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TAK-659 hydrochloride

CAS No. : 1952251-28-3

MCE 站：TAK-659 hydrochloride

产品活性：TAK-659 hydrochloride 是一种高效选择性、可逆的，口服有效的 SYK/FLT3 双抑制剂，对 SYK 和 FLT3 作用的 IC₅₀ 值分别为 3.2 nM、4.6 nM。TAK-659 hydrochloride 能诱导肿瘤细胞死亡而不作用于非肿瘤细胞，具有研究慢性淋巴细胞白血病 (CLL) 的潜力。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Syk  |  FLT3

In Vitro: TAK-659 hydrochloride inhibits cellular proliferation in SYK-dependent DLBCL and FLT3-dependent AML cell lines.
TAK-659 hydrochloride (5 ?M; 1-24 hours) induces Casp3 activation in the LMP2A/MYC cells which was readily apparent at 4 h and reached maximum levels at 8 h of treatment.
TAK-659 hydrochloride (0.01-10 μM; 1 hour) stimulates expression of phospho-Syk at Tyr525 and Tyr352 and phospho-ERK1/2 increased in Ramos cells.

In Vivo: TAK-659 hydrochloride (100 mg/kg/day; p.o.; daily, for 10 days) treatment totally abrogates splenomegaly and tumor development in LMP2A/MYC mice in both pretumor and tumor cell transfer experiments.
TAK-659 hydrochloride treatment kills tumor cells, but not host cells within the spleen and tumors.
TAK-659 hydrochloride treatment abrogates metastasis of tumor cells into bone marrow.

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