Olverembatinib (GZD824) dimesylate 是一种高效的，具有口服活性的 pan-Bcr-Abl 抑制剂。Olverembatinib dimesylate 能广泛而有效地抑制突变型 Bcr-Abl。Olverembatinib dimesylate 对天然的 Bcr-Abl 和 Bcr-Abl^T315I 作用的 IC₅₀ 值分别为 0.34 nM 和 0.68 nM。Olverembatinib dimesylate 具有抗肿瘤作用。

Olverembatinib (GZD824) dimesylate is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib dimesylate potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib dimesylate strongly inhibits native Bcr-Abl and Bcr-Abl with IC 50 s of 0.34 nM and 0.68 nM, respectively. Olverembatinib dimesylate has antitumor activity.

Solid

IC50: 0.68 nM (Bcr-Abl), 0.27 nM (Bcr-Abl) , 0.71 nM (Bcr-Abl) , 0.15 nM (Bcr-Abl), 0.35 nM (Bcr-Abl), 0.29 nM (Bcr-Abl), 0.35 nM (Bcr-Abl), Bcr-Abl

Olverembatinib dimesylate shows antiproliferative activity in stably transformed Ba/F3 cells whose growth was driven by native Bcr-Abl or Bcr-Abl mutants.
Olverembatinib dimesylate selectively and potently inhibits the proliferation of Bcr-Abl-positive leukemia cells.
Olverembatinib dimesylate inhibits Bcr-Abl signaling in K562 (1-20 nM; 4.0 hours) and Ba/F3 stable cell lines expressing native Bcr-Abl (0.1-100 nM; 4.0 hours) or Bcr-Abl(0.1-100 nM; 4.0 hours).
has not independently confirmed the accuracy of these methods. They are for reference only.

Olverembatinib dimesylate suppresses tumor growth in mice bearing allografted Ba/F3 cells expressing Bcr-Abl .
Olverembatinib dimesylate (1-20 mg/kg; i.g.; daily; for 10 days) significantly increases the median survival of the mice bearing allografted Ba/F3 cells expressing Bcr-Abl.
Olverembatinib dimesylate exhibits a good oral bioavailability (rat 48.7%) and C max (rat 390.5 μg/L) following oral administration (rat; 25 mg/kg).
Olverembatinib dimesylate exhibits terminal elimination half-lives (rat 5.6 h) due to high plasma clearance (rat 1.7 L/h/kg) following intravenous administration (rat 5 mg/kg).
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

[1]. Ren X, Pan X, Zhang Z, Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against

In Vitro: DMSO : 125 mg/mL (172.47 mM; Need ultrasonic)H₂O : ≥ 50 mg/mL (68.99 mM)