DXD hija mediċina li torbot l-antikorpi ta 'inibitur

Isem Ingliż: DXD hija mediċina li torbot antikorpi ta 'inibitur
Numru CAS: 1599440-33-1
Sinonimu Ingliż:
Dxd; Derivattiv exatecan; N - [(1s, 9s) -9- etil -5- fluoro -2, 3,9,10,13, {15- hexahydro -9-} hydroxy {12}}} Metyl -10, {13- di oxo -1 h, 12h-benzo [de] pirano [3 ', 4': 6,7] indolizino [1, {2-} b] quinolin {-1- yl] {-2- hydroxyacetamide; Derivattiv ExateCan għal ADC; Aċetamide, N - [(1s, 9s) -9- ethyl -5- fluoro -2, 3,9,10,13, {{15- hexahydro {-9- hydroxy {{38} methyl -10, 40}} dioxo -1 h, 12h-benzo [de] pirano [3 ', 4': 6,7] indolizino [1, {2- b] quinolin {-1- yl] -2- hydroxy-; Dxd (derivattiv exatecan); OQM5SD32BQ; UNII-OQM5SD32BQ

Ibgħat l-inkjesta

Deskrizzjoni tal-Prodotti

Isem Ingliż: DXD hija mediċina li torbot antikorpi ta 'inibitur

Numru CAS: 1599440-33-1

Formula molekulari C26H24FN3O6

Piż molekulari 493.48

Struttura molekulari:

Kategoriji relatati ta 'ċitotossini; Prodotti standard; Reaġent bijoloġiku; Reaġent kimiku

Propjetajiet derivattivi ta 'dx -8951

Punt tat-togħlija 957.9 ± 65. 0 grad (previst)

Densità 1.57 ± 0. 1g / cm3 (imbassar)

Aħżen fi -20 grad

Solubilità DMSO: 4 0. 0 (konċentrazzjoni massima mg / ml); 81.06 (konċentrazzjoni massima mm)

Solidu morfoloġiku

Koeffiċjent tal-Aċidità (PKA) 11.18 ± 0. 40 (imbassar)

Uża u sintesi ta 'dx -8951 derivattivi

Attività bijoloġika

DXD (derivattiv exatecan għal ADC) huwa inibitur qawwi ta 'topoisomerase tad-DNA b'IC5 0 ta' 0.31 μM. Tagħbija ta 'mediċina akkoppjata bl-antikorpi ADC (ds -8201 a) li tista' tintuża biex timmira HER2.

Post immirat

Topoisomerase i 0. 31 μm (IC 50) Camptothecins

Studju in 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).

Studju in vivo

Ds -8201 a (dxd hija l-piż tat-tagħbija, 10 mg / kg, iv) turi attività antitumor potenti fil-mudelli pożittivi tagħha 2- bi KPL4, Jimt {-1, u capan {-1 u fil-HER2 li jesprimi l-baxx ST565 u ST313 Modelli 1+ / espressjoni negattiva tal-ħut.

It-tags Popolari: DXD hija mediċina li torbot l-antikorpi ta 'inibitur, iċ-Ċina DXD hija fornituri ta' mediċini li jorbtu l-antikorpi ta 'inibitur