VX-11e
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
VX-11e是一种强效的和选择性的ERK抑制剂[1].
ERK是细胞外信号调节激酶.Ras/Raf/MEK/ERK信号转导是与各种人类癌症相关的致癌通路[1].
参考文献:
[1]. Aronov, Alex M, Tang Q, et al. Martinez-Botella, Gabriel et al. Structure-Guided Design of Potent and Selective Pyrimidylpyrrole Inhibitors of Extracellular Signal-Regulated Kinase (ERK) Using Conformational Control. Journal of Medicinal Chemistry, 2009, 52(20): 6362-6368.
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- 4. Zheng L, Guo Q, et al. "Transcriptional factor six2 promotes the competitive endogenous RNA network between CYP4Z1 and pseudogene CYP4Z2P responsible for maintaining the stemness of breast cancer cells." J Hematol Oncol. 2019 Mar 4;12(1):23. PMID: 30832689
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- 6. Kris Cameron Wood,Peter Saville Winter. "Compositions and Methods for Treating Cancer with JAK2 Activity." US Patent App. 15/027,216, 2016.
- 7. Zheng, Lufeng, et al. "The 3′ UTR of the pseudogene CYP4Z2P promotes tumor angiogenesis in breast cancer by acting as a ceRNA for CYP4Z1." Breast cancer research and treatment (2015): 1-14. PMID: 25701119
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Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 500.35 |
Cas No. | 896720-20-0 |
Formula | C24H20Cl2FN5O2 |
Synonyms | VX 11e, VX11e |
Solubility | ≥25 mg/mL in DMSO; insoluble in H2O; ≥12.65 mg/mL in EtOH with ultrasonic |
Chemical Name | 4-[2-(2-chloro-4-fluoroanilino)-5-methylpyrimidin-4-yl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide |
SDF | Download SDF |
Canonical SMILES | CC1=CN=C(N=C1C2=CNC(=C2)C(=O)NC(CO)C3=CC(=CC=C3)Cl)NC4=C(C=C(C=C4)F)Cl |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
激酶实验 [1]: | |
ERK抑制试验 |
通过分光光度偶联酶试验测定化合物对ERK2的抑制作用。在上述试验中,将固定浓度的活化ERK2 (10 nM) 与不同浓度的化合物(溶于2.5% DMSO)加入到0.1 M HEPES缓冲液(pH = 7.5,含10 mM MgCl2,2.5 mM磷酸烯醇丙酮酸盐,200 μM NADH,150 ?g/mL丙酮酸激酶,50 ?g/mL乳酸脱氢酶和200 ?M erktide多肽)中,将其置于30 ℃孵育10分钟。加入65 ?M ATP开启反应。监测340 nM下的吸光度减少率。根据抑制剂浓度估算IC50值。 |
细胞实验 [1]: | |
细胞系 |
HT29细胞 |
制备方法 |
在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
反应条件 |
≤ 10 μM;48小时 |
实验结果 |
在HT29细胞中,VX-11e有效抑制细胞增殖,其IC50值为48 nM。 |
动物实验 [2]: | |
动物模型 |
携带人黑色素瘤RPDX肿瘤的NSG小鼠 |
给药剂量 |
50 mg/kg;口服给药;每日2次 |
实验结果 |
在携带人黑色素瘤RPDX肿瘤的NSG小鼠中,VX-11e(50 mg/kg,口服给药)有效抑制pRSK和肿瘤生长。当与BKM120联合使用时,VX-11e的肿瘤生长抑制作用显著提高 |
其它注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: [1]. Aronov, Alex M, Tang Q, et al. Martinez-Botella, Gabriel et al. Structure-Guided Design of Potent and Selective Pyrimidylpyrrole Inhibitors of Extracellular Signal-Regulated Kinase (ERK) Using Conformational Control. Journal of Medicinal Chemistry, 2009, 52(20): 6362-6368. [2]. Krepler C, Xiao M, Sproesser K, et al. Personalized Preclinical Trials in BRAF Inhibitor-Resistant Patient-Derived Xenograft Models Identify Second-Line Combination Therapies. Clin Cancer Res. 2016 Apr 1;22(7):1592-602. |
质量控制和MSDS
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