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JANEX-1

CAS号

202475-60-3

分子式

C16H15N3O3

主要靶点

JAK

仅限科研使用

Cat No : CM04897

Print datasheet

Synonyms

Inhibitor|JAK|JAK3|Janus kinase|JANEX1|JANEX-1|JANEX 1|Jak3 inhibitor I|WHI-P131|WHI-P-131|WHI-P 131|inhibit

验证数据展示

  • CAS No.: 202475-60-3

    JANEX-1
    CAS#: 202475-60-3

产品信息

CAS号 202475-60-3
分子式 C16H15N3O3
主要靶点 JAK
主要通路 表观遗传|JAK/STAT 信号通路|血管生成|干细胞|蛋白酪氨酸激酶
分子量 297.31
纯度 99.73%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Inhibitor|JAK|JAK3|Janus kinase|JANEX1|JANEX-1|JANEX 1|Jak3 inhibitor I|WHI-P131|WHI-P-131|WHI-P 131|inhibit

靶点活性

JAK3:78 μM

体内活性

JANEX-1以5至100 mg/kg剂量给药。CPK活性评估显示出剂量-反应曲线，其中有效剂量50（ED50）值为7.44 mg/kg。接受JANEX-1治疗的小鼠显示出CPK和LDH水平显著降低。此外，与I/R手术小鼠（65.64±3.76%）相比，JANEX-1处理小鼠的梗塞大小显著减小（30.16±2.79%）[2]。JANEX-1（WHI-P131）被快速吸收，达到最大血浆JANEX-1浓度（tmax）的时间为24.7±1.7分钟。JANEX-1被迅速消除，其消除半衰期为45.6±5.5分钟。尽管预测的最大血浆JANEX-1浓度仅为10.5 ± 0.8 μM，是通过静脉（i.v.）给药同等剂量Cmax的一半，但腹腔内（i.p.）生物可利用度为94.6%，系统暴露水平（即AUC）与静脉注射后观察到的水平非常相似（17.1±2.2 μMh对比18.1±1.2 μMh）[3]。

体外活性

JANEX-1 (WHI-P131) 表现出强大的JAK3抑制活性（IC50为78μM），但并不抑制JAK1和JAK2、ZAP/SYK家族酪氨酸激酶SYK、TEC家族酪氨酸激酶BTK、SRC家族酪氨酸激酶LYN或受体家族酪氨酸激酶胰岛素受体激酶，即使在高达350μM的浓度下也是如此。JANEX-1在表达JAK3的人类白血病细胞系NALM-6和LC1;19中诱导凋亡，但不影响黑色素瘤（M24-MET）或鳞状细胞癌（SQ20B）细胞。WHI-P131以浓度依赖的方式抑制阳性JAK3的白血病细胞系DAUDI、RAMOS、LC1;19、NALM-6、MOLT-3和HL-60的集落形成能力，但对JAK3阴性的BT-20乳腺癌、M24-MET黑色素瘤或SQ20B鳞状细胞癌细胞系则无影响。WHI-P131对NALM-6细胞的EC50为24.4μM，对DAUDI细胞的EC50为18.8μM，能以浓度依赖性方式抑制集落生长。在100μM浓度下，WHI-P131能够抑制这些白血病细胞系的体外集落形成能力，抑制率超过99%。相反，JANEX-1不抑制JAK3阴性的M24-MET黑色素瘤或SQ20B鳞状细胞癌细胞系的集落生长。

溶解度

DMSO:55 mg/mL (184.99 mM)

细胞实验

JANEX-1 (WHI-P131) is dissolved in DMSO and stored, and then diluted with appropriate media (DMSO 0.1%) before use[1]. The following cell lines are used in various biological assays: NALM-6 (pre-B-ALL), LC1;19 (pre-B-ALL), DAUDI (B-ALL), RAMOS (B-ALL), MOLT-3 (T-cell ALL), HL60 (acute myelogenous leukemia), BT-20 (breast cancer), M24-MET (melanoma), SQ20B (squamous cell carcinoma), and PC3 (prostate cancer). These cell lines are maintained in culture. Cells are seeded in six-well tissue culture plates at a density of 50×104 cells/well in a treatment medium containing various concentrations of JANEX-1 (0.1, 0.2, 0.3, 0.4 and 0.5 nM) and incubated for 24-48 h at 37°C in a humidified 5% CO2 atmosphere. Cells are examined for apoptotic changes after treatment with JANEX-1 by the in situ TdT-mediated dUTP end-labeling assay using the ApopTag apoptosis detection kit[1].

参考文献

1.Sudbeck EA, et al. Structure-based design of specific inhibitors of Janus kinase 3 as apoptosis-inducing antileukemic agents. Clin Cancer Res. 1999 Jun;5(6):1569-82.
2.Oh YB, et al. Inhibition of Janus activated kinase-3 protects against myocardial ischemia and reperfusion injury in mice. Exp Mol Med. 2013 May 17;45:e23.
3.Uckun FM, et al. In vivo toxicity and pharmacokinetic features of the janus kinase 3 inhibitor WHI-P131 [4-(4'hydroxyphenyl)-amino-6,7- dimethoxyquinazoline. Clin Cancer Res. 1999 Oct;5(10):2954-62.

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