VX-11e

製品コードS7709 バッチS770901

印刷

化学情報

Chemical Structure Synonyms VTX-11e, Vertex-11e Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C24H20Cl2FN5O2
分子量 500.35 CAS No. 896720-20-0
Solubility (25°C)* 体外 DMSO 100 mg/mL (199.86 mM)
Ethanol 16 mg/mL (31.97 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
5.0mg/ml Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 VX-11e (VTX-11e, Vertex-11e) is a potent, selective, and orally bioavailable ERK inhibitor with IC50 of 17 nM (ERK1) and 15 nM (ERK2), over 200-fold selective over other kinases tested.
in vitro In HT29 cells, VX-11e potently inhibits cell proliferation with IC50 of 48 nM. [1]
in vivo In both rats and mice, VX-11e shows good oral bioavailability. [1] In NSG mice bearing human melanoma RPDX tumors, VX-11e (50 mg/kg, p.o.) results in robust inhibition of pRSK, and inhibits tumor growth. When used in combination with BKM120, VX-11e results in significantly improved tumor growth inhibition. [2]

プロトコル(参考用のみ)

キナーゼアッセイ ERK Inhibition Assay
Compounds are assayed for the inhibition of ERK2 by a spectophotometric coupled-enzyme assay. In this assay, a fixed concentration of activated ERK2 (10 nM) is incubated with various concentrations of the compounds in DMSO (2.5%) for 10 min. at 30 °C 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 is initiated by the addition of 65 μM ATP. The rate of decrease of absorbance at 340 nM is monitored. The IC50 is evaluated from the data as a function of inhibitor concentr
細胞アッセイ 細胞株 HT29 cells
濃度 ~10 μM
反応時間 48 h
実験の流れ Cell proliferation is measured by 3H-thymidine incorporation. The cells are plated at a concentration of 10,000 cells/well in a 96-well plate using growth media, RPMI 1640 containing 10% FBS. Serially diluted compounds are added. The cells and compounds are incubated for 48 hours at 37°C incubator. After 48 hours, 0.4 μCi of 3H-thymidine is added to each wells for 8 hours and returned to the 37°C incubator. The cells are harvested using a Tomtec 96-well cell harvester and the CPM is determined using the Wallac 1205 BETAPLATE liquid scintillation counter. The IC50 is the 50% inhibition of contr
動物実験 動物モデル NSG mice bearing human melanoma RPDX tumors
投薬量 50 mg/kg BID
投与方法 p.o.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

MAPK1 Mediates MAM Disruption and Mitochondrial Dysfunction in Diabetic Kidney Disease via the PACS-2-Dependent Mechanism [ Int J Biol Sci, 2024, 20(2):569-584] PubMed: 38169625
Integrated drug response prediction models pinpoint repurposed drugs with effectiveness against rhabdomyosarcoma [ PLoS One, 2024, 19(1):e0295629] PubMed: 38277404
Kinase-Modulated Bioluminescent Indicators Enable Noninvasive Imaging of Drug Activity in the Brain [ ACS Cent Sci, 2023, 9(4):719-732] PubMed: 37122464
ERK2-topoisomerase II regulatory axis is important for gene activation in immediate early genes [ Nat Commun, 2023, 14(1):8341] PubMed: 38097570
ERK1/2 inhibitors act as monovalent degraders inducing ubiquitylation and proteasome-dependent turnover of ERK2, but not ERK1 [ Biochem J, 2023, 480(9):587-605] PubMed: 37018014
miR-125b-5p-MAPK1-C/EBPα feedback loop regulates all-trans retinoic acid resistance in acute promyelocytic leukemia [ Gene, 2023, 889:147806] PubMed: 37717613
ERK Hyperactivation Serves as a Unified Mechanism of Escape in Intrinsic and Acquired CDK4/6 Inhibitor Resistance in Acral Lentiginous Melanoma [ Res Sq, 2023, rs.3.rs-2817876] PubMed: 37131684
Conformation Selection by ATP-competitive Inhibitors and Allosteric Communication in ERK2 [ bioRxiv, 2023, 2023.09.12.557258] PubMed: 37745518
Identification of cell type-specific correlations between ERK activity and cell viability upon treatment with ERK1/2 inhibitors [ J Biol Chem, 2022, 298(8):102226] PubMed: 35787369
Establishment and characterization of immortalized sweat gland myoepithelial cells [ Sci Rep, 2022, 12(1):7] PubMed: 34997030

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。