| CAT # | Product Name | Tsanangudzo |
| CPD2809 | AMG-510 | AMG-510 ine simba KRAS G12C covalent inhibitor. AMG-510 yakanangana neiyo KRAS p.G12C inoshanduka, ingave iyo DNA, RNA kana protein level, uye inodzivirira, nenzira isati yanyatsojekeswa, kutaura uye/kana tumor cell kusaina kuburikidza neKRAS p.G12C mutant. Izvi zvinogona kutadzisa kukura muKRAS p.G12C-inoratidza bundu maseru |
| CPD100230 | JBJ-04-125-02 R-isomer | |
| CPD102300 | S-55746 | |
| CPD101235 | DiABZI STING agonist-1 trihydrochloride | diABZI STING agonist-1 (trihydrochloride) is a selective stimulator ye interferon genes (STING) receptor agonist, ine EC50s ye130, 186 nM yevanhu nembeva, zvichiteerana. |
| CPD101234 | diABZI STING agonist-1 (Tautomerism) | diABZI STING agonist-1 Tautomerism (compound 3) is a selective stimulator ye interferon genes (STING) receptor agonist, ine EC50s ye130, 186 nM yemunhu nembeva, zvichiteerana. |
| CPD101233 | diABZI STING agonist-1 | diABZI STING agonist-1 inosarudza inokurudzira ye interferon genes (STING) receptor agonist, ine EC50s ye130, 186 nM yevanhu nembeva, zvichiteerana. |
| CPD101232 | STING agonist-4 | STING agonist-4 inosimudzira yeInterferon Genes (STING) receptor agonist ine inooneka inhibitory nguva dzose (IC50) ye20 nM. STING agonist-4 ndeye maviri amidobenzimidazole ane hukama-ane symmetry amidobenzimidazole (ABZI)-yakavakirwa musanganiswa kugadzira akabatana ABZIs (diABZIs) ane inosungirirwa kuSTING uye cellular basa. |
| CPD101231 | STING agonist-3 | STING agonist-3, yakatorwa kubva patent WO2017175147A1 (muenzaniso 10), inosarudza uye isiri-nucleotide diki-molecule STING agonist ine pEC50 uye pIC50 ye7.5 uye 9.5, zvichiteerana. STING agonist-3 ine yakasimba anti-tumor mhedzisiro uye yakakura mukana wekuvandudza kurapwa kwegomarara |
| CPD100904 | Voruciclib | Voruciclib, inozivikanwawo seP1446A-05, iprotein kinase inhibitor yakanangana necyclin-dependent kinase 4 (CDK4) ine inogona kuita antineoplastic chiitiko. CDK4 inhibitor P1446A-05 inonyanya kurambidza CDK4-mediated G1-S chikamu shanduko, kusunga sero bhasikoro uye inhibiting cancer cell kukura. Iyo serine/threonine kinase CDK4 inowanikwa mune yakaoma ine D-mhando G1 cyclins uye ndiyo yekutanga kinase kuti ishandiswe pane mitogenic kukurudzira, kuburitsa masero kubva padanho rakanyarara kupinda muG1/S kukura bhasikoro nhanho; CDK-cyclin complexes yakaratidzwa kune phosphorylate iyo retinoblastoma (Rb) chinyorwa chekunyora mukutanga kweG1, ichibvisa histone deacetylase (HDAC) uye ichivharira kudzvinyirirwa kwezvinyorwa. |
| CPD100905 | Alvocidib | Alvocidib is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. Se inhibitor ye cyclin-inotsamira kinase, alvocidib induces cell cycle kusungwa nekudzivirira phosphorylation ye cyclin-dependent kinases (CDKs) uye nekudzika-inotonga cyclin D1 uye D3 kutaura, zvichiita kuti G1 cell cycle kusungwa uye apoptosis. Uyu mumiririri zvakare inokwikwidza inhibitor yeadenosine triphosphate basa. Tarisa uone kushanda kwekiriniki miedzo kana kuvharwa kwekiriniki miedzo uchishandisa mumiririri uyu. |
| CPD100906 | BS-181 | BS-181 inonyatso kusarudza CDK inhibitor yeCDK7 ine IC(50) ye21 nmol/L. Kuongororwa kwemamwe maCDK pamwe nemamwe makumi matanhatu nemapfumbamwe kinase kwakaratidza kuti BS-181 yakangovharira CDK2 pamitsetse yakaderera pane 1 micromol/L, neCDK2 ichivharirwa makumi matatu neshanu zvishoma zvine simba (IC(50) 880 nmol/L) pane CDK7. Mumasero eMCF-7, BS-181 yakadzivisa phosphorylation yeCDK7 substrates, yakasimudzira kusungwa kwesero cycle uye apoptosis kudzivisa kukura kwekenza cell mitsara, uye yakaratidza antitumor madhara mu vivo. |
| CPD100907 | Rivicclib | Riviciclib, inozivikanwawo seP276-00, ndeye flavone uye cyclin inotsamira kinase (CDK) inhibitor ine inogona kuita antineoplastic chiitiko. P276-00 inosarudza inosunga uye inhibits Cdk4 / cyclin D1, Cdk1 / cyclin B uye Cdk9 / cyclin T1, serine / threonine kinases inobata mabasa anokosha mukugadzirisa kwesero uye kuwedzera kwemasero. Kudzivirirwa kweaya kinase kunotungamira kusungwa kwesero kusungwa panguva yeG1/S shanduko, zvichizotungamira mukuiswa kweapoptosis, uye kuvharirwa kwebundu cell kuwanda. |
| CPD100908 | MC180295 | MC180295 inonyanya kusarudza CDK9 inhibitor (IC50 = 5 nM). (MC180295 ine yakakura anti-cancer chiitiko mu vitro uye inoshanda mu vivo cancer modhi. Uyezve, CDK9 inhibition inosimudzira kune immune checkpoint inhibitor α-PD-1 mu vivo, zvichiita kuti ive chinangwa chakanakisa che epigenetic kurapa kenza. |
| 1073485-20-7 | LDC000067 | LDC000067 ine simba uye inosarudza CDK9 inhibitor. LDC000067 inhibited in vitro transcription nenzira yeATP-yemakwikwi uye inotsamira muyero. Gene expression profiling yemasero akabatwa neLDC000067 yakaratidza kuderedzwa kwakasarudzika kwemamRNAs enguva pfupi, kusanganisira akakosha ekudzora kupararira uye apoptosis. Ongororo ye de novo RNA synthesis yakakurudzira basa rakasiyana-siyana rakanaka reCDK9. Payero yemamorekuru nemaserura, LDC000067 yakadzokorodza maitiro eCDK9 inhibition senge kukwidziridzwa kumbomira kweRNA polymerase II pamajini uye, zvakanyanya kukosha, kuiswa kweapoptosis mumasero egomarara. LDC000067 inhibits P-TEFb-inotsamira mu vitro transcription. Inoita kuti apoptosis in vitro uye mu vivo musanganiswa neBI 894999. |
| CPD100910 | SEL120-34A | SEL120-34A ine simba uye inosarudza CDK8 inhibitor inoshanda muAML maseru ane yakakwira serine phosphorylation yeSTAT1 uye STAT5 transactivation domains. EL120-34A inhibits phosphorylation yeSTAT1 S727 uye STAT5 S726 mumasero ekenza mu vitro. Sezvineiwo, kudzorwa kweSTATs- uye NUP98-HOXA9- inotsamira kunyorwa yakaonekwa seyakanyanya nzira yekuita mu vivo. |
| CPD100501 | UNC2541 | UNC2541 ine simba uye MerTK-specific inhibitor inoratidza sub-micromolar inhibitory chiitiko musero-based ELISA. Mukuwedzera, chimiro che X-ray cheprotein yeMerTK yakaoma ne11 yakagadziriswa kuratidza kuti macrocycles aya anosunga muhomwe yeMerTK ATP. UNC2541 yakaratidza IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| CPD100745 | RU-302 | RU-302 inoveli pan-tam inhibitor, ichivharira iyo interface pakati pe tam ig1 ectodomain uye gas6 lg domain, zvine simba inhibiting axl reporter cell mitsara uye yekuzvarwa tam receptors cancer cell mitsara. |
| CPD100744 | R916562 | |
| CPD100743 | Ningetinib-Tosylate | CT-053, inozivikanwawo seDE-120, inhibitor yeVEGF uye PDGF inogona kurapwa kwekunyorova kwakabatana nezera remacular degeneration. |
| CPD100742 | SGI-7079 | SGI-7079 ine simba uye inosarudza Axl inhibitor ine inogona kuita anticancer chiitiko. SGI-7079 yakanyatso kuvharidzira Axl activation pamberi peiyo exogenous Gas6 ligand. SGI-7079 inhibited bundu kukura mune dosi inotsamira nzira. Axl ndiyo inogona kurapa chinangwa chekukunda EGFR inhibitor kuramba. |
| CPD100741 | 2-D08 | 2-D08 iflavone yakagadzirwa inodzivirira sumoylation. 2-D08 yakaratidza anti-aggregatory uye neuroprotective effect |
| CPD100740 | Dubematinib | Dubermatinib, inozivikanwawo seTP-0903, ine simba uye inosarudza AXL inhibitor. TP-0903 induces apoptosis yakakura muCLL B masero ane LD50 kukosha kwenanomolar range. Musanganiswa weTP-0903 neBTK inhibitors inowedzera CLL B-cell apoptosis AXL overexpression inyaya inodzokororwa inocherechedzwa mumhando dzakawanda dzebundu dzakawana kuramba kune vakasiyana vamiririri. Kurapwa kwemaseru egomarara neTP-0903 kunodzosera mesenchymal phenotype mumamodhi akawanda uye kunosimudzira maseru egomarara kuti arapwe nevamwe vamiririri vakanangwa. Kutungamirirwa kweTP-0903 kungave semumiririri mumwe chete kana kusanganiswa neBTK inhibitors kunogona kushanda mukurapa varwere vane CLL. |
| CPD100739 | NPS-1034 | NPS-1034 ibhuku reMET inhibitor, iyo inhibita iyo yakagadziriswa MET receptor uye yayo inogadzirisa inoshanda shanduko. NPS-1034, inhibits akasiyana siyana anoshanda mutant mafomu eMET pamwe neHGF-activated wild-type MET. NPS-1034 yakadzivisa kuwanda kwemasero anoratidza yakabatidzwa MET uye akakurudzira kudzoreredzwa kwemamota akaumbwa kubva mumasero akadaro mune mbeva xenograft modhi kuburikidza neanti-angiogenic uye pro-apoptotic zviito. NPS-1034 zvakare yakavharira HGF-inosimudzira activation yeMET kusaina muhupo kana kusavapo kweserum. Zvinoshamisa, NPS-1034 yakavharira matatu MET akasiyana ayo anopokana neMET inhibitors SU11274, NVP-BVU972, uye PHA665752. |
| CPD100738 | Glesatinib | Glesatinib, inozivikanwawo seMGCD-265, ndeyemuromo bioavailable, diki-morekuru, multitargeted tyrosine kinase inhibitor ine inogona kuita antineoplastic chiitiko. MGCD265 inosunga uye inhibits phosphorylation yeakawanda receptor tyrosine kinases (RTKs), kusanganisira c-Met receptor (hepatocyte growth factor receptor); iyo Tek/Tie-2 receptor; vascular endothelial growth factor receptor (VEGFR) marudzi 1, 2, uye 3; uye macrophage-inokurudzira 1 receptor (MST1R kana RON). |
