PZ0403

PF-9366

≥98% (HPLC)

• Synonym(s): 7-Chloro-N,N-dimethyl-5-phenyl-[1,2,4]triazolo[4,3-a]quinoline-1-ethanamine, PF 9366, PF9366
• Empirical Formula (Hill Notation): C₂₀H₁₉ClN₄
• CAS Number: 72882-78-1
• Molecular Weight: 350.84
• UNSPSC Code: 51111800
• NACRES: NA.77
• MDL number: MFCD31630724
• Assay: ≥98% (HPLC)
• Form: powder

Properties

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: room temp
• SMILES string: ClC(C=C1)=CC(C(C2=CC=CC=C2)=C3)=C1N4C3=NN=C4CCN(C)C
• 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
• InChI key: LYLASWLQCMKZAT-UHFFFAOYSA-N

Description

Biochem/physiol Actions

PF-9366 is a methionine adenosyltransferase 2A allosteric inhibitor (human Mat2A IC₅₀/K_d = 420 nM/170 nM) whose binding site overlaps with that of the Mat2A regulator, Mat2B. PF-9366 inhibits cellular SAM production in a Mat2B-competitive manner (IC₅₀ post 6-hr treatment = 1.2 μM wihout vs. 0.86 μM with Mat2B knockdown; H520 lung carcinoma cells) without antiproliferation efficacy in cancer cultures due to an induction of Mat2A upregulation upon allosteric inhibition. Similar to Mat2B, PF-9366 allosteric binding alters Mat2A active site, causing increased substrate affinity and decreased enzyme turnover.

Safety Information

• Storage Class: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable