TAK-659 hydrochloride is a highly potent, selective, reversible and orally available dual inhibitor ofspleen tyrosine kinase (SYK)andfms related tyrosine kinase 3 (FLT3), with anIC₅₀of 3.2 nM and 4.6 nM forSYKandFLT3, respectively. TAK-659 hydrochloride induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL)^[1][2][3][4].

IC50: 3.2 nM (Syk), 4.6 nM (FLT3)^[1]

TAK-659 hydrochloride inhibits cellular proliferation in SYK-dependent DLBCL and FLT3-dependent AML cell lines^[1][3].
TAK-659 hydrochloride (5 μM; 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^[4].
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^[2].

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^[4].
TAK-659 hydrochloride treatment kills tumor cells, but not host cells within the spleen and tumors^[4].
TAK-659 hydrochloride treatment abrogates metastasis of tumor cells into bone marrow^[4].

380.85

Solid

C₁₇H₂₂ClFN₆O

1952251-28-3

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)

H₂O : 2 mg/mL(5.25 mM;ultrasonic and adjust pH to 3 with HCl)

DMSO :< 1 mg/mL(insoluble or slightly soluble)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (stored under nitrogen, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。