WHI-P97
(Synonyms: 4-(3',5'-二溴-4-羟基苯基)氨基-6,7-二甲氧基喹唑啉,WHI-P-97;WHI P97) 目录号 : GC15956
WHI-P97 是一种有效的选择性 JAK-3 抑制剂。
Cas No.:211555-05-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
WHI-P97 is a rationally designed potent inhibitor of JAK-3.IC50 value:Target: JAK3Treatment of mast cells with WHI-P97 inhibited the translocation of 5-lipoxygenase (5-LO) from the nucleoplasm to the nuclear membrane and consequently 5-LO-dependent leukotriene (LT) synthesis after IgE receptor/FcepsilonRI crosslinking by >90% at low micromolar concentrations. WHI-P97 did not directly inhibit the enzymatic activity of 5-LO, but prevented its translocation to the nuclear membrane without affecting the requisite calcium signal. WHI-P97 was very well tolerated in mice, with no signs of toxicity at dose levels ranging from 5 microg/kg to 50 mg/kg, and LD(10) was not reached at a 50 mg/kg dose level when administered as a single i. p. or i.v. bolus dose.
References:
[1]. Ji KA, Yang MS, Jou I, Shong MH, Joe EH.Thrombin induces expression of cytokine-induced SH2 protein (CIS) in rat brain astrocytes: involvement of phospholipase A2, cyclooxygenase, and lipoxygenase.Glia. 2004 Nov 1;48(2):102-11.
[2]. Wong WS, Leong KP.Tyrosine kinase inhibitors: a new approach for asthma.Biochim Biophys Acta. 2004 Mar 11;1697(1-2):53-69.
[3]. Uckun FM, Sudbeck EA, Mao C, Ghosh S, Liu XP, Vassilev AO, Navara CS, Narla RK.Structure-based design of novel anticancer agents.Curr Cancer Drug Targets. 2001 May;1(1):59-71.
[4]. Sudbeck EA, Liu XP, Narla RK, Mahajan S, Ghosh S, Mao C, Uckun FM.Structure-based design of specific inhibitors of Janus kinase 3 as apoptosis-inducing antileukemic agents.Clin Cancer Res. 1999 Jun;5(6):1569-82.
| Cas No. | 211555-05-4 | SDF | |
| 别名 | 4-(3',5'-二溴-4-羟基苯基)氨基-6,7-二甲氧基喹唑啉,WHI-P-97;WHI P97 | ||
| 化学名 | 2,6-dibromo-4-[(6,7-dimethoxyquinazolin-4-yl)amino]phenol | ||
| Canonical SMILES | COC1=C(C=C2C(=C1)C(=NC=N2)NC3=CC(=C(C(=C3)Br)O)Br)OC | ||
| 分子式 | C16H13Br2N3O3 | 分子量 | 455.11 |
| 溶解度 | DMSO : 3.33 mg/mL (7.32 mM; ultrasonic and warming and heat to 80°C) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1973 mL | 10.9864 mL | 21.9727 mL |
| 5 mM | 0.4395 mL | 2.1973 mL | 4.3945 mL |
| 10 mM | 0.2197 mL | 1.0986 mL | 2.1973 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。