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SB-743921 hydrochloride

CAS No. : 940929-33-9

MCE 国际站：SB-743921 hydrochloride

产品活性：SB-743921 hydrochloride 是一种有效的驱动蛋白 (Eg5) 抑制剂，K_i 值为 0.1 nM。

研究领域：Cell Cycle/DNA Damage  |  Cytoskeleton

作用靶点：Kinesin

In Vitro: SB-743921 is a potent inhibitor of Eg5, with a K_i of 0.1 nM. SB-743921 (1 nM) potently inhibits colony forming cell (CFC) formation of chronic myeloid leukemia (CML) primary cells, but exhibits slight inhibitory activities on the colony-forming ability of normal bone marrow progenitors. SB-743921 (1, 3 nM) induces apoptosis of CML primary CD34 + cells, and shows slight effect on normal CD34 + cells. SB-743921 (2 nM) in combination with imatinib displays additive anti-proliferative effect in KCL22 and CML CD34 + cells. Furthermore, SB-743921 overcomes imatinib resistance in CML cells. SB-743921 (0.5 nM, 1 nM, 3 nM) inhibits MEK/ERK and AKT signaling in CML cells.

In Vivo: SB-743921 has good oral bioavailability and pharmacokinetics and induces complete tumor regression in nude mice bearing lung cancer patient xenografts.

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货号: HY-12069

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