PF-04979064

• CAT Number: I000844
• CAS Number: 1220699-06-8
• Molecular Formula: C24H26N6O3
• Molecular Weight: 446.50
• Purity: ≥95%
• Synonyms: 1-[1-[(2S)-2-hydroxypropanoyl]piperidin-4-yl]-3-methyl-8-(6-methylpyridin-3-yl)imidazo[4,5-c][1,5]naphthyridin-2-one
• InChI: InChI=1S/C24H26N6O3/c1-14-4-5-16(12-25-14)18-6-7-19-21(27-18)22-20(13-26-19)28(3)24(33)30(22)17-8-10-29(11-9-17)23(32)15(2)31/h4-7,12-13,15,17,31H,8-11H2,1-3H3/t15-/m0/s1
• InChIKey: GACQNUHFDBEIQH-HNNXBMFYSA-N
• SMILES: CC1=NC=C(C=C1)C2=NC3=C4C(=CN=C3C=C2)N(C(=O)N4C5CCN(CC5)C(=O)C(C)O)C

PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.
PF-04979064 is tested against human class I PI3K isoforms PI3Kα, PI3Kγ, and PI3Kδ, with PI3Kα Ki of 0.13 nM, PI3Kγ Ki of 0.111 nM, and PI3Kδ Ki of 0.122 nM[1].
PF-04979064 is progressed to rat in vivo PK studies and exhibits robust PK profile: Vdss=5.23 L/kg, Cl=19.3 mL/min/kg, T1/2=1.85 h, and F%=61%[1].

Reference

[1]. Cheng H et al. Discovery of the Highly Potent PI3K/mTOR Dual Inhibitor PF-04979064 through Structure-Based Drug Design. ACS Med Chem Lett, 2012 Nov 7, 4(1):91-7.
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