VX-11e

SKU: orb1304470

Description

VX-11e

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 896720-20-0
• MW: 500.35
• Purity: 98.92%
• Formula: C₂₄H₂₀Cl₂FN₅O₂
• SMILES: Cc1cnc(Nc2ccc(F)cc2Cl)nc1-c1c[nH]c(c1)C(=O)N[C@H](CO)c1cccc(Cl)c1
• Target: CDK,FLT,Aurora Kinase,ERK,GSK-3
• Solubility: Ethanol:12.5 mg/mL (24.98 mM);DMSO:50 mg/mL (99.93 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2.5 mg/mL (5 mM)

Bioactivity

• Target IC50:
  CDK2:852 (Ki)|Aurora A:540 (Ki)|ERK2:<2 nM(Ki)|GSK-3:395 (Ki)
• In Vivo:
  In both rats and mice, VX-11e shows good oral bioavailability. 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.
• In Vitro:
  In HT29 cells, VX-11e potently inhibits cell proliferation with IC50 of 48 nM.
• Cell Research:
  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(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GSK-3, GSK3, FLT3, ERK, ERK2, Extracellular signal regulated kinases, inhibit, Inhibitor, AuroraKinase, Aurora A, Aurora Kinase, CDK2, TCS ERK 11e, VTX-11e, Vertex-11e, VX11e, VX-11e, VX 11e

Compound Identifiers

PubChem CID

11634725