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PF-9366 

Cat. No.: HY-107778 Purity: 97.01%
Handling Instructions

PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor, with an IC50 of 420 nM and a Kd of 170 nM.

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

PF-9366 Chemical Structure

PF-9366 Chemical Structure

CAS No. : 72882-78-1

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 165 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
25 mg USD 520 In-stock
Estimated Time of Arrival: December 31
50 mg USD 920 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1550 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor, with an IC50 of 420 nM and a Kd of 170 nM.

IC50 & Target

IC50: 420 nM (Mat2A)[1]
Kd: 170 nM (Mat2A)[1]

In Vitro

PF-9366 is a Mat2A inhibitor, with an IC50 of 420 nM and a Kd of 170 nM. PF-9366 displays no substantial off-target activity in GPCRs, neurotransporters, phosphodiesterases, and ion channels. PF-9366 has inhibitory activity against Mat2A in cancer cells. PF-9366 inhibits cellular S-Adenosyl-L-methionine (SAM) production with an IC50 of 1.2 μM in H520 lung carcinoma cells. PF-9366 is more potent in Huh-7 cells against SAM synthesis, with an IC50 of 255 nM, and also suppresses the proliferation of cells with an IC50 of 10 μM.

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (71.26 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8503 mL 14.2515 mL 28.5030 mL
5 mM 0.5701 mL 2.8503 mL 5.7006 mL
10 mM 0.2850 mL 1.4252 mL 2.8503 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

The Mat2A and Mat2B proteins are extensively dialyzed into a buffer containing 150 mM KCl, 25 mM HEPES, pH 7.4, 5 mM MgCl2, 5% (v/v) glycerol, 2 mM TCEP. Concentrations are determined spectrophotometrically using an ɛ280 of 44,350 /M.cm for Mat2A and an ɛ280 of 36,440 /M.cm for Mat2B. Compounds (PF-9366) are diluted from 100% DMSO stocks into a buffer without DMSO. In a typical experiment, nineteen 15 μL injections of 200 μM compound or 30-35 μM Mat2B are made into 10 μM Mat2A on a VP ITC or nineteen 2 μL injections of 200 μM compound into 10 μM Mat2A on an Auto iTC200. Data are analyzed and fit to a simple 1:1 binding model[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

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 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 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 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. Luminescence is measured by an Plate Reader[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

350.84

Formula

C₂₀H₁₉ClN₄

CAS No.

72882-78-1

SMILES

CN(C)CCC1=NN=C2N1C3=CC=C(Cl)C=C3C(C4=CC=CC=C4)=C2

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
PF-9366
Cat. No.:
HY-107778
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PF-9366

Cat. No.: HY-107778