Cov khoom lag luam

Hmong npe: Exatecan mesylate

Tus lej lej: 169869-90-3

Molecular cov mis: c25h26fn3o7s

Molecular hnyav: 531.56

Einecs tsis muaj

Lwm yam pawg:

ADC Toxin tshuaj; Cytotoxin; tshuaj lom neeg cov tshuaj lom neeg; lwm

Cov Qauv Txheej Txheem:

1 -

ICTECAN MESYLINES

Kev Cia Mob Cia: 4 C, Tiv Thaiv Kev Tiv Thaiv, Cov Khw Muag Khoom

Solubility: DMSO: 7.41 (siab tshaj plaws mg / cov tshuaj lom neeg); 13.94 (siab tshaj plaws mm) dej: {{{{}}. 0 (siab tshaj mg / ml); 0. 19 (siab tshaj mm)

Daim Ntawv: Khoom

Xim: lub teeb daj rau daj-ntsuab

Stability: hygroscopicity

Inchikey: NpagDydyDjhsbmfs-otcaljqena-n

Smiles: s (o) (= o) ({1} {{4} {{{{{{{}} c4 C 5= CC6 [C @@] (C ({}}}}}} {} 17}}) (O) CC|& 1: 6,21, r |

Icitecan Mesylate, Siv thiab Khoom Siv Hluav Taws Xob

Kev siv

ICetecan mesylate yog DNA sab saum toj tolyisomerase i (sab topoisomerase i) inhositorase i) {}}}}}}} {} {thiab tuaj yeem siv rau cov kev tshawb fawb cancer.

Bioactivity

Exatecan mesylate (DX8951F) yog DNA sab saum toj tolyisomerase i (sab topoisomerase i) {} Tus nqi ntawm 2.2 μ m (0.93 thiab tuaj yeem siv rau kev tshawb fawb cancer.

Phiaj Xwm

Syoisomerase i {{0. 975 μ mL (IC 50)

Hauv kev kawm vitro

Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC 50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a). Dxd is cytotoxic to human cancer cell lines of KPL-4, NCI-N87, SK-BR-3, and MDA-MB-468 with IC 50 s of 1.43 nM-4.07 nM, but the control IgG-ADC (Dxd is the payload) shows no inhibition on the four cell lines (with HER2 expression). DS-8201a (Dxd is the payload) displays significant suppression on the HER2-positive KPL-4, NCI-N87, and SK-BR-3 cell lines, with IC 50 values of 26.8, 25.4, and 6.7 ng/mL, respectively, but with no such inhibition on MDA-MB-468 (IC 50 , >10, {{000 ng / ml).

Hauv Vivo Tshawb Fawb

Exatecan mesylate (dx {-8951 f, 3.}}}}}}}}}}} Mg, chaw ua yeeb yam tshuaj laus hauv cov mice kev tuag. Exatecan Mesylate (15, 25, 25, IV, iv) Hightly Cov Qauv Kev Loj Hlob Hauv Mia-Qib} Tus Qauv Kawm Thaum Ntxov ntawm Bxpc {}}. Exatecan Mesylate (15, 25, 25, iv, iv) kuj tau symphat getastasis thiab tag nrho tshem tawm Lung MetaSastasis hauv Bxpc {15}} theem-theem pib cancer qauv.

Cim npe nrov: Exatecan Mesylate muaj kev ua haujlwm antectumn, Tuam Tshoj exatecan mesylate muaj cov neeg siv tshuaj tiv thaiv kab mob anticator