Merestinib

SKU: orb1304187

Description

Merestinib

Research Area

Cardiovascular Research, Immunology & Inflammation, Signal Transduction

Key Properties

• CAS Number: 1206799-15-6
• MW: 552.53
• Purity: 99.24%
• Formula: C₃₀H₂₂F₂N₆O₃
• SMILES: O(C1=C(C=C2C(=C1)C=NN2C)C=3C=NNC3)C4=C(F)C=C(NC(=O)C=5C(=O)N(C(C)=CC5)C6=CC=C(F)C=C6)C=C4
• Target: FLT,Discoidin Domain Receptor (DDR),c-Met/HGFR,ROS,ROS Kinase
• Solubility: DMSO:16 mg/mL (28.96 mM);Ethanol:93 mg/mL (168.32 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (5.97 mM)

Bioactivity

• Target IC50:
  MET:2 nM(Ki)
• In Vivo:
  Merestinib shows in vivo anti-tumor effects in MET amplified (MKN45), MET autocrine (U-87 mg, and KP4) and MET over-expressed (H441) xenograft models; and in vivo vessel normalization effects. It is able to induce vessel normalization in xenograft tumors. Amon the species studied, Merestinib ha the shortest elimination half life in mice of 2.9 h, compared with 14.3 h in non-human primate. Merestinib is currently in phase 1 Clinicalal testing in patients with advanced cance.
• In Vitro:
  Merestinib demonstrates in vitro effects on MET pathway-dependent cell scattering and cell proliferation. It demonstrates more potent anti Proliferative activity in cell lines with MET gene amplification (MKN45, Hs746T and H1993) tha the cell lines without MET gene amplification (U-87 mg, KATO-III). Merestinib also maintains potency against 13 MET variants, Each bearing a Single-point mutation. It is found to have potent activity against several Other receptor tyrosine oncokinases including MST1R, FLT3, AXL, MERTK, TEK, ROS1, DDR1/2 and agains the serine/threonine kinases MKNK1/2 the mean IC50 value of Merestinib for Inhibition of MET auto-phosphorylation in HGF-stimulated H460 cells is 35. ± .9 nM an the IC50 for MET auto-phosphorylation in S114 cells is 59.2 n.
• Cell Research:
  × 0^3 DU145 cells/well on poly-D-lysine 96-well black/clear plates are treated with LY2801653 (in 0.4 % DMSO), immediately followed b the addition of human HGF (20 ng/mL), and incubated for 48 h at 37℃. 2 % formaldehyde fixed cells are stained with AlexaFluor 488 Phalloidin and counterstained with Propidium Iodide. Colony counts are quantified on Acumen Explorer laser-scanning fluorescence microplate cytometer. A colony is defined as≥4 cells.(Only for Reference)

Storage & Handling

• Storage: store at low temperature | 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

inhibit, LY2801653, LY-2801653, LY 2801653, Met, Inhibitor, HGFR, Merestinib, FLT3, DDR, Fms like tyrosine kinase 3, DiscoidinDomainReceptor, Discoidin Domain Receptor (DDR), Discoidin Domain Receptor, DiscoidinDomainReceptor(DDR), cMet, c-Met, cMet/HGFR, c-Met/HGFR, Cluster of differentiation antigen 135, CD135, ROS, ROS Kinase, ROSKinase

Compound Identifiers

PubChem CID

44603533