货号:A863648
同义名:
TAK-659;TAK-659 hydrochloride
TAK-659 HCl is a selective inhibitor of spleen tyrosine kinase (Syk) with IC50 of 3.2 nM.
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产品名称 | Syk ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
PRT062607 HCl |
++++
Syk, IC50: 1 nM |
99%+ | |||||||||||||||||
R406 |
++
Syk, IC50: 41 nM |
99%+ | |||||||||||||||||
Fostamatinib Disodium |
++
Syk, IC50: 41 nM |
99%+ | |||||||||||||||||
Piceatannol | ✔ | PKC | 99%+ | ||||||||||||||||
BAY 61-3606 2HCl |
+++
Syk, Ki: 7.5 nM |
99+% | |||||||||||||||||
Entospletinib |
+++
Syk, IC50: 7.7 nM |
99%+ | |||||||||||||||||
MNS |
+
Syk, IC50: 2.5 μM |
Src,p97 | 99%+ | ||||||||||||||||
Fostamatinib |
++
Syk, IC50: 41 nM |
99%+ | |||||||||||||||||
RO9021 |
+++
Syk, IC50: 5.6 nM |
98% | |||||||||||||||||
TAK-659 HCl |
++++
Syk, IC50: 3.2 nM |
FLT3 | 99%+ | ||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Spleen Tyrosine Kinase (SYK) is a non-receptor cytoplasmic tyrosine kinase that is primarily expressed in hematopoietic cells. SYK is a key mediator for a variety of inflammatory cells, including B cells, mast cells, macrophages and neutrophils[3]. TAK-659 hydrochloride is a potent, selective and orally available spleen tyrosine kinase (Syk) inhibitor with an IC50 of 3.2 nM[3]. In a cell proliferation assay, TAK-659 shows inhibition toward a SYK-dependent cell line (OCILY10)[3]. TAK-659 inhibited the microenvironment-induced activation of Syk and downstream signaling molecules, without inhibiting the protein homologue ZAP-70 in T cells. Importantly, the pro-survival, proliferative, chemoresistant and activation effects promoted by the microenvironment were abrogated by TAK-659, which furthermore blocked CLL cell migration toward BMSC, CXCL12, and CXCL13[4]. TAK-659 blocks anti-IgD (immune-globulin D antibody) stimulated CD86 expression in mouse peripheral B cells in vivo. In the OCI-LY10 xenograft and DLBCL PHTX-95L (primary human tumor graft from DLBCL patient) mouse models, TAK-659 demonstrates potent tumor growth inhibition (TGI) after 20 days of treatment. In the FLT3-dependent MV4-11 xenograft model, TAK-659 shows tumor regression at 60 mg/kg daily after 20 days of dosing[3]. |
Dose | Mice: 60 mg/kg/day[2] (p.o.), 100 mg/kg[3] (p.o.) |
Administration | p.o. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.63mL 0.53mL 0.26mL |
13.13mL 2.63mL 1.31mL |
26.26mL 5.25mL 2.63mL |
CAS号 | 1952251-28-3 |
分子式 | C17H22ClFN6O |
分子量 | 380.848 |
别名 | TAK-659;TAK-659 hydrochloride |
运输 | 蓝冰 |
存储条件 |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
H2O: 2 mg/mL(5.25 mM),配合低频超声,并调节pH至3 |
动物实验配方 |