| CAT # | Izina ryibicuruzwa | Ibisobanuro |
| CPD2809 | AMG-510 | AMG-510 nimbaraga zikomeye za KRAS G12C. AMG-510 ihitamo intego ya KRAS p.G12C ihinduka, haba kurwego rwa ADN, RNA cyangwa proteine, kandi ikabuza, binyuze muburyo butarasobanurwa neza, kwerekana na / cyangwa selile yibibyimba byerekana binyuze muri mutant ya KRAS p.G12C. Ibi birashobora kubuza gukura muri KRAS p.G12C-yerekana ibibyimba |
| CPD100230 | JBJ-04-125-02 R-isomer | |
| CPD102300 | S-55746 | |
| CPD101235 | diABZI STING agonist-1 trihydrochloride | diABZI STING agonist-1 (trihydrochloride) ni ikintu gitera imbaraga za interferon genes (STING) reseptor agonist, hamwe na EC50s ya 130, 186 nM kubantu nimbeba. |
| CPD101234 | diABZI STING agonist-1 (Tautomerism) | diABZI STING agonist-1 Tautomerism (compound 3) nikintu gitoranya gitera interferon genes (STING) reseptor agonist, hamwe na EC50s ya 130, 186 nM kubantu nimbeba. |
| CPD101233 | diABZI STING agonist-1 | diABZI STING agonist-1 ni ikintu gitera imbaraga za interferon genes (STING) reseptor agonist, hamwe na EC50s ya 130, 186 nM kubantu nimbeba. |
| CPD101232 | STING agonist-4 | STING agonist-4 ni moteri ya Interferon Genes (STING) reseptor agonist hamwe nikigaragara gihoraho (IC50) cya 20 nM. STING agonist-4 nuburyo bubiri bujyanye na amidobenzimidazole (ABZI) bushingiye ku guhuza ABZIs (diABZIs) hamwe no guhuza ibikorwa bya STING n'imikorere ya selile. |
| CPD101231 | STING agonist-3 | STING agonist-3, yakuwe muri patenti WO2017175147A1 (urugero 10), ni ihitamo kandi itari nucleotide nto-molekile ntoya ya STING agonist hamwe na pEC50 na pIC50 ya 7.5 na 9.5. STING agonist-3 ifite ingaruka zirambye zo kurwanya ibibyimba kandi ifite imbaraga nyinshi zo kunoza imiti ya kanseri |
| CPD100904 | Voruciclib | Voruciclib, izwi kandi nka P1446A-05, ni poroteyine ya kinase inhibitor yihariye ya kinase iterwa na kinase 4 (CDK4) ifite ibikorwa bya antineoplastique. CDK4 inhibitor P1446A-05 irabuza cyane cyane CDK4 yunganirwa na G1-S icyiciro cya kabiri, gufata amagare ya selile no kubuza gukura kwa kanseri. Serine / threonine kinase CDK4 iboneka murwego rufite D-G1 yo mu bwoko bwa G1 kandi niyo kinase ya mbere yatangiye gukora nyuma yo gukanguka kwa mitogenic, ikarekura ingirabuzimafatizo kuva mukanya gato ikagera kuri G1 / S. CDK-cyclin yerekanwe kuri fosifora yibintu byandikirwa retinoblastoma (Rb) mugitangiriro cya G1, ikuraho histone deacetylase (HDAC) no guhagarika gukandamizwa. |
| CPD100905 | Alvocidib | Alvocidib ni synthique N-methylpiperidinyl chlorophenyl flavone. Nkumwanya wa kinase iterwa na cyclin, alvocidib itera gufatwa kwingirangingo mu gukumira fosifora ya kinase iterwa na cyclin (CDKs) ndetse no kugabanya imvugo ya cyclin D1 na D3, bigatuma G1 itabwa muri yombi na apoptose. Iyi agent nayo irwanya irushanwa ryibikorwa bya adenosine triphosphate. Reba ibizamini bya clinique ikora cyangwa ibizamini bya clinique bifunze ukoresheje iyi agent. |
| CPD100906 | BS-181 | BS-181 ni CDK itoranya cyane ya CDK7 hamwe na IC (50) ya 21 nmol / L. Igeragezwa ryizindi CDK kimwe nizindi kinase 69 zerekanye ko BS-181 yabujije CDK2 gusa yibitekerezo biri munsi ya micromol / L, CDK2 ikabuzwa inshuro 35 imbaraga nke (IC (50) 880 nmol / L) kuruta CDK7. Muri selile MCF-7, BS-181 yabujije fosifora ya CDK7 insimburangingo, iteza imbere ifatwa ry’ingirabuzimafatizo na apoptose kugira ngo ibuze imikurire ya kanseri ya kanseri, kandi yerekana ingaruka za antitumor muri vivo. |
| CPD100907 | Riviciclib | Riviciclib, izwi kandi nka P276-00, ni flavone na cyclin biterwa na kinase (CDK) inhibitor hamwe nibikorwa bya antineoplastique. P276-00 guhitamo guhuza no kubuza Cdk4 / cyclin D1, Cdk1 / cyclin B na Cdk9 / cyclin T1, serine / threonine kinase igira uruhare runini mugutunganya ingirabuzimafatizo no gukwirakwiza selile. Kubuza izo kinase biganisha ku gufatwa kwingirangingo mugihe cyinzibacyuho ya G1 / S, bityo bigatuma habaho kwinjiza apoptose, no kubuza ikwirakwizwa rya selile. |
| CPD100908 | MC180295 | MC180295 ni CDK9 ihitamo cyane (IC50 = 5 nM). . |
| 1073485-20-7 | LDC000067 | LDC000067 ninzitizi ikomeye kandi itoranya CDK9. LDC000067 yabujijwe kwandukura vitro muburyo bwa ATP-irushanwa kandi ikabije. Imvugo yerekana imiterere ya selile zavuwe na LDC000067 yerekanaga igabanuka ryatoranijwe rya mRNAs zimara igihe gito, harimo nubugenzuzi bukomeye bwo gukwirakwiza na apoptose. Isesengura rya de novo RNA synthesis ryagaragaje uruhare runini rwa CDK9. Ku rwego rwa molekuline na selile, LDC000067 yerekanye ingaruka ziranga CDK9 nko guhagarika ihagarikwa rya RNA polymerase II kuri gen, cyane cyane, kwinjiza apoptose mungirangingo za kanseri. LDC000067 ibuza P-TEFb iterwa na transcription. Itera apoptose muri vitro no muri vivo ifatanije na BI 894999. |
| CPD100910 | SEL120-34A | SEL120-34A ninzitizi ikomeye kandi yatoranijwe ya CDK8 ikora muri selile ya AML ifite urwego rwo hejuru rwa fosifora ya serine ya STAT1 na STAT5 transactivation. EL120-34A ibuza fosifora ya STAT1 S727 na STAT5 S726 muri selile ya kanseri muri vitro. Mubisanzwe, amabwiriza ya STATs- na NUP98-HOXA9- kwandukura byaragaragaye nkuburyo bwiganje bwibikorwa muri vivo. |
| CPD100501 | UNC2541 | UNC2541 nigikoresho gikomeye kandi cyihariye cya MerTK cyerekana ibikorwa byo guhagarika sub-micromolar muri ELISA. Byongeye kandi, imiterere ya X-ray ya poroteyine ya MerTK muri complexe hamwe na 11 yiyemeje kwerekana ko izo macrocycle zihuza mu mufuka wa MerTK ATP. UNC2541 yerekanye IC50 MerTH = 4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| CPD100745 | RU-302 | RU-30. |
| CPD100744 | R916562 | |
| CPD100743 | Ningetinib-Tosylate | CT-053, izwi kandi nka DE-120, ni inhibitor ya VEGF na PDGF ishobora kuvura imiti iterwa n'imyaka. |
| CPD100742 | SGI-7079 | SGI-7079 ninzitizi ikomeye kandi ihitamo Axl inhibitor hamwe nibikorwa bishobora kurwanya antikanseri. SGI-7079 yabujije neza gukora Axl imbere ya ligand exogenous Gas6. SGI-7079 yabujije imikurire yikibyimba muburyo butandukanye. Axl ni intego yo kuvura yo gutsinda EGFR inhibitor. |
| CPD100741 | 2-D08 | 2-D08 ni flavone ya syntetique ibuza sumoylation. 2-D08 yerekanye ingaruka zo kurwanya igiteranyo na neuroprotective |
| CPD100740 | Dubermatinib | Dubermatinib, izwi kandi nka TP-0903, ni inhibitor ya AXL ikomeye kandi ihitamo. TP-0903 itera apoptose nini muri selile CLL B ifite LD50 indangagaciro za nanomolar. Guhuza TP-0903 hamwe na BTK inhibitor yongerera CLL B-selile apoptose AXL gukabya gukabije ni insanganyamatsiko yongeye kugaruka igaragara mubwoko butandukanye bwibibyimba byabonye kurwanya imiti itandukanye. Kuvura ingirangingo za kanseri hamwe na TP-0903 bihindura fenotype ya mesenchymal muburyo bwinshi kandi ikangurira kanseri kanseri kwivuza hamwe nibindi bikoresho bigamije. Ubuyobozi bwa TP-0903 haba nkumukozi umwe cyangwa bufatanije na BTK inhibitor irashobora kuba ingirakamaro mukuvura abarwayi bafite CLL. |
| CPD100739 | NPS-1034 | NPS-1034 nigitabo gishya cya MET inhibitor, kibuza MET reseptor ikora hamwe na mutant ikora. NPS-1034, irabuza uburyo butandukanye bwimikorere ya mutant ya MET kimwe na HGF ikora-ubwoko bwa MET. NPS-1034 yabujije ikwirakwizwa ry'utugingo ngengabuzima tugaragaza MET ikora kandi iteza imbere gusubira inyuma kw'ibibyimba biva muri selile nk'icyitegererezo cy'imbeba xenograft binyuze mu bikorwa byo kurwanya angiogenic na pro-apoptotic. NPS-1034 kandi yabujije HGF-iterwa no gukora MET yerekana ibimenyetso bya serumu ihari cyangwa idahari. Ikigaragara ni uko NPS-1034 yabujije ibintu bitatu MET irwanya MET inhibitor SU11274, NVP-BVU972, na PHA665752. |
| CPD100738 | Glesatinib | Glesatinib, izwi kandi ku izina rya MGCD-265, ni bioavailable yo mu kanwa, molekile nto, intego ya tyrosine kinase inhibitor hamwe nibikorwa bya antineoplastique. MGCD265 ihuza kandi ikabuza fosifora ya reseptor tyrosine kinase nyinshi (RTKs), harimo na c-Met reseptor (reseptor yo gukura kwa hepatocyte); reseptor ya Tek / Ikariso-2; imiyoboro y'amaraso ikura (VEGFR) ubwoko bwa 1, 2, na 3; na macrophage-itera 1 reseptor (MST1R cyangwa RON). |
