PF-9366

Name: PF-9366
Brand: MedChemExpress
SKU: HY-107778
Rating: 5.0 (14 reviews)

Cat. No.: HY-107778 Purity: 99.98%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

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

PF-9366 Chemical Structure

CAS No. : 72882-78-1

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 165	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 165	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 330	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 14 publication(s) in Google Scholar

14 Publications Citing Use of MCE PF-9366

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Description

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

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

Molecular Weight

350.84

Formula

C₂₀H₁₉ClN₄

CAS No.

72882-78-1

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 10 mg/mL (28.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.13 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (7.13 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.98%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (253 KB) HNMR (203 KB) RP-HPLC (234 KB) MS (67 KB)

Handling Instructions (2659 KB)

References

[1]. Quinlan CL, et al. Targeting S-adenosylmethionine biosynthesis with a novel allosteric inhibitor of Mat2A. Nat Chem Biol. 2017 Jul;13(7):785-792. [Content Brief]

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	[1]. Quinlan CL, et al. Targeting S-adenosylmethionine biosynthesis with a novel allosteric inhibitor of Mat2A. Nat Chem Biol. 2017 Jul;13(7):785-792. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.8503 mL	14.2515 mL	28.5030 mL	71.2576 mL
	5 mM	0.5701 mL	2.8503 mL	5.7006 mL	14.2515 mL
	10 mM	0.2850 mL	1.4252 mL	2.8503 mL	7.1258 mL
	15 mM	0.1900 mL	0.9501 mL	1.9002 mL	4.7505 mL
	20 mM	0.1425 mL	0.7126 mL	1.4252 mL	3.5629 mL
	25 mM	0.1140 mL	0.5701 mL	1.1401 mL	2.8503 mL

PF-9366 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-936672882-78-1PF9366PF 9366Methionine Adenosyltransferase (MAT)S-adenosylmethionine SynthetaseInhibitorinhibitorinhibit

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PF-9366

Customer Review

PF-9366 Related Antibodies

14 Publications Citing Use of MCE PF-9366

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

PF-9366 Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

PF-9366 Related Classifications

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