| KATSE # | Lebitso la Sehlahiswa | Tlhaloso |
| CPD2809 | AMG-510 | AMG-510 ke KRAS G12C covalent inhibitor e matla. AMG-510 e ikhethela phetoho ea KRAS p.G12C, e ka ba boemong ba DNA, RNA kapa protheine, 'me e thibela, ka mokhoa o ntseng o e-so hlakisoe, pontšo ea le/kapa tumor cell signing ka KRAS p.G12C mutant. Sena se ka thibela kholo ea lisele tsa tumor tsa KRAS p.G12C |
| CPD100230 | JBJ-04-125-02 R-isomer | |
| CPD102300 | S-55746 | |
| CPD101235 | diABZI STING agonist-1 trihydrochloride | diABZI STING agonist-1 (trihydrochloride) ke stimulator e khethollang ea liphatsa tsa lefutso tsa interferon (STING) receptor agonist, e nang le EC50s ea 130, 186 nM bakeng sa motho le mouse, ka ho latellana. |
| CPD101234 | diABZI STING agonist-1 (Tautomerism) | diABZI STING agonist-1 Tautomerism (motsoako oa 3) ke ntho e susumetsang e khethollang ea liphatsa tsa lefutso tsa interferon (STING) receptor agonist, e nang le EC50s ea 130, 186 nM bakeng sa motho le mouse, ka ho latellana. |
| CPD101233 | diABZI STING agonist-1 | diABZI STING agonist-1 ke ntho e susumetsang e khethollang ea liphatsa tsa lefutso tsa interferon (STING), tse nang le EC50s ea 130, 186 nM bakeng sa motho le mouse, ka ho latellana. |
| CPD101232 | STING agonist-4 | STING agonist-4 ke stimulator ea Interferon Genes (STING) receptor agonist e nang le inhibitory constant (IC50) ea 20 nM. STING agonist-4 ke metsoako e 'meli e amanang le amidobenzimidazole (ABZI) e amanang le symmetry ho theha li-ABZI tse hokahantsoeng (diABZIs) tse nang le tlamo e matlafalitsoeng ho STING le tšebetso ea cellular. |
| CPD101231 | STING agonist-3 | STING agonist-3, e ntšitsoeng ho patent WO2017175147A1 (mohlala 10), ke ntho e khethollang le e seng ea nucleotide e nyenyane ea molek'hule STING agonist e nang le pEC50 le pIC50 ea 7.5 le 9.5, ka ho latellana. STING agonist-3 e na le phello e tšoarellang ea anti-tumor le monyetla o moholo oa ho ntlafatsa kalafo ea mofets'e |
| CPD100904 | Voruciclib | Voruciclib, eo hape e tsejoang e le P1446A-05, ke protheine kinase inhibitor e khethehileng bakeng sa cyclin-dependent kinase 4 (CDK4) e nang le ts'ebetso e ka bang teng ea antineoplastic. CDK4 inhibitor P1446A-05 ka ho khetheha e thibela phetoho ea mohato oa CDK4-mediated G1-S, ho tšoara libaesekele tsa sele le ho thibela kholo ea lisele tsa mofetše. CDK4 ea serine / threonine kinase e fumanoa ka mokhoa o rarahaneng o nang le li-cyclins tsa mofuta oa D-mofuta oa G1 'me ke kinase ea pele e sebelisoang holim'a ts'usumetso ea mitogenic, e lokolla lisele ho tloha sethaleng se khutsitseng ho ea sethaleng sa G1 / S sa baesekele ea kholo; Li-CDK-cyclin complexes li bontšitsoe ho phosphorylate the retinoblastoma (Rb) transcription factor qalong ea G1, ho tlosa histone deacetylase (HDAC) le ho thibela khatiso ea transcriptional. |
| CPD100905 | Alvocidib | Alvocidib ke motsoako oa maiketsetso oa N-methylpiperidinyl chlorophenyl flavone. Joalo ka inhibitor ea cyclin-dependent kinase, alvocidib e etsa hore ho ts'oaroe ha cell cycle ka ho thibela phosphorylation ea cyclin-dependent kinases (CDKs) le ka ho theola taolo ea cyclin D1 le polelo ea D3, e fellang ka ho ts'oaroa ha lisele tsa G1 le apoptosis. Moemeli ona hape ke inhibitor ea tlholisano ea ts'ebetso ea adenosine triphosphate. Sheba liteko tse sebetsang tsa tleliniki kapa liteko tse koetsoeng tsa bongaka u sebelisa moemeli enoa. |
| CPD100906 | BS-181 | BS-181 ke CDK inhibitor e khethang haholo bakeng sa CDK7 e nang le IC(50) ea 21 nmol/L. Liteko tsa li-CDK tse ling hammoho le li-kinase tse ling tse 69 li bonts'itse hore BS-181 e thibela CDK2 feela maemong a tlase ho 1 micromol/L, 'me CDK2 e thibetsoe ka makhetlo a 35 ka matla (IC(50) 880 nmol/L) ho feta CDK7. Liseleng tsa MCF-7, BS-181 e thibetse phosphorylation ea li-substrates tsa CDK7, e khothalelitse ho ts'oaroa ha potoloho ea lisele le apoptosis ho thibela kholo ea lisele tsa mofetše, mme e bonts'a litlamorao tsa antitumor ho vivo. |
| CPD100907 | Rivicclib | Riviciclib, e tsejoang hape e le P276-00, ke inhibitor ea flavone le cyclin dependent kinase (CDK) e nang le ts'ebetso e ka bang teng ea antineoplastic. P276-00 e khetha ho tlama le ho thibela Cdk4 / cyclin D1, Cdk1 / cyclin B le Cdk9 / cyclin T1, serine / threonine kinases e phethang karolo ea bohlokoa taolong ea potoloho ea lisele le ho ata ha lisele. Ho thibela li-kinase tsena ho lebisa ho ts'oaroe ha potoloho ea lisele nakong ea phetoho ea G1 / S, ka hona ho lebisa ho induction ea apoptosis, le ho thibela ho ata ha lisele tsa tumor. |
| CPD100908 | MC180295 | MC180295 ke CDK9 inhibitor e khethang haholo (IC50 = 5 nM). (MC180295 e na le ts'ebetso e pharaletseng ea anti-cancer in vitro mme e sebetsa hantle mefuteng ea mofets'e oa vivo. Ho feta moo, CDK9 inhibition e hlokomelisa ho immune checkpoint inhibitor α-PD-1 in vivo, e etsa hore e be sepheo se setle sa kalafo ea epigenetic ea mofets'e. |
| 1073485-20-7 | LDC000067 | LDC000067 ke inhibitor e matla le e khethang ea CDK9. LDC000067 e thibetsoe ho ngoloa ka har'a vitro ka mokhoa oa tlholisano oa ATP le o itšetlehileng ka tekanyo. Tlhaloso ea liphatsa tsa lefutso ea lisele tse tšoaroang ka LDC000067 e bonts'itse phokotso e ikhethileng ea li-mRNA tsa nakoana, ho kenyelletsa le balaoli ba bohlokoa ba ho ata le apoptosis. Tlhahlobo ea de novo RNA synthesis e khothalelitse karolo e fapaneng e ntle ea CDK9. Boemong ba limolek'hule le liselefouno, LDC000067 e hlahisitse litlamorao tsa thibelo ea CDK9 joalo ka khefutso e ntlafalitsoeng ea RNA polymerase II liphatseng tsa lefutso, 'me haholo-holo, ho kenngoa ha apoptosis liseleng tsa mofetše. LDC000067 e thibela ho ngoloa ha P-TEFb e itšetlehileng ka in vitro. E kenya apoptosis in vitro le in vivo hammoho le BI 894999. |
| CPD100910 | SEL120-34A | SEL120-34A ke CDK8 inhibitor e matla le e khethang e sebetsang liseleng tsa AML tse nang le maemo a phahameng a serine phosphorylation ea STAT1 le STAT5 transactivation domains. EL120-34A e thibela phosphorylation ea STAT1 S727 le STAT5 S726 liseleng tsa mofetše ka vitro. Ka mokhoa o ts'oanang, taolo ea STATs- le NUP98-HOXA9- e itšetlehileng ka transcript e 'nile ea hlokomeloa e le mokhoa o ka sehloohong oa ts'ebetso ka vivo. |
| CPD100501 | UNC2541 | UNC2541 ke inhibitor e matla le e khethehileng ea MerTK e bonts'ang ts'ebetso ea sub-micromolar inhibitory ho ELISA e thehiloeng liseleng. Ho phaella moo, sebopeho sa X-ray sa protheine ea MerTK e rarahaneng le 11 e ile ea rarolloa ho bontša hore li-macrocycle tsena li tlama ka mokotleng oa MerTK ATP. UNC2541 e bontšitse IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| CPD100745 | RU-302 | RU-302 ke buka e ncha ea pan-tam inhibitor, e thibelang khokahano lipakeng tsa tam ig1 ectodomain le gas6 lg domain, e thibelang mela ea lisele tsa motlalehi oa axl le mela ea lisele tsa mofets'e tsa tam. |
| CPD100744 | R916562 | |
| CPD100743 | Ningetinib-tosylate | CT-053, eo hape e tsejoang e le DE-120, ke VEGF le PDGF inhibitor e ka bang teng bakeng sa ho phekola ho senyeha ha macular ho amanang le lilemo. |
| CPD100742 | SGI-7079 | SGI-7079 ke Axl inhibitor e matla le e khethang e nang le ts'ebetso e ka bang teng ea anticancer. SGI-7079 e ile ea thibela ka katleho ts'ebetso ea Axl ka pel'a Gas6 ligand e sa tloaelehang. SGI-7079 e thibetse ho hola ha hlahala ka mokhoa o itšetlehileng ka lethal dose. Axl ke sepheo sa kalafo se ka bang teng bakeng sa ho hlola EGFR inhibitor resistance. |
| CPD100741 | 2-D08 | 2-D08 ke flavone ea maiketsetso e thibelang sumoylation. 2-D08 e bonts'itse anti-aggregatory le neuroprotective effect |
| CPD100740 | Dubermatinib | Dubermatinib, e tsejoang hape e le TP-0903, ke inhibitor e matla le e khethang ea AXL. TP-0903 e kenya apoptosis e kholo liseleng tsa CLL B tse nang le boleng ba LD50 ba mefuta ea nanomolar. Motsoako oa TP-0903 le BTK inhibitors augments CLL B-cell apoptosis AXL overexpression ke sehlooho se hlahang hape se hlokometsoeng ka mefuta e mengata ea hlahala e fumaneng ho hanyetsa mahlahana a fapaneng. Kalafo ea lisele tsa mofetše ka TP-0903 e khutlisa mesenchymal phenotype mefuteng e mengata mme e hlokomelisa lisele tsa mofetše hore li phekoloe ka li-agent tse ling tse lebisitsoeng ho tsona. Tsamaiso ea TP-0903 e le moemeli a le mong kapa hammoho le BTK inhibitors e ka sebetsa hantle ho phekola bakuli ba CLL. |
| CPD100739 | NPS-1034 | NPS-1034 ke buka e ncha ea MET inhibitor, e thibelang li-receptor tsa MET tse kentsoeng le liphetoho tsa eona tse sebetsang hantle. NPS-1034, e thibela mefuta e fapaneng e sebetsang ea MET hammoho le HGF-activated wild-type MET. NPS-1034 e thibetse ho ata ha lisele tse hlalosang MET e sebelisitsoeng mme e khothalelitse ho fokotseha ha lihlahala tse entsoeng liseleng tse joalo ka mohlala oa mouse xenograft ka liketso tse khahlanong le angiogenic le pro-apoptotic. NPS-1034 e boetse e thibela ts'ebetso e tsositsoeng ea HGF ea lipontšo tsa MET boteng kapa bosieong ba serum. Ka ho hlakileng, NPS-1034 e thibetse mefuta e meraro ea MET e hanyetsanang le MET inhibitors SU11274, NVP-BVU972, le PHA665752. |
| CPD100738 | Glesatinib | Glesatinib, eo hape e tsejoang e le MGCD-265, ke bioavailable ka molomo, molek'hule e nyenyane, e nang le mefuta e mengata ea tyrosine kinase inhibitor e nang le ts'ebetso e ka 'nang ea e-ba teng ea antineoplastic. MGCD265 e tlama le ho thibela phosphorylation ea li-receptor tyrosine kinases tse 'maloa (RTKs), ho kenyelletsa le c-Met receptor (hepatocyte growth factor receptor); mokelikeli oa Tek/Tie-2; vascular endothelial growth factor receptor (VEGFR) mefuta ea 1, 2, le 3; le macrophage-stimulating 1 receptor (MST1R kapa RON). |
