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CAS No.: 211555-04-3

WHI-P154 Catalog No. CSN16224

Synonyms: JAK3 Inhibitor II;Janus-Associated Kinase 3 Inhibitor II;Janex1

WHI-P154 is a specific inhibitor of JAK3 with IC50 value of 1.8 μM, almost shows no activity against JAK1 or JAK2.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述WHI-P154 is a potent inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase with an IC50 value of 4nM. It also has modest activity against Janus kinase 3 (JAK3) with an IC50 value of 1.8μM^[3]. WHI-P154 at 1 and 4μM significantly enhanced the cytotoxic effects of mitoxantrone and SN-38 in ABCG2-transfected cells but not in HEK293/pcDNA3.1 cells. Treatment of parental KB-3-1 cells and ABCB1-overexpressing KB-C2 cells with 4μM WHI-P154 resulted in moderate inhibition on ABCB1. The exposure of WHI-P154 (1 and 4μM) and 2.5μM FTC significantly increased the intracellular level of [³H]-mitoxantrone in ABCG2-overexpressing cells. Treatment of ABCG2-482-R2 cells with 4μM WHI-P154 blocked the efflux function of ABCG2^[4]. In mice bearing H694R or E1384K tumors, intravenous injection of WHI-P154 (1mg/kg per day) for 5 weeks significantly suppressed tumor growth and decreased phospho-Y1604 ALK expression in xenografted tumors when compared with DMSO-treated controls^[5].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6581 mL
- 13.2906 mL
- 26.5813 mL
- 5 mM
- 0.5316 mL
- 2.6581 mL
- 5.3163 mL
- 10 mM
- 0.2658 mL
- 1.3291 mL
- 2.6581 mL

技术信息

CAS号

211555-04-3

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H14BrN3O3

运输

蓝冰

分子量

376.20

别名

JAK3 Inhibitor II;Janus-Associated Kinase 3 Inhibitor II;Janex1

溶解度

DMSO	500.0 mg/mL (1329.1 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	10 mg/mL	clear
PO	0.5% CMC-Na	47 mg/mL	suspension

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