| Ologbo # | Orukọ ọja | Apejuwe |
| CPD2809 | AMG-510 | AMG-510 jẹ apaniyan covalent KRAS G12C ti o lagbara. AMG-510 yan ni ibi-afẹde KRAS p.G12C mutant, ni boya DNA, RNA tabi ipele amuaradagba, ati idilọwọ, nipasẹ ọna ti a ko ti ṣalaye, ikosile ti ati/tabi ifihan sẹẹli tumo nipasẹ iyipada KRAS p.G12C. Eyi le ṣe idiwọ idagbasoke ni KRAS p.G12C-fifihan awọn sẹẹli tumo |
| CPD100230 | JBJ-04-125-02 R-isomer | |
| CPD102300 | S-55746 | |
| CPD101235 | diABZI STING agonist-1 trihydrochloride | diABZI STING agonist-1 (trihydrochloride) jẹ apaniyan yiyan ti awọn jiini interferon (STING) agonist olugba, pẹlu EC50s ti 130, 186 nM fun eniyan ati asin, lẹsẹsẹ. |
| CPD101234 | diABZI STING agonist-1 (Tautomerism) | diABZI STING agonist-1 Tautomerism (compound 3) jẹ apaniyan yiyan ti awọn jiini interferon (STING) agonist olugba, pẹlu EC50s ti 130, 186 nM fun eniyan ati asin, lẹsẹsẹ. |
| CPD101233 | diABZI STING agonist-1 | diABZI STING agonist-1 jẹ oludaniloju yiyan ti awọn jiini interferon (STING) agonist olugba olugba, pẹlu EC50s ti 130, 186 nM fun eniyan ati asin, lẹsẹsẹ. |
| CPD101232 | OGUN STING-4 | STING agonist-4 jẹ ohun iwuri ti Interferon Genes (STING) agonist olugba ti o han gbangba inhibitory igbagbogbo (IC50) ti 20 nM. STING agonist-4 jẹ amidobenzimidazole (ABZI) ti o ni ibatan si ami-ara meji lati ṣẹda ABZI (diABZI) ti o ni asopọ pẹlu imudara imudara si STING ati iṣẹ cellular |
| CPD101231 | OGUN STING-3 | STING agonist-3, ti a fa jade lati itọsi WO2017175147A1 (apẹẹrẹ 10), jẹ yiyan ati ti kii-nucleotide kekere-moleku STING agonist pẹlu pEC50 ati pIC50 ti 7.5 ati 9.5, lẹsẹsẹ. STING agonist-3 ni ipa egboogi-tumor ti o tọ ati agbara nla lati ni ilọsiwaju itọju ti akàn |
| CPD100904 | Voruciclib | Voruciclib, ti a tun mọ ni P1446A-05, jẹ amuaradagba kinase inhibitor kan pato fun kinase ti o gbẹkẹle cyclin 4 (CDK4) pẹlu iṣẹ-ṣiṣe antineoplastic ti o pọju. CDK4 inhibitor P1446A-05 ni pato ṣe idiwọ CDK4-mediated G1-S alakoso iyipada, mimu gigun kẹkẹ sẹẹli ati idilọwọ idagbasoke sẹẹli alakan. Serine / threonine kinase CDK4 ni a ri ni eka kan pẹlu D-type G1 cycins ati ki o jẹ akọkọ kinase lati di mu ṣiṣẹ lori mitogenic fọwọkan, dasile awọn sẹẹli lati ipele quiescent sinu ipele gigun kẹkẹ G1 / S idagbasoke; Awọn eka CDK-cyclin ti han lati phosphorylate awọn retinoblastoma (Rb) ifosiwewe transcription ni kutukutu G1, nipo histone deacetylase (HDAC) ati idilọwọ ifasilẹ transcriptional. |
| CPD100905 | Alvocidib | Alvocidib jẹ agbo N-methylpiperidinyl chlorophenyl flavone sintetiki. Gẹgẹbi oludena ti kinase ti o gbẹkẹle cyclin, alvocidib nfa imudani ọmọ inu sẹẹli nipasẹ idilọwọ phosphorylation ti awọn kinases ti o gbẹkẹle cyclin (CDKs) ati nipasẹ ilana ilana cyclin D1 ati D3 ikosile, ti o mu ki G1 cell cycle arrest ati apoptosis. Aṣoju yii tun jẹ oludena ifigagbaga ti iṣẹ ṣiṣe triphosphate adenosine. Ṣayẹwo fun awọn idanwo ile-iwosan ti nṣiṣe lọwọ tabi awọn idanwo ile-iwosan pipade ni lilo aṣoju yii. |
| CPD100906 | BS-181 | BS-181 jẹ oludaniloju CDK ti o yan pupọ fun CDK7 pẹlu IC (50) ti 21 nmol/L. Idanwo awọn CDK miiran ati awọn kinases 69 miiran fihan pe BS-181 nikan ni idinamọ CDK2 ni awọn ifọkansi ti o kere ju 1 micromol/L, pẹlu CDK2 ni idinamọ 35-fold kere si agbara (IC(50) 880 nmol/L) ju CDK7. Ninu awọn sẹẹli MCF-7, BS-181 ṣe idiwọ phosphorylation ti awọn sobusitireti CDK7, igbega imudani ọmọ sẹẹli ati apoptosis lati ṣe idiwọ idagba awọn laini sẹẹli alakan, ati ṣafihan awọn ipa antitumor ni vivo. |
| CPD100907 | Riviciclib | Riviciclib, ti a tun mọ ni P276-00, jẹ oludena flavone ati cyclin ti o gbẹkẹle kinase (CDK) pẹlu iṣẹ-ṣiṣe antineoplastic ti o pọju. P276-00 yiyan sopọ si ati ki o ṣe idiwọ Cdk4/cyclin D1, Cdk1/cyclin B ati Cdk9/cyclin T1, serine/threonine kinases ti o ṣe awọn ipa pataki ninu ilana ilana sẹẹli sẹẹli ati afikun cellular. Idinamọ ti awọn kinases wọnyi nyorisi imuni ọmọ inu sẹẹli lakoko iyipada G1/S, nitorinaa yori si ifakalẹ ti apoptosis, ati idinamọ ti ilọsiwaju sẹẹli tumo. |
| CPD100908 | MC180295 | MC180295 jẹ onidalẹkun CDK9 yiyan pupọ (IC50 = 5 nM). (MC180295 ni iṣẹ ṣiṣe egboogi-akàn gbooro ni fitiro ati pe o munadoko ninu awọn awoṣe akàn vivo. Ni afikun, idinamọ CDK9 ṣe ifarabalẹ si inhibitor checkpoint ajẹsara α-PD-1 ni vivo, ti o jẹ ki o jẹ ibi-afẹde ti o dara julọ fun itọju ailera akàn ti akàn. |
| 1073485-20-7 | LDC000067 | LDC000067 jẹ oludena CDK9 ti o lagbara ati yiyan. LDC000067 ni idinamọ in vitro transcription ni ATP-idije ati ọna ti o gbẹkẹle iwọn lilo. Isọjade ikosile jiini ti awọn sẹẹli ti a tọju pẹlu LDC000067 ṣe afihan idinku yiyan ti awọn mRNAs igba diẹ, pẹlu awọn olutọsọna pataki ti afikun ati apoptosis. Itupalẹ ti iṣelọpọ de novo RNA daba ipa rere jakejado ti CDK9. Ni ipele molikula ati cellular, LDC000067 awọn ipa ẹda ti o jẹ ihuwasi ti idinamọ CDK9 gẹgẹbi imudara imudara ti RNA polymerase II lori awọn Jiini ati, pataki julọ, ifakalẹ ti apoptosis ninu awọn sẹẹli alakan. LDC000067 ṣe idiwọ P-TEFb-igbẹkẹle in vitro transcription. Ṣe agbejade apoptosis in vitro ati in vivo ni apapo pẹlu BI 894999. |
| CPD100910 | SEL120-34A | SEL120-34A jẹ oludaniloju CDK8 ti o lagbara ati yiyan ti nṣiṣe lọwọ ninu awọn sẹẹli AML pẹlu awọn ipele giga ti serine phosphorylation ti STAT1 ati awọn ibugbe transactivation STAT5. EL120-34A ṣe idiwọ phosphorylation ti STAT1 S727 ati STAT5 S726 ninu awọn sẹẹli alakan ni fitiro. Ni igbagbogbo, ilana ti STATs- ati NUP98-HOXA9-kikọsilẹ ti o gbẹkẹle ni a ti ṣakiyesi bi ilana iṣe ti o ga julọ ni vivo. |
| CPD100501 | UNC2541 | UNC2541 jẹ oludaniloju to lagbara ati MerTK-pato ti o ṣe afihan iṣẹ ṣiṣe inhibitory sub-micromolar ni ELISA ti o da lori sẹẹli. Ni afikun, ẹya X-ray ti amuaradagba MerTK ni eka pẹlu 11 ni ipinnu lati fihan pe awọn macrocycles wọnyi sopọ mọ apo MerTK ATP. UNC2541 ṣe afihan IC50 MerTH = 4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| CPD100745 | RU-302 | RU-302 jẹ inhibitor pan-tam aramada aramada, dina wiwo laarin tam ig1 ectodomain ati gas6 lg domain, ni agbara ni idiwọ awọn laini sẹẹli onirohin axl ati abinibi tam awọn olugba awọn laini sẹẹli alakan. |
| CPD100744 | R916562 | |
| CPD100743 | Ningetinib-Tosylate | CT-053, ti a tun mọ ni DE-120, jẹ VEGF ati inhibitor PDGF ti o ni agbara fun itọju ibajẹ macular degeneration ti ọjọ-ori tutu. |
| CPD100742 | SGI-7079 | SGI-7079 jẹ oludaniloju Axl ti o lagbara ati yiyan pẹlu iṣẹ ṣiṣe anticancer ti o pọju. SGI-7079 ṣe idiwọ imuṣiṣẹ Axl ni imunadoko ni iwaju ligand Gas6 exogenous. SGI-7079 ṣe idiwọ idagbasoke tumo ni ọna ti o gbẹkẹle iwọn lilo. Axl jẹ ibi-afẹde itọju ailera ti o pọju fun bibori resistance inhibitor EGFR. |
| CPD100741 | 2-D08 | 2-D08 jẹ flavone sintetiki ti o ṣe idiwọ sumoylation. 2-D08 ṣe afihan egboogi-alaropo ati ipa neuroprotective |
| CPD100740 | Dubermatinib | Dubermatinib, ti a tun mọ ni TP-0903, jẹ oludena AXL ti o lagbara ati yiyan. TP-0903 nfa apoptosis nla ni awọn sẹẹli CLL B pẹlu awọn iye LD50 ti awọn sakani nanomolar. Apapọ ti TP-0903 pẹlu awọn inhibitors BTK augments CLL B-cell apoptosis AXL overexpression jẹ koko-ọrọ ti nwaye ti a ṣe akiyesi ni awọn oriṣi tumọ pupọ ti o ti gba resistance si awọn aṣoju pupọ. Itoju ti awọn sẹẹli alakan pẹlu TP-0903 yiyipada phenotype mesenchymal ni awọn awoṣe pupọ ati ṣe akiyesi awọn sẹẹli alakan si itọju pẹlu awọn aṣoju ìfọkànsí miiran. Isakoso ti TP-0903 boya bi oluranlowo ẹyọkan tabi ni apapo pẹlu awọn inhibitors BTK le munadoko ninu atọju awọn alaisan pẹlu CLL. |
| CPD100739 | NPS-1034 | NPS-1034 jẹ onidalẹkun MET aramada, eyiti o ṣe idiwọ olugba MET ti a mu ṣiṣẹ ati awọn mutanti ti nṣiṣe lọwọ. NPS-1034, ṣe idiwọ ọpọlọpọ awọn fọọmu mutanti ti nṣiṣe lọwọ ti MET bakanna bi MET iru-igi ti a mu ṣiṣẹ HGF. NPS-1034 ṣe idiwọ itankale awọn sẹẹli ti n ṣalaye MET ti a mu ṣiṣẹ ati igbega ipadasẹhin ti awọn èèmọ ti a ṣẹda lati iru awọn sẹẹli ni awoṣe xenograft Asin nipasẹ awọn iṣe anti-angiogenic ati pro-apoptotic. NPS-1034 tun ṣe idiwọ imuṣiṣẹ imudara HGF ti ifihan MET ni iwaju tabi isansa ti omi ara. Ni pataki, NPS-1034 ṣe idiwọ awọn iyatọ MET mẹta ti o tako si awọn inhibitors MET SU11274, NVP-BVU972, ati PHA665752. |
| CPD100738 | Glesatinib | Glesatinib, ti a tun mọ ni MGCD-265, jẹ bioavailable ẹnu, kekere-moleku, inhibitor tyrosine kinase multitarrgeted pẹlu iṣẹ ṣiṣe antineoplastic ti o pọju. MGCD265 sopọ si ati ṣe idiwọ phosphorylation ti ọpọlọpọ awọn tyrosine kinases olugba (RTKs), pẹlu olugba c-Met (olugba ifosiwewe idagbasoke hepatocyte); olugba Tek / Tie-2; Awọn olutọpa idagbasoke idagbasoke ti iṣan ti iṣan (VEGFR) awọn iru 1, 2, ati 3; ati macrophage-safikun 1 olugba (MST1R tabi RON). |
