| CAT # | Inoa Huahana | wehewehe |
| CPD2809 | AMG-510 | ʻO AMG-510 kahi mea hoʻopiʻi covalent KRAS G12C. AMG-510 koho koho i ka KRAS p.G12C mutant, ma ka DNA, RNA a me ka protein pae, a pale, ma o ka e like me ka mea i ole elucidated ano, hoike o a/a tumor cell hoailona ma o ka KRAS p.G12C mutant. Hiki paha i kēia ke keʻakeʻa i ka ulu ʻana o KRAS p.G12C-expressing tumor cells |
| CPD100230 | JBJ-04-125-02 R-isomer | |
| CPD102300 | S-55746 | |
| CPD101235 | diABZI STING agonist-1 trihydrochloride | ʻO diABZI STING agonist-1 (trihydrochloride) he mea hoʻoulu koho o nā genes interferon (STING) receptor agonist, me nā EC50 o 130, 186 nM no ke kanaka a me ka ʻiole, kēlā me kēia. |
| CPD101234 | diABZI STING agonist-1 (Tautomerism) | ʻO diABZI STING agonist-1 Tautomerism (compound 3) he mea hoʻoulu koho o nā genes interferon (STING) receptor agonist, me nā EC50 o 130, 186 nM no ke kanaka a me ka ʻiole, kēlā me kēia. |
| CPD101233 | diABZI STING agonist-1 | ʻO diABZI STING agonist-1 kahi mea hoʻoulu koho o nā genes interferon (STING) receptor agonist, me EC50s o 130, 186 nM no ke kanaka a me ka ʻiole, kēlā me kēia. |
| CPD101232 | STING agonist-4 | ʻO STING agonist-4 kahi mea hoʻoulu i ka Interferon Genes (STING) receptor agonist me kahi mea paʻa paʻa (IC50) o 20 nM. ʻO ka STING agonist-4 kahi pūhui amidobenzimidazole (ABZI) pili pili like ʻelua e hana i nā ABZI i hoʻopili ʻia (diABZIs) me ka hoʻonui ʻia ʻana o ka hoʻopaʻa ʻana iā STING a me ka hana kelepona. |
| CPD101231 | STING agonist-3 | ʻO STING agonist-3, i unuhi ʻia mai ka patent WO2017175147A1 (laʻana 10), he mea koho a me ka non-nucleotide liʻiliʻi STING agonist me ka pEC50 a me ka pIC50 o 7.5 a me 9.5. Loaʻa i ka STING agonist-3 ka hopena anti-tumor lōʻihi a hiki ke hoʻomaikaʻi i ka mālama ʻana i ka maʻi kanesa |
| CPD100904 | Voruciclib | ʻO Voruciclib, ka mea i ʻike ʻia ʻo P1446A-05, he mea pale kinase kinase kikoʻī no ka cyclin-dependent kinase 4 (CDK4) me ka hana antineoplastic. Kāohi ʻia ka CDK4 inhibitor P1446A-05 i ka CDK4-mediated G1-S phase transition, ka hopu ʻana i ke kaʻa kaʻa a me ka pale ʻana i ka ulu ʻana o ka maʻi kanesa. Loaʻa ka serine/threonine kinase CDK4 i loko o kahi paʻakikī me D-type G1 cyclins a ʻo ia ka kinase mua i hoʻāla ʻia ma luna o ka hoʻoulu ʻana i ka mitogenic, e hoʻokuʻu ana i nā cell mai kahi pae kuʻi i ka pae kaʻa kaʻa ulu G1 / S; Ua hōʻike ʻia nā paʻakikī CDK-cyclin i ka phosphorylate i ka retinoblastoma (Rb) transcription factor i ka G1 mua, ka hoʻoneʻe ʻana i ka histone deacetylase (HDAC) a me ka pale ʻana i ka repression transcriptional. |
| CPD100905 | Alvocidib | ʻO Alvocidib kahi pūhui synthetic N-methylpiperidinyl chlorophenyl flavone. Ma keʻano he mea hoʻopaneʻe o ka cyclin-dependent kinase, alvocidib induces cell cycle arrest ma ka pale ʻana i ka phosphorylation of cyclin-dependent kinases (CDKs) a me ka hoʻoponopono iho ʻana i ka cyclin D1 a me D3 hōʻike, ka hopena i ka hopu ʻia ʻana o ka pōʻai cell G1 a me ka apoptosis. He mea hoʻokūkū hoʻokūkū hoʻi kēia mea hana i ka hana adenosine triphosphate. E nānā no nā hoʻokolohua lapaʻau ikaika a i ʻole nā hoʻokolohua lapaʻau pani ʻia me ka hoʻohana ʻana i kēia mea hana. |
| CPD100906 | BS-181 | ʻO BS-181 kahi mea hoʻopaneʻe CDK koho loa no CDK7 me kahi IC(50) o 21 nmol/L. ʻO ka hoʻāʻo ʻana i nā CDK ʻē aʻe a me nā kinase 69 ʻē aʻe i hōʻike ʻia ʻo BS-181 wale nō ke kāohi i ka CDK2 ma nā haʻahaʻa haʻahaʻa haʻahaʻa ma mua o 1 micromol/L, me ka CDK2 i hoʻopaʻa ʻia he 35-fold ka liʻiliʻi (IC(50) 880 nmol/L) ma mua o CDK7. I loko o nā pūnaewele MCF-7, ua kāohi ʻo BS-181 i ka phosphorylation o nā substrates CDK7, hoʻoikaika i ka hopu ʻana o ka cell cycle a me ka apoptosis e pale ai i ka ulu ʻana o nā laina maʻi kanesa, a hōʻike i nā hopena antitumor i vivo. |
| CPD100907 | Riviciclib | ʻO Riviciclib, i kapa ʻia ʻo P276-00, he flavone a me ka cyclin dependent kinase (CDK) inhibitor me ka hana antineoplastic. P276-00 koho a hoʻopaʻa i ka Cdk4/cyclin D1, Cdk1/cyclin B a me Cdk9/cyclin T1, serine/threonine kinases e pāʻani ana i nā kuleana koʻikoʻi i ka hoʻoponopono ʻana i ka pōʻai cell a me ka hoʻonui ʻana o nā kelepona. ʻO ka hoʻopaʻa ʻana i kēia mau kinases e alakaʻi i ka hopu ʻana i ka cell cycle i ka wā o ka hoʻololi ʻana o G1/S, a laila e alakaʻi ana i kahi induction o apoptosis, a me ka pale ʻana i ka hoʻonui ʻana o ka cell tumor. |
| CPD100908 | MC180295 | ʻO MC180295 kahi mea hoʻopiʻi CDK9 koho nui loa (IC50 = 5 nM). (MC180295 he ākea anti-cancer hana in vitro a he mea pono i loko o vivo maʻi 'aʻai kŘkohu. |
| 1073485-20-7 | LDC000067 | ʻO LDC000067 kahi mea hoʻopale CDK9 ikaika a koho. LDC000067 inhibited in vitro transcription in a ATP-competitive and dose-dependent manner. Hōʻike ʻia ka hōʻike ʻana o Gene expression profile o nā cell i mālama ʻia me LDC000067 i kahi hōʻemi koho o nā mRNA pōkole, me nā mea hoʻoponopono koʻikoʻi o ka hoʻonui a me ka apoptosis. ʻO ka loiloi o ka de novo RNA synthesis i manaʻo i kahi kūlana maikaʻi ākea o CDK9. Ma ka pae molecular a me ka cellular level, LDC000067 reproduced effects hiʻona o ka CDK9 inhibition e like me ka hoʻonui ʻana i ka pausing o RNA polymerase II ma nā genes a, ʻo ka mea nui loa, ka hoʻokomo ʻana o ka apoptosis i loko o nā pūnana maʻi maʻi. Kāohi ʻo LDC000067 i ka P-TEFb i hilinaʻi ʻia i ka transcription in vitro. Induces apoptosis in vitro a in vivo i hui pū me BI 894999. |
| CPD100910 | SEL120-34A | ʻO SEL120-34A kahi mea hoʻopale CDK8 ikaika a koho i loko o nā pūnaewele AML me nā kiʻekiʻe o ka serine phosphorylation o STAT1 a me STAT5 transactivation domain. Kāohi ʻo EL120-34A i ka phosphorylation o STAT1 S727 a me STAT5 S726 i loko o nā pūnana maʻi maʻi in vitro. I ka manawa like, ua ʻike ʻia ka hoʻoponopono ʻana o STATs- a me NUP98-HOXA9- hilinaʻi transcription ma ke ʻano he hana mana o ka hana ma vivo. |
| CPD100501 | UNC2541 | ʻO UNC2541 kahi mea hoʻopaneʻe ikaika a me MerTK-specific e hōʻike ana i ka hana pale sub-micromolar i ka ELISA i hoʻokumu ʻia. Eia kekahi, ua hoʻoholo ʻia kahi hanana X-ray o MerTK protein i loko o ka paʻakikī me 11 e hōʻike i ka paʻa ʻana o kēia mau macrocycles i ka ʻeke MerTK ATP. Ua hōʻike ʻo UNC2541 iā IC50 MerTH=4.4 nM; IC50 AXL = 120 nM; IC50 TYRO3 = 220 nM; IC50 FLT3 = 320 nM. |
| CPD100745 | RU-302 | ʻO RU-302 kahi mea hoʻopaneʻe pan-tam hou, e ālai ana i ka pilina ma waena o tam ig1 ectodomain a me gas6 lg domain, hiki ke pale i nā laina kelepona axl reporter a me nā mea hoʻokipa tam maoli. |
| CPD100744 | R916562 | |
| CPD100743 | Ningetinib-Tosylate | ʻO CT-053, ʻike ʻia hoʻi ʻo DE-120, he VEGF a me PDGF inhibitor hiki ke mālama i ka macular degeneration pili i ka makahiki. |
| CPD100742 | SGI-7079 | ʻO SGI-7079 kahi mea hoʻopaneʻe Axl ikaika a koho me ka hana anticancer. Ua pale pono ʻo SGI-7079 i ka hoʻoulu ʻana o Axl i mua o ka ligand Gas6 exogenous. Ua kāohi ʻo SGI-7079 i ka ulu ʻana o ka maʻi maʻi ma ke ʻano i hilinaʻi ʻia. ʻO Axl kahi pahuhopu lapaʻau kūpono no ka lanakila ʻana i ka pale ʻana i ka EGFR inhibitor. |
| CPD100741 | 2-D08 | ʻO 2-D08 kahi flavone synthetic e pale ai i ka sumoylation. Ua hōʻike ʻo 2-D08 i ka hopena anti-aggregatory a me ka neuroprotective |
| CPD100740 | ʻO Dubermatinib | ʻO Dubermatinib, ka mea i kapa ʻia ʻo TP-0903, he mea hoʻokae AXL ikaika a koho. Hoʻoulu ʻo TP-0903 i ka apoptosis nui i nā pūnae CLL B me nā waiwai LD50 o nā pae nanomolar. ʻO ka hui pū ʻana o TP-0903 me BTK inhibitors e hoʻonui i ka CLL B-cell apoptosis AXL overexpression kahi kumuhana reoccurring i ʻike ʻia i nā ʻano tumora he nui i loaʻa ke kū'ē i nā ʻano mea like ʻole. ʻO ka mālama ʻana i nā pūnaewele maʻi maʻi me TP-0903 e hoʻohuli i ka mesenchymal phenotype i loko o nā kumu hoʻohālike he nui a hoʻonaʻauao i nā cell cancer i ka mālama ʻana me nā mea hana ʻē aʻe. ʻO ka lawelawe ʻana o TP-0903 ma ke ʻano he mea hoʻokahi a i hui pū ʻia me nā mea hoʻopaneʻe BTK hiki ke kūpono i ka mālama ʻana i nā maʻi me CLL. |
| CPD100739 | NPS-1034 | ʻO NPS-1034 kahi mea hoʻopaneʻe MET hou, kahi e kāohi ai i ka mea hoʻokipa MET i hoʻāla ʻia a me kāna mau mutants constitutively actively actively. NPS-1034, kaohi i nā ʻano mutant constitutively active o MET a me HGF-activated wild-type MET. Ua kāohi ʻo NPS-1034 i ka hoʻonui ʻana o nā cell e hōʻike ana i ka MET i hoʻāla ʻia a hāpai i ka regression o nā maʻi koko i hoʻokumu ʻia mai ia mau cell i loko o kahi hoʻohālike xenograft mouse ma o nā hana anti-angiogenic a pro-apoptotic. ʻO NPS-1034 hoʻi i kāohi i ka hoʻoulu ʻana o ka HGF-hoʻoulu ʻia o ka hōʻailona MET i ke alo a i ʻole ka nele o ka serum. ʻO ka mea nui, ua kāohi ʻo NPS-1034 i ʻekolu mau ʻokoʻa MET e kū kūʻē i ka MET inhibitors SU11274, NVP-BVU972, a me PHA665752. |
| CPD100738 | ʻO Glesatinib | ʻO Glesatinib, ka mea i ʻike ʻia ʻo MGCD-265, he mea hiki ke hoʻohana ʻia i ka waha, liʻiliʻi-mole, multitargeted tyrosine kinase inhibitor me ka hana antineoplastic. Hoʻopili ʻo MGCD265 a hoʻopaʻa i ka phosphorylation o kekahi mau receptor tyrosine kinases (RTKs), me ka c-Met receptor (hepatocyte growth factor receptor); ka mea hoʻokipa Tek/Tie-2; vascular endothelial growth factor receptor (VEGFR) ʻano 1, 2, a me 3; a me ka macrophage-stimulating 1 receptor (MST1R a i ʻole RON). |
