| GW441756TrkA inhibitor,potent and selective |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 99.95%
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- NMR (Nuclear Magnetic Resonance)
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Chemical structure
Related Biological Data
| Description | GW441756 is a potent, selective inhibitor of TrkA with an IC50 value of 2 nM. | |||||
| Targets | TrkA | CDK2 | C-Raf-1 | |||
| IC50 | 2 nM | >7 μM | >12 μM | |||
| Cell experiment [1]: | |
Cell lines | human muscle sarcoma cancer cell line HTB114 |
Preparation method | The solubility of this compound in DMSO is >13.8mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | IC50 = 2nM |
Applications | In human muscle sarcoma cancer cell line HTB114, GW441756 dose-dependently decreased neoplastic proliferation and significantly increased apoptosis in a dose-dependent way. GW441756 also increased the level of caspase-3, which then led to apoptosis. |
| Animal experiment [2]: | |
Animal models | Alzheimer’s disease (AD) mouse model, PDAPP (J20) mice |
Dosage form | 10 mg/kg/day (subcutaneous injection, Sub-Q); 5 days |
Application | In Alzheimer’s disease (AD) mouse model, PDAPP (J20) mice, GW441756 at 10 mg/kg increased the level of sAβPPα and increased the sAβPPα to Aβ42 ratio to 1.85 times over control. At this dose, GW441756 gave measurable brain levels with a maximum brain concentration (Cmax, 1 h) of ~1×IC50 (50 nM). |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Montagnoli C, Pistilli A, Stabile A M, et al. Anti-proliferative effects of GW441756, a novel inhibitor of NGFreceptor tyrosine kinase a (TRKA), in human sarcoma. Italian Journal of Anatomy and Embryology, 2010, 115(1/2): 117. [2]. Zhang Q#1, Descamps O#1, Hart MJ1, et al. Paradoxical effect of TrkA inhibition in Alzheimer"s disease models. J Alzheimers Dis. 2014;40(3):605-617. | |
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| Cas No. | 504433-23-2 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | (3Z)-3-[(1-methylindol-3-yl)methylidene]-1H-pyrrolo[3,2-b]pyridin-2-one | ||
| Canonical SMILES | CN1C=C(C2=CC=CC=C21)C=C3C4=C(C=CC=N4)NC3=O | ||
| Formula | C17H13N3O | M.Wt | 275.3 |
| Solubility | ≥13.75mg/mL in DMSO | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
GW441756 is an inhibitor of TrkA kinase and LRRK2 with IC50 value of 320nM and 2nM, respectively [1].
The activity of TrkA kinase can affect its downstream signaling and involves in many biological processes including proliferation, differentiation and apoptosis. Thereby the inhibitor of TrkA is developed for the treatment of cancers. GW441756 belongs to the oxindole series and is found to be a potent inhibitor of TrkA. It is also selective against TrkA. The IC50 values of it for cRaf1 and CDK2 are above 12μM and 7μM, respectively. In human muscle sarcoma cancer cell line HTB114, treatment of GW441756 dose-dependently suppresses neoplastic proliferation and induces apoptosis [1, 2].
In addition, GW441756 is also found to be an LRRK2 inhibitor. It inhibits the Ser935 phosphorylation of LRRK2 in cellular TR-FRET assay with IC50 value of 2.2μM. It shows no significant cytotoxicity with IC50 value of >20μM [3].
References:[1] Wood E R, Kuyper L, Petrov K G, et al. Discovery and in vitro evaluation of potent TrkA kinase inhibitors: oxindole and aza-oxindoles. Bioorganic & medicinal chemistry letters, 2004, 14(4): 953-957.[2] Montagnoli C, Pistilli A, Stabile A M, et al. Anti-proliferative effects of GW441756, a novel inhibitor of NGFreceptor tyrosine kinase a (TRKA), in human sarcoma. Italian Journal of Anatomy and Embryology, 2010, 115(1/2): 117.[3] Hermanson S B, Carlson C B, Riddle S M, et al. Screening for novel LRRK2 inhibitors using a high-throughput TR-FRET cellular assay for LRRK2 Ser935 phosphorylation. PloS one, 2012, 7(8): e43580.
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请各位大侠给予帮助！！
谢谢！！
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氨基类染料是包含自由氨基的活性染料，染料可与活化羧酸衍生物和其他亲电子的试剂结合。比如：氨基与EDC-活化的羧基结合。
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健那绿染液是一种活体染液，实验对象必须是活细胞，健那绿可以使活细胞中的线粒体呈现蓝绿色，而细胞质接近无色。
分子生物学实验的染料主要涉及到核酸染料和蛋白质染料.核酸染料主要有EB（溴化乙锭,高致癌性）,goldview,sybr green（实时定量PCR时常用染料）.这些染料可以和核酸双链分子特异性结合发出强荧光而被检测到.蛋白质染料最常用的是考马斯亮蓝 R-250,硝酸银.其中硝酸银有时也用于核酸染色.
染料分为天然染料和人工染料两种。天然染料有胭脂虫红、地衣素、石蕊和苏木素等，它们多从植物体中提取得到，其成分复杂，有些至今还未搞清楚。目前主要采用人工染料，也称煤焦油染料，多从煤焦油中提取获得，是苯的衍生物。多数染料为带色的有机酸或碱类，难溶于水，而易溶于有机溶剂中。为使它们易溶于水，通常制成盐类。
染料可按其电离后染料离子所带电荷的性质，分为酸性染料、碱性染料、中性（复合）染料和单纯染料四大类。 标本干燥后即进行固定，固定的目的有三个：
1）杀死微生物，固定细胞结构。
2）保证菌体能更牢的粘附在载玻片上，防止标本被水冲洗掉。
3）改变染料对细胞的通透性，因为死的原生质比活的原生质易于染色。
而且样品中的无水硫酸钠未变色,而做标准曲线的五个和空白对照的变为蓝色了,请高手指教,多谢!
还有,是否变蓝对测定结果有影响吗?
谢了哈
欢迎你！请下次规范发贴:)
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2、苏丹三 脂肪 橙红
3、苏丹四 脂肪 红
4、双缩脲 蛋白质 紫
5、龙胆紫 染色质 紫
6、碘 淀粉 蓝
7、健那绿 线粒体 绿
8、甲基绿 DNA 绿
9、吡罗红 RNA 红
10、溴麝香草酚蓝 CO2 由蓝变绿再变黄
11、重铬酸钾 酒精 酸性条件下由橙色变成灰绿
12、醋酸洋红（龙胆紫、改良苯酚品红） 染色质 红
13、台盼蓝 检验活死细胞 死细胞会被染成蓝色（不常用）
