| CAT # | Ingoa Hua | Whakaahuatanga |
| CPD2809 | AMG-510 | Ko te AMG-510 he kaha kaha KRAS G12C aukati. Ko te AMG-510 e whai ana i te KRAS p.G12C mutant, i te DNA, RNA, i te taumata pūmua ranei, me te aukati, na roto i te ahua kaore ano kia whakamaramatia, te whakaputanga o te tohu me te / ranei te tohu pūtau puku ma te KRAS p.G12C mutant. Ma tenei ka aukati i te tipu o te KRAS p.G12C-whakaputa i nga pūtau puku |
| CPD100230 | JBJ-04-125-02 R-isomer | |
| CPD102300 | S-55746 | |
| CPD101235 | diABZI STING agonist-1 trihydrochloride | Ko te diABZI STING agonist-1 (trihydrochloride) he kaiwhakatairanga whiriwhiri o nga ira interferon (STING) kaiwhakawhiwhi agonist, me nga EC50 o 130, 186 nM mo te tangata me te kiore, ia. |
| CPD101234 | diABZI STING agonist-1 (Tautomerism) | diABZI STING agonist-1 Tautomerism (compound 3) is a selective stimulator of interferon genes (STING) receptor agonist, with EC50s of 130, 186 nM mo te tangata me te kiore, ia. |
| CPD101233 | diABZI STING agonist-1 | Ko te diABZI STING agonist-1 he kaiwhakatairanga maataki o nga ira interferon (STING) kaiawhina agonist, me nga EC50 o 130, 186 nM mo te tangata me te kiore. |
| CPD101232 | STING agonist-4 | Ko te STING agonist-4 he kaiwhakatairanga o te Interferon Genes (STING) agonist kaiawhina me te kaha aukati (IC50) o te 20 nM. Ko te STING agonist-4 he pūhui hangarite e rua-a-amidobenzimidazole (ABZI) hei hanga i nga ABZI hono (diABZI) me te pai ake o te here ki te STING me te mahi pūkoro. |
| CPD101231 | STING agonist-3 | Ko te STING agonist-3, he mea tango mai i te patent WO2017175147A1 (tauira 10), he agonist STING iti-mucleotide iti me te pEC50 me te pIC50 o te 7.5 me te 9.5, ia. Ko te STING agonist-3 he awenga aukati-puku mauroa me te kaha nui ki te whakapai ake i te maimoatanga o te mate pukupuku |
| CPD100904 | Voruciclib | Ko Voruciclib, e mohiotia ana ko P1446A-05, he aukati kinase pūmua mo te kinase 4 (CDK4) e whakawhirinaki ana ki te cyclin me te mahi antineoplastic pea. Ko te aukati CDK4 P1446A-05 ka aukati i te whakawhitinga o te wahanga G1-S e CDK4-takawaenga, te hopu i te eke pahikara me te aukati i te tipu o te mate pukupuku. Ko te serine/threonine kinase CDK4 ka kitea i roto i te matatini me nga momo D-momo paihikara G1, a ko te kinase tuatahi ki te whakahohe i runga i te whakaihiihi mitogenic, te tuku i nga pūtau mai i te ata noho ki roto i te wahanga paihikara tipu G1/S; Kua whakaatuhia nga matatini CDK-cyclin ki te phosphorylate te retinoblastoma (Rb) tauwehe whakamaoritanga i te timatanga o te G1, te whakakore i te histone deacetylase (HDAC) me te aukati i te aukati tuhinga. |
| CPD100905 | Alvocidib | Ko Alvocidib he pūhui N-methylpiperidinyl chlorophenyl flavone. Hei aukati i te kinase cyclin-dependent, ka whakaawehia e alvocidib te hopu huringa pūtau ma te aukati i te phosphorylation o nga kinases cyclin-dependent (CDKs) me te whakaheke i te cyclin D1 me te D3, ka hua te hopukina huringa pūtau G1 me te apoptosis. Ko tenei kaihoko he kaiwhakataetae whakataetae mo te mahi adenosine triphosphate. Tirohia mo nga whakamatautau haumanu kaha, nga whakamatautau haumanu kati ranei ma te whakamahi i tenei kaihoko. |
| CPD100906 | BS-181 | Ko te BS-181 he aukati CDK tino whiriwhiri mo te CDK7 me te IC(50) o 21 nmol/L. Ko te whakamatautau i etahi atu CDK tae atu ki etahi atu 69 kinases i whakaatu ko te BS-181 anake te whakakore i te CDK2 i nga kohinga iti iho i te 1 micromol/L, me te CDK2 e aukati ana i te 35-fold iti ake te kaha (IC(50) 880 nmol/L) i te CDK7. I roto i nga pūtau MCF-7, ka aukati te BS-181 i te phosphorylation o nga taputapu CDK7, i whakatairanga i te hopu huringa pūtau me te apoptosis ki te aukati i te tipu o nga raina pūtau mate pukupuku, me te whakaatu i nga paanga antitumor i roto i te vivo. |
| CPD100907 | Riviciclib | Ko Riviciclib, e mohiotia ana ko P276-00, he flavone me te cyclin dependent kinase (CDK) aukati me te mahi antineoplastic pea. Ko te P276-00 ka herea, ka aukati i te Cdk4/cyclin D1, Cdk1/cyclin B me Cdk9/cyclin T1, serine/threonine kinases e whai waahi nui ana ki te whakahaere i te huringa o te pūtau me te whakatipu pūtau. Ko te whakakore i enei kinases ka arahi ki te hopu i te huringa pūtau i te wa o te whakawhitinga G1 / S, na reira ka arahina ki te whakauru o te apoptosis, me te aukati i te tipu o te pukupuku pukupuku. |
| CPD100908 | MC180295 | Ko te MC180295 he kaitautoko CDK9 tino whiriwhiri (IC50 = 5 nM). (MC180295 he mahi aukati-mate pukupuku i roto i te vitro me te whai hua i roto i nga tauira mate pukupuku in vivo. Hei taapiri, ko te aukati CDK9 e whakamohio ana ki te aukati α-PD-1 i roto i te vivo, ka waiho hei kaupapa pai mo te rongoa epigenetic o te mate pukupuku. |
| 1073485-20-7 | LDC000067 | Ko te LDC000067 he aukati CDK9 kaha me te whiriwhiri. Ko te LDC000067 i aukati i roto i te tuhi in vitro i roto i te ATP-whakataetae me te horopeta-whakawhirinaki. Ko te whakaaturanga whakaaturanga ira o nga pūtau i rongoahia ki te LDC000067 i whakaatu i te whakahekenga o nga mRNA poto poto, tae atu ki nga kaiwhakahaere nui o te tipu me te apoptosis. Ko te tātaritanga o te de novo RNA synthesis i kii i te whānuitanga pai o te CDK9. I te taumata ngota me te taumata pūtau, ka whakaputahia e LDC000067 nga ahuatanga o te aukati CDK9 penei i te whakaroa ake o te RNA polymerase II i runga i nga ira, me te mea nui, te whakaurunga o te apoptosis i roto i nga pūtau mate pukupuku. Ko te LDC000067 te aukati i te P-TEFb-whakawhirinaki i roto i te tuhinga in vitro. Ka whakakorikori i te apoptosis in vitro me in vivo me te BI 894999. |
| CPD100910 | SEL120-34A | Ko te SEL120-34A he kaiwawao CDK8 kaha me te whiriwhiri i roto i nga kamera AML me nga taumata teitei o te phosphorylation serine o nga rohe whakawhiti STAT1 me STAT5. Ko te EL120-34A ka whakakore i te phosphorylation o STAT1 S727 me STAT5 S726 i roto i nga pukupuku pukupuku i roto i te vitro. I nga wa katoa, kua kitea nga whakaritenga o nga tuhinga e whakawhirinaki ana ki te STATs- me te NUP98-HOXA9-he tikanga nui o te mahi i roto i te vivo. |
| CPD100501 | UNC2541 | Ko te UNC2541 he kaiwawao kaha me te MerTK-motuhake e whakaatu ana i nga mahi aukati iti-micromolar i roto i te ELISA e pa ana ki te pūtau. I tua atu, he hanga X-ray o te pūmua MerTK i roto i te matatini me te 11 i whakatauhia hei whakaatu ka herea enei macrocycles i roto i te putea MerTK ATP. I whakaatu a UNC2541 i te IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| CPD100745 | RU-302 | Ko te RU-302 he kaitao pan-tam hou, e aukati ana i te atanga i waenga i te tam ig1 ectodomain me te rohe gas6 lg, he kaha te aukati i nga raina axl kairipoata me nga kaiwhakawhiwhi tam taketake nga raina pūtau mate pukupuku. |
| CPD100744 | R916562 | |
| CPD100743 | Ningetinib-Tosylate | Ko te CT-053, e mohiotia ana ko DE-120, he aukati VEGF me te PDGF pea mo te maimoatanga o te whakahekenga o te maaka e pa ana ki te tau. |
| CPD100742 | SGI-7079 | Ko te SGI-7079 he aukati Axl kaha me te whiriwhiri me te mahi anticancer pea. Ko te SGI-7079 i kaha te aukati i te whakahohenga a Axl i te aroaro o te herenga Gas6 o waho. Ko te SGI-7079 i aukati i te tipu o te puku i runga i te tikanga o te horopeta. Ko te Axl he kaupapa rongoa mo te aukati i te aukati aukati EGFR. |
| CPD100741 | 2-D08 | Ko te 2-D08 he flavone waihanga e aukati ana i te whakahiatotanga. I whakaatu a 2-D08 i te hua anti-agregatory me te neuroprotective |
| CPD100740 | Dubermatinib | Ko Dubermatinib, e mohiotia ana ko TP-0903, he kaha me te whiriwhiri i te aukati AXL. Ko te TP-0903 e whakaawe ana i te apoptosis nui i roto i nga ruma CLL B me nga uara LD50 o nga awhe nanomolar. Ko te whakakotahitanga o te TP-0903 me te aukati BTK hei whakanui ake i te CLL B-cell apoptosis AXL overexpression he kaupapa hou ka kitea i roto i nga momo pukupuku maha kua mau i te aukati ki nga momo apiha. Ko te maimoatanga o nga pūtau mate pukupuku me te TP-0903 ka huri i te tohu tohu mesenchymal i roto i nga tauira maha, me te whakamohio i nga pūtau mate pukupuku ki te maimoatanga me etahi atu matū kua tohua. Ko te whakahaeretanga o te TP-0903 hei kaihoko kotahi, ma te whakakotahi ranei me nga aukati BTK ka whai hua ki te rongoa i nga turoro whai CLL. |
| CPD100739 | NPS-1034 | Ko te NPS-1034 he aukati MET hou, e aukati ana i te kaiwhakawhiwhi MET kua whakahohehia me ona mutants kaha. NPS-1034, ka aukati i nga momo mutant kaha kaha o te MET tae atu ki te MET momo mohoao kua whakahohehia e te HGF. Ko te NPS-1034 i aukati i te tipu o nga pūtau e whakaatu ana i te MET kua whakahohehia, me te whakatairanga i te whakahekenga o nga pukupuku i puta mai i aua pūtau i roto i te tauira xenograft kiore na roto i nga mahi anti-angiogenic me te pro-apoptotic. Ko te NPS-1034 hoki i aukati i te whakahoahoatanga o te HGF-whakaongaonga o te tohu MET i te aroaro o te kore ranei o te serum. Ko te mea nui, ko te NPS-1034 i aukati i nga momo MET e toru e aukati ana ki nga aukati MET SU11274, NVP-BVU972, me PHA665752. |
| CPD100738 | Glesatinib | Ko te Glesatinib, e mohiotia ana ko MGCD-265, he kaiao-a-waha, he iti-ngota ngota, he aukati tyrosine kinase multitargeted me te mahi antineoplastic pea. Ko te MGCD265 te here me te aukati i te phosphorylation o te maha o nga kinases tyrosine (RTKs), tae atu ki te c-Met receptor (hepatocyte growth factor receptor); te Tek/Tie-2 receptor; vascular endothelial growth factor receptor (VEGFR) momo 1, 2, me te 3; me te kaiwhiwhi 1 whakaihiihi macrophage (MST1R, RON ranei). |
