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TAK-659 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TAK-659 hydrochloride图片
CAS NO:1952251-28-3
包装与价格:
包装价格(元)
2mg电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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。
生物活性

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& Target

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

体外研究
(In Vitro)

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].

Apoptosis Analysis[4]

Cell Line:LMP2A/MYC cells
Concentration:5 μM
Incubation Time:1 hour, 2 hours, 4 hours, 8 hours, 24 hours
Result:Induced apoptosis in LMP2A/MYC lymphoma cells.

Western Blot Analysis[2]

Cell Line:Ramos cells
Concentration:0.01 μM,0.1 μM,1 μM,10 μM
Incubation Time:1 hour
Result:Enhanced expression of phospho-Syk at Tyr525 and Tyr352 and phospho-ERK1/2 in stimulated Ramos cells.
体内研究
(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[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].

Animal Model:LMP2A/MYC double transgenic mice[4]
Dosage:100 mg/kg/day
Administration:Oral gavage; for 10 days
Result:Inhibited LMP2A-induced tumor cell survival in vivo.
Clinical Trial
分子量

380.85

性状

Solid

Formula

C17H22ClFN6O

CAS 号

1952251-28-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, stored under nitrogen, away from moisture

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

溶解性数据
In Vitro: 

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

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

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.6257 mL13.1285 mL26.2571 mL
5 mM0.5251 mL2.6257 mL5.2514 mL
10 mM---------
*

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。