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 is a potent and selective inhibitor of ERK [1].
ERK is extracellular signal-regulated kinases. The Ras/Raf/MEK/ERK signal transduction is an oncogenic pathway related to a variety of human cancers [1].
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.
- 1. Jingman Li, Yuchen Pan, et al. "Urokinase-type plasminogen activator receptor is required for impairing toll-like receptor 7 signaling on macrophage efferocytosis in lupus." Mol Immunol. 2020 Nov;127:38-45. PMID:32911323
- 2. 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
- 3. Gao L, Guo Q, et al. "MiR-873/PD-L1 axis regulates the stemness of breast cancer cells." EBioMedicine. 2019 Feb 22. pii: S2352-3964(19)30112-4. PMID:30803931
- 4. Kris Cameron Wood,Peter Saville Winter. "Compositions and Methods for Treating Cancer with JAK2 Activity." US Patent App. 15/027,216, 2016.
- 5. 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
- 6. Winter PS, et al. "RAS signaling promotes resistance to JAK inhibitors by suppressing BAD-mediated apoptosis." Sci Signal. 2014 Dec 23. PMID:25538080
| 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, ≥12.65 mg/mL in EtOH with ultrasonic, insoluble in H2O |
| 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 |
| Shipping Condition | Evaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request. |
| General tips | For obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months. |
| Kinase experiment [1]: | |
|
ERK inhibition assay |
Compounds were assayed for the inhibition of ERK2 by a spectophotometric coupled-enzyme assay. In this assay, a fixed concentration of activated ERK2 (10 nM) was incubated with various concentrations of the compounds in DMSO (2.5%) for 10 mins at 30 ℃ in 0.1 M HEPES buffer, pH = 7.5, containing 10 mM MgCl2, 2.5 mM phosphoenolpyruvate, 200 μM NADH, 150 μg/mL pyruvate kinase, 50 μg/mL lactate dehydrogenase and 200 μM erktide peptide. The reaction was initiated by the addition of 65 μM ATP. The rate of decrease of absorbance at 340 nM was monitored. The IC50 was evaluated from the data as a function of inhibitor concentration. |
| Cell experiment [1]: | |
|
Cell lines |
HT29 cells |
|
Preparation method |
The solubility of this compound in DMSO is >10 mM. 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. |
|
Reaction Conditions |
≤ 10 μM; 48 hrs |
|
Applications |
In HT29 cells, VX-11e potently inhibited cell proliferation with an IC50 value of 48 nM. |
| Animal experiment [2]: | |
|
Animal models |
NSG mice bearing human melanoma RPDX tumors |
|
Dosage form |
50 mg/kg; p.o.; b.i.d. |
|
Applications |
In NSG mice bearing human melanoma RPDX tumors, VX-11e (50 mg/kg, p.o.) potently inhibited pRSK and tumor growth. VX-11e, combined with BKM120, resulted in significantly improved tumor growth inhibition. |
|
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]. 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. | |
Quality Control & MSDS
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