Cov khoom lag luam
English Lub Npe: Kev Txiav Txim Siab
Tus lej lej: 114899-77-3
Molecular cov mis: c39h43n3o11s
Molecular hnyav: 761.84
Einecs tus lej:
Lwm Qeb
Lub xov tooj ntawm tes; Cov ntaub ntawv rawcuitical; Reagent rau kev tshawb fawb; Cov tshuaj hauv tsev; General Biochemical reagents - cov khoom ntuj; Cov ntaub ntawv raw; Cov ntaub ntawv rawcuitical; Tshuaj lom neeg cov tshuaj lom neeg; Amines; Cov tshuaj lom neeg; Intermediates & Finchemicals; Kws muag tshuaj; API
Mol Cov Ntaub Ntawv: 114899-77-3. Mol
Cov Qauv Txheej Txheem:

Cov Khoom Siv Tribetidine
Melting point: >143 Qib (Dec.)
Kev sib hloov tshwj xeeb: D 25+114 degree (c =0. 1inmethanol)
Ceev: 1.55 ± {0. 1g / cm3 (20ºC760Torr)
Kev Cia Mob Cia: {- 20 degree cfrechemicalmoyloer Underinertatmosphera
Solubility: soluble hauv cloroform (me ntsis), methanol (me ntsis)
Acidity Coefficient (Pka): 9.73 ± 0. 40 (kwv yees)
Daim Ntawv: Khoom
Xim: lub teeb daj kom tuab daj
Kev ua kho qhov muag tau kho qhov muag: -53. 824.5 (Chcl3)
Inchikey: PkvrcirhQMYSYIX-HAHYLZASNA-n
Siv thiab synthesis ntawm tribetidine
Kev siv
Tribetidine yog ib tus neeg sawv cev alkylating rau cov neeg mob uas tsis raug cai los yog kev ua kom zoo nkauj liposarcoma uas tau txais ib qho tsis muaj npe - uas muaj redimen.
Tribetidine, ib cov tshuaj tshiab rau kev kho cov nqaij mos ntawm cov nqaij mosararara
Thaum Lub Kaum Hlis 23, 2015, Asmeskas tau pom zoo cov tshuaj txiav Rau kev kho mob ntawm unresectable lossis Metastatic Liposarcoma mispos phau ntawv thiab Leiomyosarcoma hauv cov neeg mob Kws Kho Mob uas muaj ib qho anthracycline. Tribetidine, ib lub cytotoxic alkylating alkylating tus neeg sawv cev, tau pom zoo thawj zaug hauv Tebchaws Europe los ntawm kev kho mob ntawm cov muag muag salcoma. Tom qab ntawd, nws tau pom zoo los kho cov mob zes qe menyuam kab mob cancer hauv Tebchaws Europe thiab Canada. Cov neeg tsim khoom yog Zeltia, lub tuam txhab Spanish Biotechnology, Andjohnson & Johnson ntawm Tebchaws Asmeskas.
Kev ua haujlwm biological
Kev Txiav Txim Siab (Eteinascidin743; et {1}}}) yog qhov ua rau ectentumnumin, cais los ntawm ecteinascidiaturbinata. Kev Txiav Txim Siab rau qhov me me Sulci ntawm DchemicalBiTBook, thiab nce Ros ntau lawm hauv cov kabmob qog nqaij hlav, thiab mb -453 hlwb. Kev txiav txim siab tuaj yeem siv tau hauv kev tshawb fawb ntawm cov mos mos nqaij sarcoma thiab zes qe menyuam.
Phiaj taw tes
IC5 {0: 0.1 nm (mx {3}} cov hlwb) thiab 3.7 nm (MCR7 / DXR cov xov tooj)
Kev npau liab
Hauv kev kawm vitro
Kev txiav txim siab (thiab {{{{{0}}; {}}}}? Kev Txiav Txim Siab (Eteinascidin 743) Interhits Cell Kev Loj Hlob ntawm Mx {6}}, MCR7 thiab MC 50 Qhov Tseem Ceeb ntawm 0.1 NM, 1.5 NM, feem. Kev txiav txim siab Interuces CyTotoxicity thiab Apoptosis hauv cov kabmob cancer mis hauv lub sijhawm thiab kev pom zoo. Cov qib kev ntseeg receptor pathwor molecules, trail-r1 / dN4}}}}}} {{{32 {}} thiab 4. {{{{0- daim quav los ntawm kev tu ncua kev kho mob hauv MCF -7 cells. Hauv Mda-MB -453} Cov ntsiab lus Mitochrome Pax, smac / {41}}}, 6-, 4. {8-, 4. {}}}}}}}}}} {}}}}}}}} MDA-MB -453 cov hlwb. Nyob rau hauv kev kho vitro nrog cov kev txiav txim siab uas tsis muaj kev txwv tsis pub muaj CCL2,}} Kev Ntsuam Xyuas Cell
Cell Kab: Mcf7 Hlwb
Kev siab: 10 nm
Lub sijhawm tsim txom: 24 teev, 48 teev, 72 teev
Qhov tshwm sim: coj mus tshaj tawm SG 2- mjectulation.
Hauv Vivo kawm
Kev txiav txim siab (li {-743; poj niam}}} mg; mg; txhua peb hnub; Tus xenograft nas merxoid Liposarcoma (CCCL8, cxcl8, cd {}} kev txo qis ntawm PTX3 tom qab kev txiav txim siab.
Tsiaj Qauv: Poj Niam Kws Ncaws Pob Noob Kab Npag Cov kabmob NU / {{{} g) txhaj nrog mx -1 lub hlwb
Dosage: 30 Ug / kg, 40 ug / kg, 50 tus dab, 50 ug / kg
Kev tswj hwm: kev txhaj tshuaj tiv thaiv zoo; txhua txhua peb hnub
Qhov tshwm sim: nce cov tshuaj tiv thaiv kab mob liab qab hauv cov kabmob nas mx {} mi} Motau} Motau} Motau} Motau} Niam Nkev tsis muaj kev vam meej.
Cim npe nrov: Kev Txiav Txim Cov Tshuaj Txhuam Antitum, Tuam Tshoj Chaw Muag Khoom Siv Antitum tshuaj

