PF06747775

• CAT Number: I010182
• CAS Number: 1776112-90-3
• Molecular Formula: C18H22FN9O2
• Molecular Weight: 415.433
• Purity: ≥95%
• Synonyms: N-((3R,4R)-4-fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidin-3-yl)acrylamide
• Target: EGFR
• Storage: 0 - 4 °C
• IUPAC Name: N-[(3R,4R)-4-fluoro-1-[6-[(3-methoxy-1-methylpyrazol-4-yl)amino]-9-methylpurin-2-yl]pyrrolidin-3-yl]prop-2-enamide
• InChI: InChI=1S/C18H22FN9O2/c1-5-13(29)21-11-8-28(6-10(11)19)18-23-15(14-16(24-18)26(2)9-20-14)22-12-7-27(3)25-17(12)30-4/h5,7,9-11H,1,6,8H2,2-4H3,(H,21,29)(H,22,23,24)/t10-,11-/m1/s1
• InChIKey: JYIUNVOCEFIUIU-GHMZBOCLSA-N
• SMILES: CN1C=C(C(=N1)OC)NC2=NC(=NC3=C2N=CN3C)N4CC(C(C4)F)NC(=O)C=C

PF-06747775(CAT: I010182) is an orally available inhibitor that specifically targets the mutant form of the epidermal growth factor receptor (EGFR) known as T790M. This compound has potential antineoplastic activity, meaning it may be effective in treating certain types of cancer. PF-06747775 demonstrates potent activity against the four common EGFR mutant forms, including exon 19 deletion (Del), L858R, and the double mutants T790M/L858R and T790M/Del. It exhibits selectivity for the mutant EGFR while sparing the wild-type EGFR. Additionally, PF-06747775 possesses desirable absorption, distribution, metabolism, and excretion (ADME) properties, which are important considerations for its therapeutic potential.

Reference

1: Planken S, Behenna DC, Nair SK, Johnson TO, Nagata A, Almaden C, Bailey S,
Ballard TE, Bernier L, Cheng H, Cho-Schultz S, Dalvie D, Deal JG, Dinh DM,
Edwards MP, Ferre RA, Gajiwala KS, Hemkens M, Kania RS, Kath JC, Matthews J,
Murray BW, Niessen S, Orr ST, Pairish M, Sach NW, Shen H, Shi M, Solowiej J, Tran
K, Tseng E, Vicini P, Wang Y, Weinrich SL, Zhou R, Zientek M, Liu L, Luo Y, Xin
S, Zhang C, Lafontaine J. Discovery of
N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-
purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug
Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants
with Selectivity over Wild-Type EGFR. J Med Chem. 2017 Apr 13;60(7):3002-3019.
doi: 10.1021/acs.jmedchem.6b01894. Epub 2017 Mar 29. PubMed PMID: 28287730.