| CAT # | Magaca Alaabta | Sharaxaada |
| CPD2809 | AMG-510 | AMG-510 waa ka hortag awood leh oo KRAS G12C. AMG-510 waxay si xushmad leh u bartilmaameedsanaysaa mutant-ga KRAS p.G12C, mid ka mid ah DNA, RNA ama heerka borotiinka, waxayna ka hortagtaa, iyada oo loo marayo hab aan weli la caddayn, muujinta iyo/ama unugyada burooyinka ee calaamadinta KRAS p.G12C mutant. Tani waxay joojin kartaa koritaanka KRAS p.G12C-muujinta unugyada burooyinka |
| CPD100230 | JBJ-04-125-02 R-isomer | |
| CPD102300 | S-55746 | |
| CPD101235 | diABZI STING agonist-1 trihydrochloride | diABZI STING agonist-1 (trihydrochloride) waa kiciyeyaasha xulashada ee hiddo-wadaha interferon (STING) agonist receptor agonist, oo leh EC50s ee 130, 186 nM dadka iyo jiirka, siday u kala horreeyaan. |
| CPD101234 | diABZI STING agonist-1 (Tautomerism) | diABZI STING agonist-1 Tautomerism (compound 3) waa kiciyeyaasha la xushay ee hiddo-wadaha interferon (STING) agonist receptor agonist, oo leh EC50s ee 130, 186 nM dadka iyo jiirka, siday u kala horreeyaan. |
| CPD101233 | diABZI STING agonist-1 | diABZI STING agonist-1 waa kiciyeyaasha xulashada ee hiddo-wadaha interferon (STING) agonist receptor agonist, oo leh EC50s ee 130, 186 nM dadka iyo jiirka, siday u kala horreeyaan. |
| CPD101232 | STING agonist-4 | STING agonist-4 waa kiciyeyaasha Interferon Genes (STING) agonist receptor agonist oo leh joogto ah inhibitory (IC50) ee 20 nM. STING agonist-4 waa laba asymmetry-xiriira amidobenzimidazole (ABZI) - xarun ku salaysan si loo abuuro ABZI (diABZI) oo ku xidhan STING iyo shaqada gacanta |
| CPD101231 | STING agonist-3 | STING agonist-3, oo laga soosaaray patent WO2017175147A1 (tusaale 10), waa xulashada iyo non-nucleotide yar-molecule STING agonist leh pEC50 iyo pIC50 ee 7.5 iyo 9.5, siday u kala horreeyaan. STING agonist-3 waxay leedahay saameyn joogto ah oo ka hortagga burooyinka iyo awood weyn oo lagu wanaajiyo daaweynta kansarka |
| CPD100904 | Voruciclib | Voruciclib, oo sidoo kale loo yaqaan P1446A-05, waa borotiinka kinase inhibitor gaar ah kinase 4 (CDK4) ku tiirsan cyclin oo leh firfircoonida antineoplastic. CDK4 inhibitor P1446A-05 waxay si gaar ah u joojisaa CDK4-dhexdhexaadinta G1-S marxaladda kala-guurka, xiritaanka baaskiilka unugyada iyo joojinta koritaanka unugyada kansarka. Serine / threonine kinase CDK4 waxaa laga helaa isku-dhafan oo leh nooca D-nooca G1 cyclins waana kinase-kii ugu horreeyay ee lagu dhaqo kicinta mitogenic, oo sii daaya unugyada marxaladda quiescent ee heerka wareegga wareegga G1 / S; Dhismayaasha CDK-cyclin ayaa la tusay inay fosphorylate fayriska retinoblastoma (Rb) horraantii G1, meesha ka saaraysa histone deacetylase (HDAC) iyo xannibaadda cadaadiska qoraalka. |
| CPD100905 | Alvocidib | Alvocidib waa isku-darka N-methylpiperidinyl chlorofenyl flavone-ka. Sida xannibaadaha kinase-ku-tiirsanaanta cyclin-ku-tiirsan, alvocidib wuxuu keenaa xiritaanka wareegga unugyada isagoo ka hortagaya fosforyaalka kinases-ku-tiirsanaanta cyclin (CDKs) iyo hoos-u-habaynta cyclin D1 iyo D3 muujinta, taasoo keentay in la xiro wareegga unugyada G1 iyo apoptosis. Wakiilkani sidoo kale waa horjooge tartan u ah waxqabadka adenosine triphosphate. Hubi tijaabooyin caafimaad oo firfircoon ama tijaabooyin caafimaad oo xidhan adoo isticmaalaya wakiilkan. |
| CPD100906 | BS-181 | BS-181 waa CDK inhibitor aad u dooratey CDK7 oo leh IC(50) ee 21 nmol/L. Tijaabada CDK-yada kale iyo sidoo kale 69 kinase oo kale ayaa muujisay in BS-181 kaliya ay joojisay CDK2 xajmiyada ka hooseeya 1 micromol/L, iyadoo CDK2 laga mamnuucay 35-laab in ka yar (IC(50) 880 nmol/L) marka loo eego CDK7. Unugyada MCF-7, BS-181 waxay joojiyeen fosforyaalka CDK7 substrates, kor u qaadista wareegga unugyada iyo apoptosis si loo xakameeyo koritaanka khadadka unugyada kansarka, waxayna muujisay saameynta antitumor ee vivo. |
| CPD100907 | Riviciclib | Riviciclib, oo sidoo kale loo yaqaan P276-00, waa flavone iyo kinase ku tiirsan cyclin (CDK) oo leh firfircoonida antineoplastic ee suurtagalka ah. P276-00 waxay si xushmad leh u xidhaa oo joojisaa Cdk4/cyclin D1, Cdk1/cyclin B iyo Cdk9/cyclin T1, serine/threonine kinases oo door muhiim ah ka ciyaara nidaaminta wareegga unugyada iyo kororka unugyada. Joojinta kinase-yadani waxay keenaysaa in la xiro wareegga unugyada inta lagu jiro kala-guurka G1/S, taas oo horseedaysa induction of apoptosis, iyo xakameynta kororka unugyada burooyinka. |
| CPD100908 | MC180295 | MC180295 waa xakameynta CDK9 aad u dooratay (IC50 = 5 nM). (MC180295 waxa uu leeyahay hawlo ballaadhan oo ka hortagga kansarka oo ku jira vitro waxana uu wax ku ool u yahay moodooyinka kansarka vivo. Intaa waxa dheer, xannibaadda CDK9 waxay dareensiisaa isbaarada difaaca ee α-PD-1 in vivo, taasoo ka dhigaysa bartilmaameed aad u fiican daaweynta epigenetic ee kansarka. |
| 1073485-20-7 | LDC000067 | LDC000067 waa horjooge awood leh oo door ah CDK9. LDC000067 waxay joojisay qoraalka faytrooga ee ATP-tartan iyo hab ku-tiirsanaan ah. Muujinta hidda-wadaha unugyada lagu daweeyay LDC000067 waxay muujisay hoos u dhigista xulashada mRNA-yada muddada gaaban, oo ay ku jiraan xeeriyeyaasha muhiimka ah ee faafinta iyo apoptosis. Falanqaynta isku-dhafka de novo RNA waxay soo jeedisay door wanaagsan oo ballaaran oo CDK9 ah. Marka la eego heerka molecular iyo unugga, LDC000067 waxay soo saartay saamaynta lagu garto xannibaadda CDK9 sida joojinta la xoojiyey ee RNA polymerase II ee hiddo-wadaha iyo, tan ugu muhiimsan, soo-gelinta apoptosis ee unugyada kansarka. LDC000067 waxay joojisaa qoraalka ku-tiirsanaanta P-TEFb. Waxay keentaa apoptosis in vitro iyo in vivo oo ay weheliso BI 894999. |
| CPD100910 | SEL120-34A | SEL120-34A waa xakameyn awood leh oo door ah CDK8 oo firfircoon oo ku jira unugyada AML oo leh heerar sare oo fosforyaalka serine ee STAT1 iyo STAT5 domains transactivation. EL120-34A waxay joojisaa fosforyaalka STAT1 S727 iyo STAT5 S726 ee unugyada kansarka ee vitro. Si joogto ah, sharciyeynta STATs- iyo NUP98-HOXA9-ku-tiirsanaanta qoraalka ayaa loo arkay inay tahay habka ugu muhiimsan ee ficilka gudaha vivo. |
| CPD100501 | UNC2541 | UNC2541 waa horjooge awood leh oo MerTK-gaar ah oo muujiya waxqabadyo ka-hortagga-yar-yar ee ELISA-ku-saleysan unugga. Intaa waxaa dheer, qaab-dhismeedka raajada ee borotiinka MerTK ee kakan oo leh 11 ayaa la xalliyey si loo muujiyo in makroskooladani ay ku xidhan yihiin jeebka MerTK ATP. UNC2541 waxay muujisay IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| CPD100745 | RU-302 | RU-302 waa sheeko cusub oo pan-tam inhibitor ah, oo xannibaysa is-dhexgalka u dhexeeya tam ig1 ectodomain iyo gaaska 6 lg domain, oo si xooggan u xannibaya khadadka unugyada axl ee saxafiyiinta iyo kuwa asaliga ah ee tam receptors khadadka unugyada kansarka |
| CPD100744 | R916562 | |
| CPD100743 | Ningetinib-Tosylate | CT-053, oo sidoo kale loo yaqaan DE-120, waa VEGF iyo PDGF inhibitor oo awood u leh daaweynta da'da qoyan ee hoos u dhaca maskaxda. |
| CPD100742 | SGI-7079 | SGI-7079 waa Axl inhibitor awood leh oo la xushay oo leh firfircoonida ka hortagga kansarka. SGI-7079 waxay si wax ku ool ah u joojisay firfircoonida Axl iyada oo ay jirto ligand Gas6 exogenous. SGI-7079 waxay joojisay korriinka burada ee qiyaasta qiyaasta. Axl waa bartilmaameed daweyn oo suurtagal ah si looga gudbo iska caabbinta EGFR. |
| CPD100741 | 2-D08 | 2-D08 waa flavone synthetic oo joojisa sumoylation. 2-D08 waxay muujisay saameyn lid ku ah isku-darka iyo neuroprotective |
| CPD100740 | Dubermatinib | Dubermatinib, oo sidoo kale loo yaqaan TP-0903, waa xakameyn awood leh oo xulashada AXL. TP-0903 waxay keentaa apoptosis weyn oo ku jira unugyada CLL B oo leh LD50 qiyam ah oo kala duwan oo nanomolar ah. Isku darka TP-0903 oo leh BTK inhibitors waxay kordhisaa CLL B-unugyada apoptosis AXL xad dhaafka ah waa mawduuc soo noqnoqda oo lagu arkay noocyo badan oo burooyin ah kuwaas oo helay caabbinta wakiilada kala duwan. Daawaynta unugyada kansarka ee leh TP-0903 waxay beddeshaa phenotype mesenchymal ee noocyo badan waxayna dareensiisaa unugyada kansarka inay ku daaweeyaan wakiilada kale ee la beegsaday. Maamulka TP-0903 ha ahaato hal wakiil ama marka lagu daro BTK inhibitors waxay waxtar u yeelan kartaa daaweynta bukaanada qaba CLL. |
| CPD100739 | NPS-1034 | NPS-1034 waa hor-jooge cusub oo MET ah, kaas oo xannibaya soo-dhoweynta MET ee firfircoon iyo mutant-keeda firfircoon. NPS-1034, waxay joojisaa noocyo kala duwan oo mutant ah oo firfircoon ee MET iyo sidoo kale HGF-firfircoon ee nooca duurjoogta ah ee MET. NPS-1034 waxay joojisay faafinta unugyada muujinaya MET firfircoon waxayna kor u qaadday dib u soo noqoshada burooyinka laga sameeyay unugyadaas oo ku jira qaabka xenograft jiirka iyada oo loo marayo ficillada anti-angiogenic iyo pro-apoptotic. NPS-1034 waxay kaloo joojisay firfircoonida HGF-kicinta ee calaamadaynta MET ee joogitaanka ama maqnaanshaha serum. Si gaar ah, NPS-1034 waxay joojisay saddex nooc oo MET ah kuwaas oo u adkeysanaya MET inhibitors SU11274, NVP-BVU972, iyo PHA665752. |
| CPD100738 | Glesatinib | Glesatinib, oo sidoo kale loo yaqaan MGCD-265, waa noole afka laga heli karo, unug yar-yar, tyrosine kinase inhibitor oo badan oo bartilmaameed leh oo leh firfircoonida antineoplastic ee suurtagalka ah. MGCD265 waxay ku xidhan tahay oo joojisaa fosforyaalka dhowr tayroosin kinases (RTKs), oo ay ku jiraan soo-dhoweeyaha c-Met (receptor factor factor koritaanka hepatocyte); receptor Tek / Tie-2; Noocyada kobaca xuubka xuubka xuubka (VEGFR) ee 1, 2, iyo 3; iyo macrophage-kicinta 1 reseptor (MST1R ama RON). |
