TAK-659 hydrochloride|cas:1952251-28-3|西域试剂

TAK-659 hydrochloride,99.91%

产品编号：Bellancom-100867A| CAS NO：1952251-28-3| 分子式：C₁₇H₂₂ClFN₆O| 分子量：380.85

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货号	价格	库存与货期
Bellancom-100867A	￥950.00	杭州北京（现货）
Bellancom-100867A	￥1400.00	杭州北京（现货）
Bellancom-100867A	￥2800.00	杭州北京（现货）
Bellancom-100867A	￥4200.00	杭州北京（现货）
Bellancom-100867A	￥6500.00	杭州北京（现货）

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TAK-659 hydrochloride

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 of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC₅₀ of 3.2 nM and 4.6 nM for SYK and FLT3, 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)^[4].

体外研究

TAK-659 hydrochloride inhibits cellular proliferation in SYK-dependent DLBCL and FLT3-dependent AML cell lines.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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

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].

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

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 mg	5 mg	10 mg

1 mM	2.6257 mL	13.1285 mL	26.2571 mL
5 mM	0.5251 mL	2.6257 mL	5.2514 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°C, 6 months; -20°C, 1 month (stored under nitrogen, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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)

参考文献