| PUSI # | Igoa Oloa | Fa'amatalaga |
| CPD2809 | AMG-510 | AMG-510 o se KRAS G12C covalent inhibitor malosi. AMG-510 filifili fa'atatau ile KRAS p.G12C mutant, i le DNA, RNA po'o le porotini, ma puipuia, e ala i se auala e le'i fa'amalamalamaina, fa'aaliga o ma/po'o le tumo fa'ailo e ala ile KRAS p.G12C mutant. E ono taofia ai le tupu a'e o le KRAS p.G12C-fa'aalia sela tumo |
| CPD100230 | JBJ-04-125-02 R-isomer | |
| CPD102300 | S-55746 | |
| CPD101235 | diABZI STING agonist-1 trihydrochloride | o le diABZI STING agonist-1 (trihydrochloride) o se faʻamalosi filifilia o kenera interferon (STING), faʻatasi ai ma EC50s o le 130, 186 nM mo le tagata ma le isumu. |
| CPD101234 | diABZI STING agonist-1 (Tautomerism) | diABZI STING agonist-1 Tautomerism (compound 3) o se mea e fa'aosofia ai le filifilia o genes interferon (STING) receptor agonist, fa'atasi ai ma EC50s o le 130, 186 nM mo tagata ma isumu. |
| CPD101233 | diABZI STING agonist-1 | o le diABZI STING agonist-1 o se fa'aoso fa'aoso filifilia o genes interferon (STING) receptor agonist, fa'atasi ai ma EC50s o le 130, 186 nM mo le tagata ma le isumu. |
| CPD101232 | STING agonist-4 | STING agonist-4 o se stimulator o Interferon Genes (STING) receptor agonist faʻatasi ai ma se faʻalavelave faʻafuaseʻi (IC50) o le 20 nM. STING agonist-4 o se lua fa'atusa fa'atatau amidobenzimidazole (ABZI) fa'avae fa'avae e fausia ai ABZIs feso'ota'i (diABZIs) fa'atasi ai ma le fa'aleleia atili o le fusifusia i le STING ma le telefoni feavea'i. |
| CPD101231 | STING agonist-3 | STING agonist-3, maua mai le pateni WO2017175147A1 (faʻataʻitaʻiga 10), o se faʻataʻitaʻiga STING agonist laiti ma le nucleotide faʻatasi ma le pEC50 ma le pIC50 o le 7.5 ma le 9.5, i le faasologa. O le STING agonist-3 e iai sona aafiaga umi e tetee atu ai i le pumo ma e tele lona malosi e faaleleia atili ai togafitiga o le kanesa |
| CPD100904 | Voruciclib | Voruciclib, lea e lauiloa foi o le P1446A-05, o se polotini kinase inhibitor faapitoa mo le cyclin-faalagolago kinase 4 (CDK4) ma gaioiga antineoplastic gafatia. O le CDK4 inhibitor P1446A-05 fa'apitoa e fa'alavelaveina le CDK4-mediated G1-S vaega suiga, pu'eina le uila uila ma fa'alavelaveina le tuputupu a'e o le kanesa. O le serine / threonine kinase CDK4 o loʻo maua i totonu o se faʻalavelave faʻatasi ma D-ituaiga G1 cyclins ma o le kinase muamua lea e faʻagaoioia ile mitogenic stimulation, tuʻuina atu sela mai se tulaga quiescent i le G1 / S tuputupu aʻe uila laasaga; CDK-cyclin complexes ua faʻaalia e phosphorylate le retinoblastoma (Rb) transcription factor i le amataga o le G1, faʻateʻaina le histone deacetylase (HDAC) ma poloka le faʻasaʻoina o tusitusiga. |
| CPD100905 | Alvocidib | Alvocidib o le N-methylpiperidinyl chlorophenyl flavone fa'afefiloi. I le avea ai o se inhibitor o le cyclin-dependent kinase, alvocidib faʻaosofia le puʻeina o le taamilosaga e ala i le puipuia o le phosphorylation o cyclin-dependent kinases (CDKs) ma e ala i le faʻatonutonuina o le cyclin D1 ma le D3 faʻamatalaga, e mafua ai le G1 cell cycle puʻeina ma apoptosis. O lenei sooupu o se faʻatauvaʻa faʻatauvaʻa o gaioiga adenosine triphosphate. Siaki mo faʻataʻitaʻiga faʻapitoa faʻataʻitaʻiga poʻo faʻataʻitaʻiga tapuni faʻataʻitaʻiga e faʻaaoga ai lenei sooupu. |
| CPD100906 | BS-181 | O le BS-181 ose CDK e sili ona filifilia mo le CDK7 ma le IC(50) o le 21 nmol/L. O suʻesuʻega o isi CDKs faʻapea foʻi ma isi 69 kinases na faʻaalia ai naʻo le BS-181 na te taofia le CDK2 i faʻamaʻi maualalo ifo i le 1 micromol / L, ma le CDK2 o loʻo taofia 35-faʻaitiitia le malosi (IC (50) 880 nmol / L) nai lo CDK7. I sela MCF-7, BS-181 taofia le phosphorylation o le CDK7 substrates, siitia le taamilosaga o le puʻeina ma apoptosis e taofia ai le tuputupu aʻe o laina sela o le kanesa, ma faʻaalia aʻafiaga antitumor i vivo. |
| CPD100907 | Riviciclib | Riviciclib, lea e lauiloa foi o le P276-00, o se flavone ma cyclin dependent kinase (CDK) inhibitor ma gaioiga antineoplastic gafatia. P276-00 filifili faʻatasi ma faʻalavelave Cdk4 / cyclin D1, Cdk1 / cyclin B ma Cdk9 / cyclin T1, serine / threonine kinases o loʻo taʻalo i matafaioi taua i le faatonutonuina o le taamilosaga o le cell ma le faʻalauteleina o le telefoni. O le faʻasaina o nei kinases e taʻitaʻia ai le puʻeina o le taamilosaga i le taimi o le suiga o le G1 / S, ma oʻo atu ai i le faʻaogaina o le apoptosis, ma le faʻalavelaveina o le faʻateleina o le tumo. |
| CPD100908 | MC180295 | MC180295 o se inhibitor CDK9 sili ona filifilia (IC50 = 5 nM). (MC180295 o loʻo i ai le lautele o le gaioiga o le kanesa i vitro ma e aoga i faʻataʻitaʻiga o le kanesa in vivo. E le gata i lea, o le CDK9 inhibition e faʻaalia ai le puipuia o le puipuiga o le α-PD-1 i vivo, ma avea ai ma taulaʻiga sili mo togafitiga epigenetic o le kanesa. |
| 1073485-20-7 | LDC000067 | LDC000067 ose malosi ma filifili CDK9 inhibitor. LDC000067 faʻasaina in vitro transcription i se ATP-faʻatauva ma faʻalagolago i fua. O faʻamatalaga faʻamatalaga faʻamatalaga o sela na togafitia i le LDC000067 na faʻaalia ai se faʻaitiitiga filifilia o mRNA pupuu, e aofia ai faʻatonuga taua o le faʻateleina ma apoptosis. O le su'esu'ega o le de novo RNA synthesis na fa'ailoa mai ai se tulaga lelei tele o le CDK9. I le molecular ma le cellular level, LDC000067 toe gaosia aafiaga uiga o le CDK9 inhibition e pei o le faʻaleleia o le taofi o le RNA polymerase II i genes ma, sili ona taua, faʻaosoina o apoptosis i sela o le kanesa. LDC000067 faʻalavelave P-TEFb-faʻalagolago i le faʻaliliuga in vitro. Fa'aoso apoptosis in vitro ma in vivo fa'atasi ma BI 894999. |
| CPD100910 | SEL120-34A | SEL120-34A o le malosi ma le filifilia CDK8 inhibitor o loʻo galue i sela AML ma maualuga maualuga o serine phosphorylation o STAT1 ma STAT5 transactivation domains. O le EL120-34A e taofia ai le phosphorylation o STAT1 S727 ma STAT5 S726 i sela o le kanesa in vitro. E le gata i lea, o tulafono faatonutonu o STATs- ma le NUP98-HOXA9-faʻalagolago transcription ua matauina o se faiga faʻapitoa o gaioiga i vivo. |
| CPD100501 | UNC2541 | O le UNC2541 o se inhibitor malosi ma le MerTK-faʻapitoa e faʻaalia ai le faʻaogaina o le sub-micromolar i le ELISA faʻavae. E le gata i lea, o le X-ray fausaga o le MerTK protein i le lavelave ma le 11 na faʻamautuina e faʻaalia ai o nei macrocycles e fusifusia i totonu o le MerTK ATP taga. UNC2541 fa'aalia IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| CPD100745 | RU-302 | O le RU-302 o se tala fou pan-tam inhibitors, polokaina le fesoʻotaʻiga i le va o le tam ig1 ectodomain ma le gas6 lg domain, faʻalavelave faʻafefe axl reporter laina sela ma tagata masani tam receptors laina sela sela. |
| CPD100744 | R916562 | |
| CPD100743 | Ningetinib-Tosylate | CT-053, lea e taʻua foi o DE-120, o se VEGF ma PDGF inhibitor e ono mafai ona togafitia ai le susu o le macular degeneration. |
| CPD100742 | SGI-7079 | SGI-7079 o se fa'atosina malosi ma filifili Axl fa'atasi ai ma gaioiga fa'amasani fa'amasani. O le SGI-7079 na faʻamalosia lelei le faʻamalosia o le Axl i le i ai o le gas6 ligand exogenous. SGI-7079 taofia le tuputupu aʻe o le tuma i se fua faʻalagolago. O le Axl o se faʻamoemoega faʻapitoa mo togafitiga mo le faʻatoʻilaloina o le tetee o le inhibitor EGFR. |
| CPD100741 | 2-D08 | 2-D08 o se flavone synthetic e taofia sumoylation. 2-D08 na faʻaalia ai le anti-aggregatory ma le neuroprotective effect |
| CPD100740 | Dubermatinib | Dubermatinib, lea e lauiloa foi o le TP-0903, o se faʻamalosi malosi ma le filifilia o le AXL. TP-0903 fa'aoso apoptosis tele i sela CLL B ma LD50 tau o laina nanomolar. O le tu'ufa'atasiga o le TP-0903 ma le BTK inhibitors fa'aopoopoina le CLL B-cell apoptosis AXL overexpression o se autu toe fa'afouina o lo'o matauina i le tele o ituaiga tumo lea na maua ai le tete'e atu i vaila'au eseese. Togafitiga o sela o le kanesa i le TP-0903 e fesuia'i ai le mesenchymal phenotype i le tele o fa'ata'ita'iga ma fa'alauiloa sela o le kanesa i togafitiga ma isi sui fa'atatau. Fa'atonuina o le TP-0903 pe o se sui e tasi pe fa'atasi ma BTK inhibitors e mafai ona aoga i le togafitia o tagata mama'i ma le CLL. |
| CPD100739 | NPS-1034 | O le NPS-1034 o se tala fou o le inhibitor MET, lea e taofia ai le faʻaogaina o le MET faʻaogaina ma ona mutants malosi. NPS-1034, fa'asalaina ituaiga mutant fa'atosina malosi o le MET fa'apea fo'i ma le HGF-fa'agaoioia ituaiga MET. O le NPS-1034 na faʻalavelaveina le faʻateleina o sela e faʻaalia ai le MET faʻagaoioia ma faʻamalosia le toe faʻafoʻisia o tumo na faia mai ia sela i se faʻataʻitaʻiga xenograft kiore e ala i gaioiga anti-angiogenic ma pro-apoptotic. NPS-1034 na faʻalavelaveina foi le faʻamalosia o le HGF o le MET faʻailoga i le i ai poʻo le leai o se serum. O le mea moni, o le NPS-1034 na faʻalavelaveina ni suiga MET e tolu e tetee atu i le MET inhibitors SU11274, NVP-BVU972, ma le PHA665752. |
| CPD100738 | Glesatinib | Glesatinib, e ta'ua fo'i o le MGCD-265, ose fa'ato'aga fa'atosina o le tyrosine kinase e mafai ona tu'u tautala, e mafai ona maua i le gutu, ma le fa'aogaina o le tyrosine kinase. O le MGCD265 e fusifusia ma taofia le phosphorylation o le tele o le receptor tyrosine kinases (RTKs), e aofia ai le c-Met receptor (hepatocyte growth factor receptor); le Tek/Tie-2 talitali; vascular endothelial growth factor receptor (VEGFR) ituaiga 1, 2, ma le 3; ma le macrophage-stimulating 1 receptor (MST1R poʻo le RON). |
