1. Protein Tyrosine Kinase/RTK
  2. c-Met/HGFR
  3. NVP-BVU972

NVP-BVU972 

Cat. No.: HY-15456 Purity: 98.38%
Handling Instructions

NVP-BVU972 is a selective and potent Met inhibitor (IC50 = 14 nM). Antitumor agents.

For research use only. We do not sell to patients.

NVP-BVU972 Chemical Structure

NVP-BVU972 Chemical Structure

CAS No. : 1185763-69-2

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 264 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 264 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 240 In-stock
Estimated Time of Arrival: December 31
10 mg USD 378 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1020 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Description

NVP-BVU972 is a selective and potent Met inhibitor (IC50 = 14 nM). Antitumor agents. IC50 value: 14 nM [1] Target: Met NVP-BVU972 potently inhibits MET kinase but displays low inhibition against other kinases including the most closely related kinase RON with IC50 values of more than 1000 nM. NVP-BVU972 also suppresses constitutive MET phosphorylation in GTL-16 cells or HGF-stimulated MET phosphorylation in A549 cells with IC50 values of 7.3 nM and 22 nM, respectively. NVP-BVU972 potently prevents the growth of the MET gene amplified cell lines GTL-16, MKN-45 and EBC-1 with IC50 values of 66 nM, 82 nM and 32 nM, respectively. In line with their high frequency in the NVP-BVU972 screen, Y1230 and D1228 mutations give rise to dramatic shifts in the measured IC50 values for NVP-BVU972 in BaF3 cell line. Resistance triggered by V1155L is more limited to NVP-BVU972. A dose-dependent reduction in TPR-MET phosphorylation when applying NVP-BVU972 to BaF3 cells expressing wild-type TPR-MET. Both Y1230H and D1228A mutations abrogated the effect of NVP-BVU972 but not AMG 458. However, F1200I and L1195V interferes with the potency of NVP-BVU972 to prevent TPR-MET phosphorylation.

Molecular Weight

340.38

Formula

C₂₀H₁₆N₆

CAS No.
SMILES

CN1N=CC(C2=NN3C(C=C2)=NC=C3CC4=CC=C(N=CC=C5)C5=C4)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (293.79 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9379 mL 14.6895 mL 29.3789 mL
5 mM 0.5876 mL 2.9379 mL 5.8758 mL
10 mM 0.2938 mL 1.4689 mL 2.9379 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.34 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.34 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

NVP-BVU972c-Met/HGFRInhibitorinhibitorinhibit

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Product Name:
NVP-BVU972
Cat. No.:
HY-15456
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