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GZD824

CAS No. : 1257628-77-5

MCE 站：GZD824

产品活性：GZD824 (HQP1351) 是一种高效的，具有口服活性的 pan-Bcr-Abl 抑制剂。GZD824 能广泛而有效地抑制突变型 Bcr-Abl。GZD824 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。GZD824 具有抗肿瘤作用。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Bcr-Abl

In Vitro: GZD824 shows antiproliferative activity in stably transformed Ba/F3 cells whose growth was driven by native Bcr-Abl or Bcr-Abl mutants.
GZD824 selectively and potently inhibits the proliferation of Bcr-Abl-positive leukemia cells.
GZD824 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^T315I(0.1-100 nM; 4.0 hours).

In Vivo: GZD824 suppresses tumor growth in mice bearing allografted Ba/F3 cells expressing Bcr-Abl ^WT.
GZD824 (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^T315I.
GZD824 exhibits a good oral bioavailability (rat 48.7%) and C_max (rat 390.5 μg/L) following oral administration (rat; 25 mg/kg).
GZD824 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).

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