NVP-BVU972

SKU: orb1305175

Description

NVP-BVU972

Research Area

Signal Transduction

Key Properties

• CAS Number: 1185763-69-2
• MW: 340.38
• Purity: 99.99% (May vary between batches)
• Formula: C₂₀H₁₆N₆
• SMILES: Cn1cc(cn1)-c1ccc2ncc(Cc3ccc4ncccc4c3)n2n1
• Target: c-Met/HGFR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.88 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:63 mg/mL (185.09 mM);DMSO:45 mg/mL (132.21 mM)

Bioactivity

• Target IC50:
  MET:14 nM
• In Vivo:
  NVP-BVU972 effectively inhibited the growth of MET gene-dispersed cell lines GTL-16, MKN-45, and EBC-1 with IC50 of 66, 82, and 32 nM, respectively.NVP-BVU972 effectively inhibited the MET kinase, while the inhibition of other kinases (including the most closely related ones), RON, was very low, with an IC50 of >1000 nM.NVP-BVU972 inhibited GTL-16, MKN-45 and EBC-1 with IC50 of >1000 nM.NVP-BVU972 inhibited GTL-16, MKN-45 and EBC-1 with IC50 of >1000 nM. BVU972 inhibited constitutive MET phosphorylation in GTL-16 cells and HGF-stimulated MET phosphorylation in A549 cells with IC50s of 7.3 and 22 nM, respectively.NVP-BVU972 acted on BaF3 cells expressing wild-type TPR-MET and dose-dependently decreased TPR-MET phosphorylation.
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• Cell Research:
  BaF3 cells containing TPR-MET or various mutants thereof are grown in RPMI 1640 medium containing 10% fetal calf serum. For maintenance of parental BaF3 cells the medium is additionally supplemented with 10 ng/mL interleukin-3 (IL-3). For proliferation assays, BaF3 cells are seeded on 96-well-plates in triplicates at 104 cells per well and incubated with various concentrations of NVP-BVU972 for 72 hours followed by quantification of viable cells using a resazurin sodium salt dye reduction readout. IC50 values are determined with the XLFit Excel Add-In using a 4-parameter dose response model.(Only for Reference)
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HGFR, Inhibitor, MET resistance mutations, Met, NVP BVU972, NVP-BVU 972, NVPBVU972, NVP-BVU972, NVP-BVU-972, inhibit, cMet, c-Met/HGFR, cMet/HGFR, c-Met, cancer, anti-proliferation, BaF3, BaF3 TPR-MET, phosphorylation

Compound Identifiers

PubChem CID

44206063