PF-9366

SKU: orb1302010

Description

PF-9366 is a potent and selective small molecule inhibitor of methionine adenosyltransferase 2A (MAT2A), exhibiting an IC50 of 420 nM and a Kd of 170 nM. It is a valuable chemical probe for researching methyl metabolism in cancers, with utility in both in vitro biochemical assays and in vivo xenograft studies.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 72882-78-1
• MW: 350.84
• Purity: >99.99% (May vary between batches)
• Formula: C₂₀H₁₉ClN₄
• SMILES: CN(C)CCc1nnc2cc(-c3ccccc3)c3cc(Cl)ccc3n12
• Target: Methionine Adenosyltransferase (MAT)
• Solubility: DMSO:20 mg/mL (57.01 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.7 mM)

Bioactivity

• Target IC50:
  Mat2A:420 nM (cell free)
• In Vitro:
  H520 lung carcinoma cells were treated with PF-9366 for 6 h. PF-9366 inhibited cellular SAM production with an IC50 of 1.2 μM. The IC50s of PF-9366 was modestly decreased in the H520 cells with Mat2B knockdown, to 0.86 mM. Huh-7 cells were more sensitive to compound exposure than the H520 cell line. After 6-h exposure to PF-9366, the IC50 for SAM synthesis inhibition was 225 nM.
• Cell Research:
  Huh-7 cells are seeded at a concentration of 15,000 cells per well for 6-h incubation with compound (PF-9366) and 4,000 cells per well for 72-h incubation with the compound in 96-well plates in 200 μL of growth medium. NCI-H520 MAT2B knockdown cells are seeded at a concentration of 20,000 cells per well for 6 h incubation or 10,000 cells per well for 72 h incubation with the compound in 96 well plates in 200 μL of growth medium. Cells are allowed to attach overnight at 37°C with 5% CO2. A 5× solution of cycloleucine is prepared fresh from powder stock in the growth medium. Other compounds (PF-9366) are diluted in 100% DMSO using a three-fold dilution scheme and further diluted in growth medium to give 0.5% DMSO final. Consistency of cellular confluence for each cell line is monitored with the IncuCyte Zoom live cell imager. Proliferation is measured using CellTiterGlo reagent. Growth media is removed from the cell plates following compound treatment and 80 μL/well CellTiter Glo diluted 1:1 in PBS added.

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

MAT, Mat2A, Inhibitor, MethionineAdenosyltransferase, MethionineAdenosyltransferase(MAT), Methionine Adenosyltransferase, Methionine Adenosyltransferase (MAT), inhibit, PF 9366, PF9366, PF-9366

Compound Identifiers

PubChem CID

12612431