| CAT # | Khoom npe | Kev piav qhia |
| PEB 2809 | AMG-510 | AMG-510 yog KRAS G12C covalent inhibitor muaj zog. AMG-510 xaiv lub hom phiaj ntawm KRAS p.G12C mutant, ntawm DNA, RNA lossis qib protein, thiab tiv thaiv, los ntawm qhov tseem tsis tau piav qhia, kev qhia ntawm thiab / lossis qog cell signaling los ntawm KRAS p.G12C mutant. Qhov no tuaj yeem cuam tshuam kev loj hlob hauv KRAS p.G12C-expressing qog hlwb |
| PIB 100230 | JBJ-04-125-02 R-isomer | |
| PIB 102300 | S-55746 | |
| PIB 101235 | DiABZI STING agonist-1 trihydrochloride | diABZI STING agonist-1 (trihydrochloride) yog ib qho kev xaiv stimulator ntawm interferon genes (STING) receptor agonist, nrog EC50s ntawm 130, 186 nM rau tib neeg thiab nas, feem. |
| PIB 101234 | DiABZI STING agonist-1 (Tautomerism) | diABZI STING agonist-1 Tautomerism (compound 3) yog ib qho kev xaiv stimulator ntawm interferon genes (STING) receptor agonist, nrog EC50s ntawm 130, 186 nM rau tib neeg thiab nas, feem. |
| PIB 101233 | DABZI STING agonist-1 | diABZI STING agonist-1 yog ib qho kev xaiv stimulator ntawm interferon genes (STING) receptor agonist, nrog EC50s ntawm 130, 186 nM rau tib neeg thiab nas, feem. |
| PIB 101232 | STING agonist-4 | STING agonist-4 yog ib qho stimulator ntawm Interferon Genes (STING) receptor agonist nrog qhov pom tseeb inhibitory tas li (IC50) ntawm 20 nM. STING agonist-4 yog ob qhov sib xyaw ua ke ntawm amidobenzimidazole (ABZI)-raws li kev sib txuas los tsim kev sib txuas ABZIs (diABZIs) nrog txhim kho kev khi rau STING thiab cellular muaj nuj nqi |
| PIB 101231 | STING agonist-3 | STING agonist-3, muab rho tawm los ntawm patent WO2017175147A1 (piv txwv 10), yog ib qho kev xaiv thiab tsis yog nucleotide me-molecule STING agonist nrog pEC50 thiab pIC50 ntawm 7.5 thiab 9.5, raws li. STING agonist-3 muaj zog tiv thaiv qog noj ntshav thiab muaj peev xwm ua tau zoo los txhim kho kev kho mob qog noj ntshav |
| PIB 100904 | Voruciclib | Voruciclib, tseem hu ua P1446A-05, yog ib qho protein kinase inhibitor tshwj xeeb rau cyclin-dependent kinase 4 (CDK4) uas muaj peev xwm ua haujlwm antineoplastic. CDK4 inhibitor P1446A-05 tshwj xeeb inhibits CDK4-mediated G1-S theem hloov pauv, ntes cell cycling thiab inhibiting mob qog noj ntshav. Lub serine / threonine kinase CDK4 muaj nyob rau hauv ib qho nyuaj nrog D-hom G1 cyclins thiab yog thawj kinase los ua kom tau raws li mitogenic stimulation, tso hlwb los ntawm ib tug quiescent theem mus rau lub G1 / S loj hlob cycling theem; CDK-cyclin complexes tau pom tias phosphorylate lub retinoblastoma (Rb) transcription factor nyob rau hauv thaum ntxov G1, displacing histone deacetylase (HDAC) thiab thaiv transcriptional repression. |
| PIB 100905 | Alvocidib | Alvocidib yog ib qho hluavtaws N-methylpiperidinyl chlorophenyl flavone compound. Raws li tus inhibitor ntawm cyclin-dependent kinase, alvocidib induces cell voj voog ntes los ntawm kev tiv thaiv phosphorylation ntawm cyclin-dependent kinases (CDKs) thiab los ntawm down-regulating cyclin D1 thiab D3 qhia, ua rau G1 cell voj voog ntes thiab apoptosis. Tus neeg sawv cev no kuj yog ib qho kev sib tw inhibitor ntawm adenosine triphosphate kev ua haujlwm. Tshawb xyuas cov kev sim tshuaj kho mob lossis kaw qhov kev sim tshuaj uas siv tus neeg sawv cev no. |
| PIB 100906 | IB-181 | BS-181 yog ib qho kev xaiv CDK inhibitor rau CDK7 nrog IC (50) ntawm 21 nmol / L. Kev ntsuam xyuas ntawm lwm cov CDKs thiab lwm yam 69 kinases pom tau tias BS-181 tsuas yog inhibited CDK2 ntawm cov concentrations qis dua 1 micromol/L, nrog CDK2 raug inhibited 35-fold tsawg zog (IC(50) 880 nmol/L) dua CDK7. Hauv MCF-7 hlwb, BS-181 inhibited phosphorylation ntawm CDK7 substrates, txhawb nqa lub voj voog ntawm tes thiab apoptosis txhawm rau tiv thaiv kev loj hlob ntawm cov kab mob qog noj ntshav, thiab pom cov teebmeem antitumor hauv vivo. |
| PAB 100907 | Riviciclib | Riviciclib, tseem hu ua P276-00, yog ib qho flavone thiab cyclin dependent kinase (CDK) inhibitor uas muaj peev xwm ua haujlwm antineoplastic. P276-00 xaiv khi rau thiab inhibits Cdk4/cyclin D1, Cdk1/cyclin B thiab Cdk9/cyclin T1, serine/threonine kinases uas ua lub luag haujlwm tseem ceeb hauv kev tswj ntawm lub voj voog ntawm tes thiab kev loj hlob ntawm tes. Inhibition ntawm cov kinases ua rau lub voj voog ntawm tes raug ntes thaum lub sij hawm hloov G1 / S, yog li ua rau induction ntawm apoptosis, thiab inhibition ntawm qog cell proliferation. |
| PIB 100908 | TIAB SA 180295 | MC180295 yog ib qho kev xaiv CDK9 inhibitor (IC50 = 5 nM). (MC180295 muaj kev tiv thaiv kabmob kheesxaws hauv vitro thiab muaj txiaj ntsig zoo hauv vivo cov qauv mob qog noj ntshav. Tsis tas li ntawd, CDK9 inhibition sensitizes rau lub cev tiv thaiv kab mob inhibitor α-PD-1 hauv vivo, ua rau nws lub hom phiaj zoo rau kev kho mob qog noj ntshav. |
| 1073485-20-7 | LDC000067 | LDC000067 yog ib qho muaj zog thiab xaiv CDK9 inhibitor. LDC000067 inhibited hauv vitro transcription nyob rau hauv ATP-kev sib tw thiab koob tshuaj-raws li. Gene qhia profileing ntawm cov hlwb kho nrog LDC000067 pom tau tias txo qis ntawm mRNAs luv luv, suav nrog cov tswj hwm tseem ceeb ntawm kev loj hlob thiab apoptosis. Kev tshuaj xyuas ntawm de novo RNA synthesis qhia txog lub luag haujlwm zoo ntawm CDK9. Ntawm qib molecular thiab cellular, LDC000067 rov tsim cov yam ntxwv ntawm CDK9 inhibition xws li txhim kho kev ncua ntawm RNA polymerase II ntawm cov noob thiab, qhov tseem ceeb tshaj, induction ntawm apoptosis hauv cov qog nqaij hlav cancer. LDC000067 inhibits P-TEFb-nyob rau hauv vitro transcription. Induces apoptosis hauv vitro thiab hauv vivo ua ke nrog BI 894999. |
| PIB 100910 | SEL120-34A | SEL120-34A yog lub zog thiab xaiv CDK8 inhibitor nquag ua haujlwm hauv AML hlwb nrog qib siab ntawm serine phosphorylation ntawm STAT1 thiab STAT5 transactivation domains. EL120-34A inhibits phosphorylation ntawm STAT1 S727 thiab STAT5 S726 hauv cov qog nqaij hlav hauv vitro. Raws li txoj cai, kev tswj hwm ntawm STATs- thiab NUP98-HOXA9- nyob ntawm qhov kev hloov pauv tau raug pom tias yog qhov tseem ceeb ntawm kev ua haujlwm hauv vivo. |
| PIB 100501 | UNC2541 | UNC2541 yog ib qho muaj zog thiab MerTK tshwj xeeb inhibitor uas nthuav tawm cov kev ua haujlwm ntawm cov micromolar inhibitory hauv cell-based ELISA. Tsis tas li ntawd, X-ray qauv ntawm MerTK protein nyob rau hauv complex nrog 11 tau txiav txim siab los qhia tias cov macrocycles khi hauv MerTK ATP hnab ris. UNC2541 qhia IC50 MerTH = 4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| PIB 100745 | UA-302 | RU-302 yog ib qho tshiab pan-tam inhibitor, thaiv qhov sib cuam tshuam ntawm tam ig1 ectodomain thiab gas6 lg domain, muaj zog inhibiting axl reporter cell kab thiab haiv neeg tam receptors kab mob qog noj ntshav. |
| PIB 100744 | r91656 2 | |
| PIB 100743 | Ningetinib-Tosylate | CT-053, tseem hu ua DE-120, yog VEGF thiab PDGF inhibitor muaj peev xwm los kho cov hnub nyoog ntub dej ntsig txog macular degeneration. |
| PIB 100742 | TSI-7079 | SGI-7079 yog ib qho muaj zog thiab xaiv Axl inhibitor uas muaj peev xwm tiv thaiv qog noj ntshav. SGI-7079 zoo inhibited Axl activation nyob rau hauv lub xub ntiag ntawm exogenous Gas6 ligand. SGI-7079 inhibited qog loj hlob nyob rau hauv ib koob tshuaj raws li. Axl yog lub hom phiaj kho mob rau kev kov yeej EGFR inhibitor tsis kam. |
| PIB 100741 | 2-D 08 | 2-D08 yog ib qho hluavtaws flavone uas inhibits suoylation. 2-D08 tau pom tias muaj cov nyhuv anti-aggregatory thiab neuroprotective |
| PIB 100740 | Dubermatinib | Dubermatinib, tseem hu ua TP-0903, yog lub zog thiab xaiv AXL inhibitor. TP-0903 induces loj apoptosis hauv CLL B hlwb nrog LD50 qhov tseem ceeb ntawm nanomolar ranges. Kev sib xyaw ntawm TP-0903 nrog BTK inhibitors augments CLL B-cell apoptosis AXL overexpression yog lub ntsiab lus rov tshwm sim pom nyob rau hauv ntau hom qog uas tau txais kev tiv thaiv rau ntau tus neeg ua haujlwm. Kev kho mob qog noj ntshav nrog TP-0903 thim rov qab cov tshuaj mesenchymal phenotype hauv ntau cov qauv thiab ua rau mob qog noj ntshav rau kev kho mob nrog rau lwm cov tshuaj tiv thaiv. Kev tswj hwm ntawm TP-0903 yog ib tus neeg sawv cev lossis ua ke nrog BTK inhibitors tuaj yeem ua tau zoo hauv kev kho cov neeg mob nrog CLL. |
| PAB 100739 | NPE-1034 | NPS-1034 yog ib qho tshiab MET inhibitor, uas inhibits MET receptor activated thiab nws constitutively active mutants. NPS-1034, inhibits ntau yam kev hloov pauv hloov pauv ntawm MET nrog rau HGF-activated wild-type MET. NPS-1034 inhibited qhov kev loj hlob ntawm cov hlwb uas nthuav tawm MET thiab txhawb kev rov ua haujlwm ntawm cov qog tsim los ntawm cov hlwb hauv cov qauv nas xenograft los ntawm kev ua haujlwm anti-angiogenic thiab pro-apoptotic. NPS-1034 kuj inhibited HGF-stimulated activation ntawm MET signaling nyob rau hauv lub xub ntiag los yog tsis muaj ntshav. Qhov tseem ceeb, NPS-1034 inhibited peb MET variants uas tiv taus MET inhibitors SU11274, NVP-BVU972, thiab PHA665752. |
| PAB 100738 | Glesatinib | Glesatinib, tseem hu ua MGCD-265, yog ib qho kev hais lus bioavailable, me me-molecule, multitargeted tyrosine kinase inhibitor uas muaj peev xwm ua haujlwm antineoplastic. MGCD265 khi rau thiab inhibits phosphorylation ntawm ob peb receptor tyrosine kinases (RTKs), nrog rau cov c-Met receptor (hepatocyte loj hlob receptor receptor); Tek/Tie-2 receptor; vascular endothelial growth factor receptor (VEGFR) hom 1, 2, thiab 3; thiab macrophage-stimulating 1 receptor (MST1R lossis RON). |
