Lestaurtinib来他替尼,111358-88-4

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Lestaurtinib

CAS No. : 111358-88-4

MCE 国际站：Lestaurtinib

产品活性：Lestaurtinib 是一种口服有效的选择性受体酪氨酸激酶抑制剂，能竞争性地抑制 ATP 与 TrkA/B/C 激酶结合。Lestaurtinib 可抑制 RPTKs 的磷酸化，其对 FLT3、TrkA、JAK2 的 IC₅₀ 值分别为 2, 25 和 0.9 nM。Lestaurtinib 能诱导细胞凋亡和周期停滞，可显著抑制肿瘤的生长。

研究领域：Epigenetics  |  Protein Tyrosine Kinase/RTK  |  JAK/STAT Signaling  |  Stem Cell/Wnt  |  Neuronal Signaling  |  Apoptosis

作用靶点：JAK  |  FLT3  |  Trk Receptor  |  Apoptosis  |  STAT

In Vitro: Lestaurtinib (0.01-10 µM; 72 h) inhibits growth of ATC cells, with IC₅₀s of 0.21, 0.41 and 2.35 µM for KMH2, CAL62 and THJ-21T cells, respectively.
Lestaurtinib (0.125-4 µM; 24 h) decreases STAT5 phosphorylation in a concentration-dependent manner, and completely inhibits expression of pSTAT5 at 4 μM.
Lestaurtinib (0.5 µM; 24 h) shows antiproliferative effect on WI-38, CAL62 and KMH2 cells.
Lestaurtinib (4 μM; 24 h) induces cell cycle arrest in the G2/M phase in CAL62 and KMH2 cells.
Lestaurtinib (30-300 nM; 48 h) induces apoptosis in a dose-dependent manner in HL (hodgkin lymphoma) cell lines.
Lestaurtinib (30, 100, 300 nM; 1 h) inhibits JAK2, STAT5 and STAT3 phosphorylation when at 300 nM.

In Vivo: Lestaurtinib (20 mg/kg; s.c.; twice daily (monday to friday) and once daily (saturday and sunday); 3 weeks) significantly inhibits growth of tumor in vivo.

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