PF-9366
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 526342

CAS#: 72882-78-1

Description: PF-9366 is a novel inhibitor of human methionine adenosyltransferase 2A (Mat2A), the extrahepatic isoform.

Chemical Structure

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PF-9366
CAS# 72882-78-1
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 526342
Name: PF-9366
CAS#: 72882-78-1
Chemical Formula: C20H19ClN4
Exact Mass: 350.13
Molecular Weight: 350.850
Elemental Analysis: C, 68.47; H, 5.46; Cl, 10.10; N, 15.97

Price and Availability

Size Price Availability Quantity
10mg USD 150 Ready to ship
25mg USD 250 Ready to ship
50mg USD 450 Ready to ship
100mg USD 750 Ready to ship
200mg USD 1350 Ready to ship
500mg USD 2850 2 Weeks
1g USD 3850 2 Weeks
2g USD 6250 2 Weeks
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Synonym: PF-9366; PF 9366; PF9366.

IUPAC/Chemical Name: 2-(7-Chloro-5-phenyl-[1,2,4]triazolo[4,3-a]quinolin-1-yl)-N,N-dimethylethan-1-amine

InChi Key: LYLASWLQCMKZAT-UHFFFAOYSA-N

InChi Code: InChI=1S/C20H19ClN4/c1-24(2)11-10-19-22-23-20-13-16(14-6-4-3-5-7-14)17-12-15(21)8-9-18(17)25(19)20/h3-9,12-13H,10-11H2,1-2H3

SMILES Code: CN(C)CCC1=NN=C2N1C3=C(C=C(Cl)C=C3)C(C4=CC=CC=C4)=C2

Appearance: Solid powder

Purity: >96% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target: PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor, with an IC50 of 420 nM and a Kd of 170 nM.
In vitro activity: Untreated (DMSO control) CRISPR/Cas9-MLLr cells presented an immature morphology whereas treatment with PF-9366 resulted in macrophage-like cells with an increase of apoptotic cells consistent with the upregulation of CD14 expression (Figure 4A,B). Consistently, a trend to downregulate the target gene expression of MEIS1 and HOXA9 upon PF-9366 treatment was observed, irrespective of day 4 or 6, although significance was not reached in all performed experiments (Figure 4C). These data suggest that the inhibition of MAT2A results in cell differentiation, induction of cell cycle arrest, and finally apoptosis in MLL fusion protein-driven leukemogenesis without any impact on control cells. Reference: Cancers (Basel). 2020 May; 12(5): 1342. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7281730/
In vivo activity: TBD

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 2.0 5.70

Preparing Stock Solutions

The following data is based on the product molecular weight 350.85 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Secker KA, Bloechl B, Keppeler H, Duerr-Stoerzer S, Schmid H, Schneidawind D, Jeong J, Hentrich T, Schulze-Hentrich JM, Schneidawind C. MAT2A as Key Regulator and Therapeutic Target in MLLr Leukemogenesis. Cancers (Basel). 2020 May 24;12(5):1342. doi: 10.3390/cancers12051342. PMID: 32456310; PMCID: PMC7281730. 2. Quinlan CL, Kaiser SE, Bolaños B, Nowlin D, Grantner R, Karlicek-Bryant S, Feng JL, Jenkinson S, Freeman-Cook K, Dann SG, Wang X, Wells PA, Fantin VR, Stewart AE, Grant SK. Targeting S-adenosylmethionine biosynthesis with a novel allosteric inhibitor of Mat2A. Nat Chem Biol. 2017 Jul;13(7):785-792. doi: 10.1038/nchembio.2384. Epub 2017 May 29. PMID: 28553945.
In vitro protocol: 1. Secker KA, Bloechl B, Keppeler H, Duerr-Stoerzer S, Schmid H, Schneidawind D, Jeong J, Hentrich T, Schulze-Hentrich JM, Schneidawind C. MAT2A as Key Regulator and Therapeutic Target in MLLr Leukemogenesis. Cancers (Basel). 2020 May 24;12(5):1342. doi: 10.3390/cancers12051342. PMID: 32456310; PMCID: PMC7281730. 2. Quinlan CL, Kaiser SE, Bolaños B, Nowlin D, Grantner R, Karlicek-Bryant S, Feng JL, Jenkinson S, Freeman-Cook K, Dann SG, Wang X, Wells PA, Fantin VR, Stewart AE, Grant SK. Targeting S-adenosylmethionine biosynthesis with a novel allosteric inhibitor of Mat2A. Nat Chem Biol. 2017 Jul;13(7):785-792. doi: 10.1038/nchembio.2384. Epub 2017 May 29. PMID: 28553945.
In vivo protocol: TBD

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1: Quinlan CL, Kaiser SE, Bolaños B, Nowlin D, Grantner R, Karlicek-Bryant S, Feng JL, Jenkinson S, Freeman-Cook K, Dann SG, Wang X, Wells PA, Fantin VR, Stewart AE, Grant SK. Targeting S-adenosylmethionine biosynthesis with a novel allosteric inhibitor of Mat2A. Nat Chem Biol. 2017 May 29. doi: 10.1038/nchembio.2384. [Epub ahead of print] PubMed PMID: 28553945.