| CAT # | Magaca Alaabta | Sharaxaada |
| 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. |
| CPDB1540 | MSC2530818 | MSC2530818 waa Awood, Xulasho, iyo Af-ka-soo-baxa Bioavailable CDK8 Inhibitor leh CDK8 IC50 = 2.6 nM; Saadaasha PK ee aadanaha: Cl ~ 0.14 L/H/Kg; t1/2 ~ 2.4h; F > 75%. |
| CPDB1574 | CYC-065 | CYC065 waa jiil labaad, af laga heli karo ATP-horjoogaha tartanka CDK2/CDK9 kinases oo leh hawlo antineoplastic iyo kiimiko- ilaalin kara. |
| CPDB1594 | THZ531 | THZ531 waa isku-darka CDK12 iyo CDK13 covalent inhibitor. Kinases-ku-tiirsanaanta cyclin 12 iyo 13 (CDK12 iyo CDK13) ayaa door muhiim ah ka ciyaara habaynta qoraalka hiddo-wadaha. |
| CPDB1587 | THZ2 | THZ2, analooga ah THZ1, oo leh suurtogalnimada in lagu daaweeyo kansarka naasaha ee Triple-negative (TNBC), waa awood iyo xushay CDK7 inhibitor kaas oo ka adkaada xasilloonida THZ1 ee vivo. IC50: CDK7= 13.9 nM; Unugyada TNBC= 10 nM |
