferon genes (STING) i-receptor agonist, kunye ne-EC50s ye-130, i-186 nM yomntu kunye nemouse, ngokulandelanayo. |
| CPD101233 | i-diABZI STING agonist-1 | I-diABZI STING i-agonist-1 i-stimulator ekhethiweyo ye-interferon genes (STING) i-receptor agonist, kunye ne-EC50s ye-130, i-186 nM yomntu kunye nemouse, ngokulandelanayo. |
| CPD101232 | I-agonist ye-STING-4 | I-STING agonist-4 yi-stimulator ye-Interferon Genes (STING) i-receptor agonist ene-inhibitory constant ecacileyo (IC50) ye-20 nM. I-STING agonist-4 yi-symmetry enxulumene ne-amidobenzimidazole (ABZI)-enxulumene nekhompawundi esekwe ukwenza ii-ABZIs ezidityanisiweyo (diABZIs) kunye nokubophelela okuphuculweyo kwi-STING kunye nokusebenza kweselula. |
| CPD101231 | I-agonist ye-STING-3 | I-STING agonist-3, ekhutshwe kwi-patent WO2017175147A1 (umzekelo we-10), i-molecule ekhethiweyo kunye ne-non-nucleotide encinci ye-STING agonist kunye ne-peC50 kunye ne-pIC50 ye-7.5 kunye ne-9.5, ngokulandelanayo. I-STING agonist-3 inefuthe elihlala ixesha elide lokulwa ne-tumor kunye namandla amakhulu okuphucula unyango lomhlaza |
| CPD100904 | I-Voruciclib | I-Voruciclib, ekwabizwa ngokuba yi-P1446A-05, yiprotein kinase inhibitor ethe ngqo kwi-cyclin-dependent kinase 4 (CDK4) enomsebenzi we-antineoplastic. I-CDK4 inhibitor P1446A-05 inqanda ngokukodwa inguqu yesigaba se-CDK4-mediated G1-S, ukubamba i-cell cycling kunye nokuthintela ukukhula kweeseli zomhlaza. I-serine / threonine kinase CDK4 ifumaneka kwi-complex kunye ne-D-type G1 cyclins kwaye yi-kinase yokuqala ukuba isebenze ngokuvuselela i-mitogenic, ukukhulula iiseli ukusuka kwinqanaba elipholileyo ukuya kwinqanaba lokukhula kwebhayisikili ye-G1 / S; I-CDK-cyclin complexes iboniswe ukuba i-phosphorylate i-retinoblastoma (Rb) i-transcription factor in early G1, displaceing histone deacetylase (HDAC) kunye nokuthintela ukunyanzeliswa kwe-transcriptional. |
| CPD100905 | Alvocidib | I-Alvocidib yi-synthetic N-methylpiperidinyl chlorophenyl flavone compound. Njenge-inhibitor ye-cyclin-dependent kinase, i-alvocidib yenza ukuba kubanjwe umjikelezo weseli ngokuthintela i-phosphorylation ye-cyclin-dependent kinases (CDKs) kunye ne-down-regulating cyclin D1 kunye ne-D3 expression, okubangelwa ukubanjwa kwe-cell cycle ye-G1 kunye ne-apoptosis. Le arhente ikwayi-inhibitor ekhuphisanayo yomsebenzi we-adenosine triphosphate. Khangela izilingo zeklinikhi ezisebenzayo okanye izilingo zekliniki ezivaliweyo usebenzisa le arhente. |
| CPD100906 | BS-181 | I-BS-181 yi-CDK inhibitor ekhethiweyo kakhulu ye-CDK7 ene-IC (50) ye-21 nmol / L. Uvavanyo lwezinye ii-CDKs kunye nenye i-69 kinases ibonise ukuba i-BS-181 ivimbele i-CDK2 kuphela kwiindawo ezingaphantsi kwe-1 micromol / L, kunye ne-CDK2 ivinjelwe i-35-fold less potently (IC (50) 880 nmol / L) kune-CDK7. Kwiiseli ze-MCF-7, i-BS-181 inqande i-phosphorylation ye-CDK7 substrates, ikhuthaze ukubanjwa komjikelo weseli kunye ne-apoptosis ukuthintela ukukhula kwemigca yeseli yomhlaza, kwaye ibonise iziphumo ze-antitumor kwi-vivo. |
| CPD100907 | Rivicclib | I-Riviciclib, eyaziwa nangokuthi i-P276-00, i-flavone kunye ne-cyclin exhomekeke kwi-kinase (CDK) inhibitor enokuthi isebenze i-antineoplastic. I-P276-00 ibophelela ngokukhethekileyo kwaye inqanda i-Cdk4 / i-cyclin D1, i-Cdk1 / i-cyclin B kunye ne-Cdk9 / i-cyclin T1, i-serine / i-threonine kinases edlala indima ebalulekileyo ekulawuleni umjikelezo weseli kunye nokunyuka kwamaselula. Ukuvinjelwa kwezi kinases kukhokelela ekubanjweni komjikelo weeseli ngexesha lenguqu ye-G1/S, ngaloo ndlela ikhokelela ekungenweni kwe-apoptosis, kunye nokuthintela ukwanda kweeseli zethumba. |
| CPD100908 | MC180295 | I-MC180295 yi-CDK9 inhibitor ekhethiweyo kakhulu (IC50 = 5 nM). (I-MC180295 inomsebenzi obanzi wokuchasana nomhlaza kwi-vitro kwaye iyasebenza kwiimodeli zomhlaza we-vivo. Ukongeza, i-CDK9 inhibition ivakalisa i-immune checkpoint inhibitor α-PD-1 kwi-vivo, iyenza ibe yinjongo egqwesileyo yonyango lwe-epigenetic lomhlaza. |
| 1073485-20-7 | LDC000067 | I-LDC000067 yi-CDK9 inhibitor enamandla kwaye ekhethiweyo. I-LDC000067 inhibited in vitro transcription ngendlela ye-ATP-ekhuphisanayo kunye ne-dose-dependent. Ukuchazwa kweprofayili ye-Gene yeeseli eziphathwe nge-LDC000067 kubonise ukucuthwa okukhethiweyo kwee-mRNA ezihlala ixesha elifutshane, kubandakanywa nabalawuli ababalulekileyo bokwanda kunye ne-apoptosis. Uhlalutyo lwe-de novo RNA synthesis lucebise indima ebanzi eyahlukahlukeneyo ye-CDK9. Kwinqanaba lemolekyuli kunye neselula, i-LDC000067 iphinde yavelisa iziphumo ze-CDK9 inhibition ezifana nokuphuculwa kokunqumamisa kwe-RNA polymerase II kwiigenes kwaye, okona kubaluleke kakhulu, ukufakwa kwe-apoptosis kwiiseli zomhlaza. I-LDC000067 inqanda i-P-TEFb exhomekeke kwi-vitro transcription. Yenza i-apoptosis kwi-vitro kunye ne-vivo ngokudibanisa ne-BI 894999. |
| CPD100910 | SEL120-34A | I-SEL120-34A yi-CDK8 inhibitor enamandla kwaye ekhethiweyo esebenzayo kwiiseli ze-AML ezinamazinga aphezulu e-serine phosphorylation ye-STAT1 kunye ne-STAT5 ye-transactivation domains. I-EL120-34A inqanda i-phosphorylation ye-STAT1 S727 kunye ne-STAT5 S726 kwiiseli zomhlaza kwi-vitro. Ngokuqhubekayo, ukulawulwa kwe-STATs- kunye ne-NUP98-HOXA9- exhomekeke kwi-transcript ibonwe njengendlela ebalaseleyo yesenzo kwi-vivo. |
| CPD100501 | UNC2541 | I-UNC2541 inamandla kunye ne-MerTK-specific inhibitor ebonisa umsebenzi we-sub-micromolar inhibitory kwi-cell-based ELISA. Ukongezelela, isakhiwo se-X-ray seprotheni ye-MerTK kwi-complex kunye ne-11 yasombululwa ukubonisa ukuba ezi macrocycles zibophe kwi-pocket ye-MerTK ATP. I-UNC2541 ibonise i-IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| CPD100745 | RU-302 | I-RU-302 iyinoveli ye-pan-tam inhibitor, ivalela ujongano phakathi kwe-tam ig1 ectodomain kunye ne-gas6 lg domain, inqanda ngokunamandla imigca yeeseli ze-axl kunye nemigca yeeseli zomhlaza ze-tam receptors. |
| CPD100744 | R916562 | |
| CPD100743 | I-Ningetinib-Tosylate | I-CT-053, ekwabizwa ngokuba yi-DE-120, yi-VEGF kunye ne-PDGF inhibitor enokubakho kunyango lwe-macular degeneration emanzi enxulumene nobudala. |
| CPD100742 | SGI-7079 | I-SGI-7079 yinto enamandla kunye ne-Axl inhibitor ekhethiweyo kunye nomsebenzi onokuthi ube ne-anticancer. I-SGI-7079 ithintele ngokufanelekileyo ukusebenza kwe-Axl phambi kobukho be-Gas6 ligand yangaphandle. I-SGI-7079 ithintele ukukhula kwethumba ngendlela exhomekeke kwithamo. I-Axl yinto ekujoliswe kuyo yonyango enokuthi iphumelele ukuxhatshazwa kwe-EGFR inhibitor. |
| CPD100741 | 2-D08 | I-2-D08 yi-flavone yokwenziwa evimbela ukuxutywa kwe-sumoylation. I-2-D08 ibonise i-anti-aggregatory kunye ne-neuroprotective effect |
| CPD100740 | I-Dubermatinib | I-Dubermatinib, eyaziwa ngokuba yi-TP-0903, inamandla kwaye i-AXL inhibitor ekhethiweyo. I-TP-0903 yenza i-apoptosis enkulu kwiiseli ze-CLL B ezinexabiso le-LD50 le-nanomolar ranges. Ukudityaniswa kwe-TP-0903 kunye ne-BTK inhibitors augments CLL B-cell apoptosis AXL overexpression ngumxholo oqhubekayo obonwa kwiintlobo ezininzi zamathumba eziye zafumana ukuxhathisa kwii-arhente ezahlukeneyo. Unyango lweeseli zomhlaza nge-TP-0903 ibuyisela umva i-mesenchymal phenotype kwiimodeli ezininzi kwaye ivuselele iiseli zomhlaza kunyango kunye nezinye iiarhente ezichongiweyo. Ulawulo lwe-TP-0903 mhlawumbi njenge-arhente enye okanye ngokudibanisa ne-BTK inhibitors inokusebenza ekunyangeni izigulane ezine-CLL. |
| CPD100739 | NPS-1034 | I-NPS-1034 iyinoveli ye-MET inhibitor, evimbela i-MET receptor esebenzayo kunye ne-constitutively active mutants. I-NPS-1034, inqanda iindlela ezahlukeneyo eziguqukayo ezisebenzayo ze-MET kunye ne-HGF-activated wild-type MET. I-NPS-1034 ithintele ukwanda kweeseli ezibonisa i-MET esebenzayo kwaye yakhuthaza ukuhlehla kwamathumba akhiwe kwiiseli ezinjalo kwimodeli ye-mouse xenograft ngokusebenzisa izenzo ezichasene ne-angiogenic kunye ne-pro-apoptotic. I-NPS-1034 iphinde ivimbele ukusetyenziswa kwe-HGF-ivuselelwe ukubonakaliswa kwe-MET kubukho okanye ukungabikho kwe-serum. Ngokucacileyo, i-NPS-1034 inqanda iintlobo ezintathu ze-MET ezichasene ne-MET inhibitors SU11274, NVP-BVU972, kunye ne-PHA665752. |
| CPD100738 | Glesatinib | I-Glesatinib, eyaziwa ngokuba yi-MGCD-265, i-bioavailable yomlomo, i-molecule encinci, i-multitargeted tyrosine kinase inhibitor enokuthi isebenze i-antineoplastic. I-MGCD265 ibophelela kwaye inqanda i-phosphorylation ye-receptor tyrosine kinases (RTKs) ezininzi, kuquka i-c-Met receptor (i-hepatocyte ukukhula factor receptor); i-Tek/Tie-2 receptor; i-vascular endothelial growth factor receptor (VEGFR) iindidi ze-1, i-2, kunye ne-3; kunye ne-macrophage-stimulating 1 receptor (MST1R okanye RON). |
