| MPAKA # | Dzina lazogulitsa | Kufotokozera |
| CPD2809 | AMG-510 | AMG-510 ndi wamphamvu KRAS G12C covalent inhibitor. AMG-510 imayang'ana mosankha KRAS p.G12C mutant, pamlingo wa DNA, RNA kapena puloteni, ndikuletsa, kudzera m'njira yomwe sinadziwikebe, kuwonetsa ndi/kapena ma cell a chotupa kudzera mu KRAS p.G12C mutant. Izi zitha kulepheretsa kukula kwa maselo a chotupa a KRAS p.G12C |
| CPD100230 | JBJ-04-125-02 R-isomer | |
| CPD102300 | S-55746 | |
| CPD101235 | diABZI STING agonist-1 trihydrochloride | diABZI STING agonist-1 (trihydrochloride) ndi cholimbikitsa chosankha cha interferon majini (STING) receptor agonist, ndi EC50s ya 130, 186 nM ya anthu ndi mbewa, motsatana. |
| CPD101234 | diABZI STING agonist-1 (Tautomerism) | diABZI STING agonist-1 Tautomerism (compound 3) ndi cholimbikitsa chosankha cha interferon gene (STING) receptor agonist, ndi EC50s ya 130, 186 nM ya anthu ndi mbewa, motsatana. |
| CPD101233 | diABZI STING agonist-1 | diABZI STING agonist-1 ndi cholimbikitsa chosankha cha interferon majini (STING) receptor agonist, ndi EC50s ya 130, 186 nM ya anthu ndi mbewa, motsatana. |
| CPD101232 | STING agonist-4 | STING agonist-4 ndi stimulator ya Interferon Genes (STING) receptor agonist yokhala ndi inhibitory constant (IC50) ya 20 nM. STING agonist-4 ndi amidobenzimidazole (ABZI) yogwirizana ndi ma symmetry awiri kuti apange ma ABZI (diABZIs) omwe amamangirira ku STING ndi ntchito zama cell. |
| CPD101231 | STING agonist-3 | STING agonist-3, yotengedwa ku patent WO2017175147A1 (chitsanzo 10), ndiyosankha komanso yopanda nucleotide yaying'ono ya STING agonist yokhala ndi pEC50 ndi pIC50 ya 7.5 ndi 9.5, motsatira. STING agonist-3 ili ndi anti-chotupa chokhazikika komanso kuthekera kwakukulu kothandizira chithandizo cha khansa |
| CPD100904 | Voruciclib | Voruciclib, yomwe imadziwikanso kuti P1446A-05, ndi protein kinase inhibitor yeniyeni ya cyclin-dependent kinase 4 (CDK4) yokhala ndi ntchito yoletsa antiineoplastic. CDK4 inhibitor P1446A-05 makamaka imaletsa kusintha kwa gawo la CDK4-mediated G1-S, kumanga ma cell njinga ndikuletsa kukula kwa maselo a khansa. Serine / threonine kinase CDK4 imapezeka mu zovuta ndi D-mtundu wa G1 cyclins ndipo ndiye kinase woyamba kutsegulidwa pa mitogenic stimulation, kutulutsa maselo kuchokera pa siteji ya quiescent kupita ku G1 / S kukula kwa njinga; Ma CDK-cyclin complexes awonetsedwa kuti ali ndi phosphorylate the retinoblastoma (Rb) transcript factor kumayambiriro kwa G1, kuchotsa histone deacetylase (HDAC) ndikuletsa kuponderezedwa kwa transcriptional. |
| CPD100905 | Alvocidib | Alvocidib ndi mankhwala opangidwa ndi N-methylpiperidinyl chlorophenyl flavone. Monga inhibitor ya cyclin-dependent kinase, alvocidib imapangitsa kuti maselo asamamangidwe poletsa phosphorylation ya cyclin-dependent kinases (CDKs) ndi kutsika-regulating cyclin D1 ndi D3 mawu, zomwe zimapangitsa kuti G1 cell cycle kumangidwa ndi apoptosis. Wothandizira uyu ndiyenso mpikisano woletsa ntchito ya adenosine triphosphate. Yang'anani mayesero azachipatala omwe akugwira ntchito kapena mayesero otsekedwa achipatala pogwiritsa ntchito wothandizira uyu. |
| CPD100906 | Chithunzi cha BS-181 | BS-181 ndi choletsa kwambiri cha CDK cha CDK7 chokhala ndi IC(50) ya 21 nmol/L. Kuyesedwa kwa ma CDK ena komanso ma kinase ena 69 kunawonetsa kuti BS-181 idangoletsa CDK2 pamalo otsika kuposa 1 micromol/L, pomwe CDK2 idaletsedwa 35-fold less potently (IC(50) 880 nmol/L) kuposa CDK7. M'maselo a MCF-7, BS-181 inaletsa phosphorylation ya magawo a CDK7, kulimbikitsa kumangidwa kwa ma cell cycle ndi apoptosis kuti alepheretse kukula kwa maselo a khansa, ndikuwonetsa zotsatira za antitumor mu vivo. |
| CPD100907 | Rivicclib | Riviciclib, yemwe amadziwikanso kuti P276-00, ndi flavone ndi cyclin dependent kinase (CDK) inhibitor yomwe ingathe kuchitapo kanthu. P276-00 imamangiriza ndikuletsa Cdk4 / cyclin D1, Cdk1 / cyclin B ndi Cdk9 / cyclin T1, serine / threonine kinases yomwe imagwira ntchito yofunika kwambiri pakuwongolera ma cell ndi kuchuluka kwa ma cell. Kuletsa kwa kinasewa kumabweretsa kumangidwa kwa ma cell panthawi ya kusintha kwa G1/S, zomwe zimapangitsa kuti apoptosis alowe, ndikuletsa kuchulukana kwa maselo otupa. |
| CPD100908 | Mtengo wa MC180295 | MC180295 ndi yosankha kwambiri CDK9 inhibitor (IC50 = 5 nM). (MC180295 ili ndi ntchito zambiri zotsutsana ndi khansa mu vitro ndipo imagwira ntchito mu zitsanzo za khansa ya vivo. Kuwonjezera apo, CDK9 inhibition imalimbikitsa chitetezo cha mthupi α-PD-1 mu vivo, ndikupangitsa kuti ikhale chandamale chabwino kwambiri cha epigenetic therapy ya khansa. |
| 1073485-20-7 | LDC000067 | LDC000067 ndi choletsa champhamvu komanso chosankha cha CDK9. LDC000067 inhibited in vitro transcript mu ATP-mpikisano komanso kutengera mlingo. Kufotokozera kwa ma gene kuma cell omwe amathandizidwa ndi LDC000067 kunawonetsa kuchepetsedwa kosankha kwa ma mRNA osakhalitsa, kuphatikiza owongolera ofunikira pakuchulukira ndi apoptosis. Kuwunika kwa kaphatikizidwe ka de novo RNA kunawonetsa mbali zambiri zabwino za CDK9. Pama cell ndi ma cell, LDC000067 idatulutsanso zotsatira za CDK9 zoletsa monga kuyimitsidwa kwa RNA polymerase II pamajini ndipo, chofunikira kwambiri, kulowetsedwa kwa apoptosis m'maselo a khansa. LDC000067 imalepheretsa kulembedwa kwa P-TEFb mu vitro. Imapangitsa apoptosis mu vitro ndi mu vivo kuphatikiza BI 894999. |
| CPD100910 | Chithunzi cha SEL120-34A | SEL120-34A ndi CDK8 inhibitor yamphamvu komanso yosankha yogwira ntchito m'maselo a AML okhala ndi serine phosphorylation ya STAT1 ndi STAT5 transactivation domains. EL120-34A imalepheretsa phosphorylation ya STAT1 S727 ndi STAT5 S726 m'maselo a khansa mu vitro. Nthawi zonse, kuwongolera kwa STATs- ndi NUP98-HOXA9- kutengera zolembera kwawonedwa ngati njira yayikulu yochitira zinthu mu vivo. |
| CPD100501 | UNC2541 | UNC2541 ndi choletsa champhamvu komanso cha MerTK-specific chomwe chimawonetsa zochitika zoletsa ma micromolar mu cell-based ELISA. Kuphatikiza apo, mawonekedwe a X-ray a mapuloteni a MerTK muzovuta ndi 11 adatsimikiza kuti ma macrocycles awa amamanga m'thumba la MerTK ATP. UNC2541 inawonetsa IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| Chithunzi cha CPD100745 | Mtengo wa RU-302 | RU-302 ndi buku la pan-tam inhibitor, kutsekereza mawonekedwe pakati pa tam ig1 ectodomain ndi gas6 lg domain, kuletsa mwamphamvu ma cell a axl atolankhani ndi mizere yama cell a tam receptors. |
| CPD100744 | Mtengo wa 916562 | |
| CPD100743 | Ningetinib-tosylate | CT-053, yomwe imadziwikanso kuti DE-120, ndi VEGF ndi PDGF inhibitor yomwe ingathe kuchiza kunyowa kwa macular chifukwa cha ukalamba. |
| Chithunzi cha CPD100742 | SGI-7079 | SGI-7079 ndi Axl inhibitor yamphamvu komanso yosankha yokhala ndi zochita zolimbana ndi khansa. SGI-7079 inaletsa bwino Axl kutsegula pamaso pa exogenous Gas6 ligand. SGI-7079 inaletsa kukula kwa chotupa m'njira yodalira mlingo. Axl ndi chandamale chothandizira kuthana ndi EGFR inhibitor resistance. |
| CPD100741 | 2-D08 | 2-D08 ndi flavone yopanga yomwe imalepheretsa sumoylation. 2-D08 inawonetsa anti-aggregatory ndi neuroprotective effect |
| CPD100740 | Dubematinib | Dubermatinib, yomwe imadziwikanso kuti TP-0903, ndi yamphamvu komanso yosankha AXL inhibitor. TP-0903 imapangitsa apoptosis yayikulu m'maselo a CLL B okhala ndi ma LD50 amitundu ya nanomolar. Kuphatikiza kwa TP-0903 ndi BTK inhibitors augments CLL B-cell apoptosis AXL overexpression ndi mutu wobwerezabwereza womwe umawonedwa mumitundu ingapo ya chotupa yomwe yayamba kukana othandizira osiyanasiyana. Kuchiza kwa ma cell a khansa ndi TP-0903 kumabweza mesenchymal phenotype m'mitundu ingapo ndikulimbikitsa ma cell a khansa kuti alandire chithandizo ndi othandizira ena omwe akuwaganizira. Ulamuliro wa TP-0903 mwina ngati wothandizira m'modzi kapena kuphatikiza ndi BTK inhibitors zitha kukhala zothandiza pochiza odwala omwe ali ndi CLL. |
| CPD100739 | NPS-1034 | NPS-1034 ndi buku la MET inhibitor, lomwe limalepheretsa cholandilira cha MET chokhazikitsidwa ndi zosinthika zake zosinthika. NPS-1034, imalepheretsa mitundu yosiyanasiyana yosinthika ya MET komanso HGF-activated wild-type MET. NPS-1034 inaletsa kuchuluka kwa maselo omwe akuwonetsa MET yoyendetsedwa ndikulimbikitsa kuyambiranso kwa zotupa zomwe zimapangidwa kuchokera ku maselo oterowo mumtundu wa mbewa wa xenograft kudzera muzochita zotsutsa-angiogenic ndi pro-apoptotic. NPS-1034 idaletsanso kuyambitsa kwa HGF-kukondoweza kwa siginecha ya MET pamaso kapena kusakhalapo kwa seramu. Makamaka, NPS-1034 idaletsa mitundu itatu ya MET yomwe imalimbana ndi MET inhibitors SU11274, NVP-BVU972, ndi PHA665752. |
| CPD100738 | Glesatinib | Glesatinib, yomwe imadziwikanso kuti MGCD-265, ndi bioavailable pamlomo, yaing'ono-molecule, multitargeted tyrosine kinase inhibitor yomwe ingathe kuchitapo kanthu. MGCD265 imamangiriza ndi kulepheretsa phosphorylation ya angapo receptor tyrosine kinases (RTKs), kuphatikizapo c-Met receptor (hepatocyte kukula factor receptor); cholandilira cha Tek/Tie-2; vascular endothelial growth factor receptor (VEGFR) mitundu 1, 2, ndi 3; ndi macrophage-stimulating 1 receptor (MST1R kapena RON). |
