| CAT # | Sunan samfur | Bayani |
| Saukewa: CPD2809 | Saukewa: AMG-510 | AMG-510 shine mai hanawa mai ƙarfi na KRAS G12C. AMG-510 zaɓen yana hari da mutantan KRAS p.G12C, a ko dai DNA, RNA ko matakin furotin, kuma yana hana, ta hanyar da ba a fayyace ba tukuna, bayyanar da siginar ƙwayar ƙwayar cuta ta KRAS p.G12C. Wannan na iya hana girma a cikin KRAS p.G12C-bayyana ƙwayoyin ƙari |
| Saukewa: CPD100230 | JBJ-04-125-02 R-isomer | |
| Saukewa: CPD102300 | S-55746 | |
| Saukewa: CPD101235 | DIABZI STING agonist-1 trihydrochloride | diABZI STING agonist-1 (trihydrochloride) wani zaɓi ne na agonist mai karɓa na interferon genes (STING), tare da EC50s na 130, 186 nM don mutum da linzamin kwamfuta, bi da bi. |
| Saukewa: CPD101234 | diABZI STING agonist-1 (Tautomerism) | diABZI STING agonist-1 Tautomerism (compound 3) wani zaɓi ne mai zaɓaɓɓen agonist mai karɓa na ƙwayoyin cuta na interferon (STING), tare da EC50s na 130, 186 nM don ɗan adam da linzamin kwamfuta, bi da bi. |
| Saukewa: CPD101233 | diABZI STING agonist-1 | diABZI STING agonist-1 zaɓi ne mai zaɓaɓɓen agonist mai karɓa na ƙwayoyin interferon (STING), tare da EC50s na 130, 186 nM don ɗan adam da linzamin kwamfuta, bi da bi. |
| Saukewa: CPD101232 | STING agonist-4 | STING agonist-4 shine mai kara kuzari na Interferon Genes (STING) agonist mai karɓa tare da tabbataccen inhibitory akai (IC50) na 20 nM. STING agonist-4 wani abu ne na amidobenzimidazole (ABZI) da ke da alaƙa guda biyu don ƙirƙirar ABZI mai alaƙa (diABZIs) tare da haɓaka haɓakawa zuwa STING da aikin salula. |
| Saukewa: CPD101231 | STING agonist-3 | STING agonist-3, wanda aka samo daga lamban kira WO2017175147A1 (misali 10), zaɓi ne kuma mara-nucleotide ƙananan ƙwayoyin STING agonist tare da pEC50 da pIC50 na 7.5 da 9.5, bi da bi. STING agonist-3 yana da tasirin anti-tumor mai dorewa da babban yuwuwar inganta maganin cutar kansa |
| Saukewa: CPD100904 | Voruciclib | Voruciclib, wanda kuma aka sani da P1446A-05, shine mai hana furotin kinase na musamman don kinase 4 (CDK4) mai dogara da cyclin tare da yiwuwar aikin antineoplastic. CDK4 inhibitor P1446A-05 musamman yana hana CDK4-matsakaici G1-S lokaci mika mulki, kama hawan keke da kuma hana ciwon daji girma. Ana samun serine / threonine kinase CDK4 a cikin hadaddun tare da nau'in D-type G1 cyclins kuma shine kinase na farko don kunnawa akan haɓakar mitogenic, sakin sel daga matakin quiescent zuwa matakin hawan keke na G1 / S; CDK-cyclin complexes an nuna su phosphorylate da retinoblastoma (Rb) transcription factor a farkon G1, murkushe histone deacetylase (HDAC) da kuma toshe transcriptional danniya. |
| Saukewa: CPD100905 | Alvocidib | Alvocidib wani abu ne na roba N-methylpiperidinyl chlorophenyl flavone fili. A matsayin mai hana cyclin-dogara kinase, alvocidib yana haifar da kamawar kwayar halitta ta hanyar hana phosphorylation na cyclin-dependent kinases (CDKs) da kuma ta hanyar ƙaddamar da cyclin D1 da D3 magana, wanda ya haifar da kama G1 cell cycle da apoptosis. Wannan wakili kuma mai gasa ne mai hana aikin adenosine triphosphate. Bincika gwaje-gwajen asibiti masu aiki ko rufaffiyar gwajin asibiti ta amfani da wannan wakili. |
| Saukewa: CPD100906 | BS-181 | BS-181 babban zaɓi ne mai hana CDK don CDK7 tare da IC(50) na 21 nmol/L. Gwajin wasu CDKs da kuma wani 69 kinases ya nuna cewa BS-181 kawai ya hana CDK2 a matakan ƙasa da 1 micromol/L, tare da hana CDK2 35-ninka ƙasa da ƙarfi (IC(50) 880 nmol/L) fiye da CDK7. A cikin sel na MCF-7, BS-181 ya hana phosphorylation na CDK7 substrates, inganta tsarin sake zagayowar cell da apoptosis don hana ci gaban ƙwayoyin cutar kansa, kuma ya nuna tasirin antitumor a cikin vivo. |
| Saukewa: CPD100907 | Riviciclib | Riviciclib, wanda kuma aka sani da P276-00, shine mai hana flavone da cyclin kinase (CDK) mai hanawa tare da yiwuwar aikin antineoplastic. P276-00 zaɓaɓɓen ɗaure da kuma hana Cdk4/cyclin D1, Cdk1/cyclin B da Cdk9/cyclin T1, serine/threonine kinases waɗanda ke taka muhimmiyar rawa a cikin ka'idar tsarin tantanin halitta da haɓakar salula. Hana waɗannan kinases yana haifar da kamawar ƙwayar ƙwayar cuta a lokacin canjin G1/S, wanda hakan zai haifar da ƙaddamar da apoptosis, da kuma hana yaduwar ƙwayar ƙwayar cuta. |
| Saukewa: CPD100908 | Saukewa: MC180295 | MC180295 mai hanawa CDK9 ne mai zaɓin zaɓi (IC50 = 5 nM). (MC180295 yana da faffadan aikin rigakafin ciwon daji a cikin vitro kuma yana da tasiri a cikin nau'ikan ciwon daji na vivo. Bugu da ƙari, hana CDK9 yana da hankali ga mai hanawa na rigakafi α-PD-1 a cikin vivo, yana mai da shi kyakkyawan manufa don maganin ciwon daji na epigenetic. |
| 1073485-20-7 | Saukewa: LDC000067 | LDC000067 mai ƙarfi ne kuma mai hanawa CDK9. LDC000067 an hana rubutun in vitro a cikin gasa-ATP da kuma dogaro da kashi. Bayyanar bayanan kwayoyin halitta na sel da aka bi da su tare da LDC000067 sun nuna raguwar zaɓi na mRNAs na ɗan gajeren lokaci, gami da mahimman masu kula da yaduwa da apoptosis. Binciken hadawar de novo RNA ya ba da shawarar faffadan ingantacciyar rawar CDK9. A matakin kwayoyin halitta da salon salula, LDC000067 ya haifar da tasirin halayen halayen hana CDK9 kamar ingantaccen dakatarwar RNA polymerase II akan kwayoyin halitta kuma, mafi mahimmanci, shigar da apoptosis a cikin ƙwayoyin kansa. LDC000067 yana hana P-TEFb-dogara a rubutun in vitro. Yana haifar da apoptosis a cikin vitro da in vivo a hade tare da BI 894999. |
| Saukewa: CPD100910 | Saukewa: SEL120-34A | SEL120-34A shine mai hanawa CDK8 mai ƙarfi da zaɓi mai aiki a cikin sel AML tare da manyan matakan serine phosphorylation na STAT1 da STAT5 yankuna transactivation. EL120-34A yana hana phosphorylation na STAT1 S727 da STAT5 S726 a cikin ƙwayoyin ciwon daji a cikin vitro. A koyaushe, an lura da ƙa'idodin STATs- da NUP98-HOXA9- masu dogaro da rubutun a matsayin babban tsarin aiki a vivo. |
| Saukewa: CPD100501 | Saukewa: UNC2541 | UNC2541 mai ƙarfi ne kuma takamaiman mai hanawa MerTK wanda ke nuna ayyukan hanawa na ƙananan ƙwayoyin cuta a cikin tushen ELISA. Bugu da kari, an warware tsarin X-ray na furotin MerTK a hadaddun tare da 11 don nuna cewa waɗannan macrocycles suna ɗaure a cikin aljihun MerTK ATP. UNC2541 ya nuna IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| Saukewa: CPD100745 | Farashin RU-302 | RU-302 sabon inhibitor pan-tam ne, yana toshe mu'amala tsakanin tam ig1 ectodomain da gas6 lg yankin, da ƙarfi yana hana layin salula na axl da masu karɓar tam na asali. |
| Saukewa: CPD100744 | R916562 | |
| Saukewa: CPD100743 | Ningetinib-Tosylate | CT-053, wanda kuma aka sani da DE-120, VEGF ne da mai hana PDGF mai yuwuwa don kula da jigon macular degeneration. |
| Saukewa: CPD100742 | SGI-7079 | SGI-7079 shine mai hanawa Axl mai ƙarfi kuma mai zaɓi tare da yuwuwar aikin rigakafin ciwon daji. SGI-7079 yadda ya kamata ya hana Axl kunnawa a gaban exogenous Gas6 ligand. SGI-7079 ya hana haɓakar ƙwayar cuta ta hanyar dogaro da kashi. Axl shine yuwuwar manufa ta warkewa don shawo kan juriya mai hana EGFR. |
| Saukewa: CPD100741 | 2-D08 | 2-D08 flavone ne na roba wanda ke hana sumoylation. 2-D08 ya nuna anti-aggregatory da neuroprotective sakamako |
| Saukewa: CPD100740 | Dubermatinib | Dubermatinib, wanda kuma aka sani da TP-0903, shine mai hanawa AXL mai ƙarfi da zaɓi. TP-0903 yana haifar da babban apoptosis a cikin ƙwayoyin CLL B tare da ƙimar LD50 na jeri na nanomolar. Haɗin TP-0903 tare da masu hana BTK suna haɓaka CLL B-cell apoptosis AXL overexpression jigo ne mai sake faruwa a cikin nau'ikan ƙari da yawa waɗanda suka sami juriya ga wakilai daban-daban. Kula da sel na ciwon daji tare da tp-0903 ya juya da m phenchymal phenchympe a cikin samfura da yawa da sel sel sel mai magani tare da wasu wakilan da aka yi niyya. Gudanar da TP-0903 ko dai a matsayin wakili ɗaya ko a hade tare da masu hana BTK na iya zama tasiri a cikin kula da marasa lafiya tare da CLL. |
| Saukewa: CPD100739 | Saukewa: NPS-1034 | NPS-1034 sabon labari ne mai hanawa MET, wanda ke hana mai karɓar MET da aka kunna da mutants ɗin sa. NPS-1034. NPS-1034 ya hana yaduwar kwayoyin halitta da ke bayyana MET da aka kunna kuma ya inganta farfadowa na ciwace-ciwacen da aka samo daga irin waɗannan kwayoyin halitta a cikin samfurin xenograft na linzamin kwamfuta ta hanyar anti-angiogenic da pro-apoptotic ayyuka. NPS-1034 kuma ya hana HGF-ƙarfafa kunna siginar MET a gaban ko babu ruwan magani. Musamman, NPS-1034 ya hana bambance-bambancen MET guda uku waɗanda ke da juriya ga masu hana MET SU11274, NVP-BVU972, da PHA665752. |
| Saukewa: CPD100738 | Glesatinib | Glesatinib, wanda kuma aka sani da MGCD-265, abu ne da ake iya samu ta baki, ƙananan ƙwayoyin cuta, mai hana tyrosine kinase mai yawan niyya tare da yuwuwar aikin antineoplastic. MGCD265 yana ɗaure da kuma hana phosphorylation na tyrosine kinases masu karɓa da yawa (RTKs), ciki har da mai karɓa na c-Met (mai karɓar haɓakar haɓakar hepatocyte); mai karɓar Tek / Tie-2; Nau'in nau'in 1, 2, da 3 masu karɓa (VEGFR) na jijiyoyi na endothelial; da macrophage-stimulating 1 mai karɓa (MST1R ko RON). |
