TAK-659 hydrochloride

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

TAK-659 hydrochloride  纯度: 99.91%

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。

TAK-659 hydrochloride

TAK-659 hydrochloride Chemical Structure

CAS No. : 1952251-28-3

规格 价格 是否有货 数量
2 mg ￥900 In-stock
5 mg ￥1400 In-stock
10 mg ￥1900 In-stock
25 mg ￥3900 In-stock
50 mg ￥5900 In-stock
100 mg ￥9900 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

TAK-659 hydrochloride 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • Clinical Compound Library Plus
  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Clinical Compound Library
  • Drug Repurposing Compound Library
  • Anti-COVID-19 Compound Library
  • Orally Active Compound Library
  • Anti-Blood Cancer Compound Library

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)[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].

上海金畔生物科技有限公司 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[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].

上海金畔生物科技有限公司 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.

Clinical Trial

分子量

380.85

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

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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)。-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。
参考文献

  • [1]. Lam B, et al. Discovery of TAK-659 an orally available investigational inhibitor of Spleen Tyrosine Kinase (SYK). Bioorg Med Chem Lett. 2016 Dec 15;26(24):5947-5950.

    [2]. Purroy N, et al. Inhibition of BCR signaling using the Syk inhibitor TAK-659 prevents stroma-mediated signaling in chronic lymphocytic leukemia cells. Oncotarget. 2017 Jan 3;8(1):742-756.

    [3]. Jie Yu, et al. Anti-tumor activity of TAK-659, a dual inhibitor of SYK and FLT-3 kinases, in AML models. Journal of Clinical Oncology 34, no. 15_suppl.

    [4]. Cen O, et al. Spleen Tyrosine Kinase Inhibitor TAK-659 Prevents Splenomegaly and Tumor Development in a Murine Model of Epstein-Barr Virus-Associated Lymphoma. mSphere. 2018 Aug 22;3(4).

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务