PF-04979064
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MedKoo CAT#: 525950

CAS#: 1220699-06-8

Description: PF-04979064 is a potent and selective PI3K/mTOR inhibitor. PF-04979064 regulates tumor growth in gastric cancer and enhances drug sensitivity of gastric cancer cells to 5-FU. F-04979064 significantly inhibited the proliferation of human gastric adenocarcinoma AGS cells and the undifferentiated GC cell line HGC-27, promoting cell apoptosis. Combination treatment with PF-04979064 and the GC first-line clinical drug 5-FU showed synergistic effects, and PF-04979064 markedly increased the sensitivity of GC cells to chemotherapy drugs. Western blot results showed that PF-04979064 significantly inhibited the PI3K/AKT/mTOR signaling pathway in GC cells, whereas RNA seq results demonstrated substantial alterations in gene expression profiles upon treatment with PF-04979064.

Chemical Structure

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PF-04979064
CAS# 1220699-06-8
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 525950
Name: PF-04979064
CAS#: 1220699-06-8
Chemical Formula: C24H26N6O3
Exact Mass: 446.21
Molecular Weight: 446.511
Elemental Analysis: C, 64.56; H, 5.87; N, 18.82; O, 10.75

Price and Availability

Size Price Availability Quantity
10mg USD 250 2 Weeks
25mg USD 450 2 Weeks
50mg USD 750 2 Weeks
100mg USD 1250 2 Weeks
1g USD 6450 2 Weeks
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Synonym: PF-04979064; PF 04979064; PF04979064.

IUPAC/Chemical Name: 2H-Imidazo(4,5-C)(1,5)naphthyridin-2-one, 1,3-dihydro-1-(1-((2S)-2-hydroxy-1-oxopropyl)-4-piperidinyl)-3-methyl-8-(6-methyl-3-pyridinyl)-

InChi Key: GACQNUHFDBEIQH-HNNXBMFYSA-N

InChi Code: 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

SMILES Code: O=C(N1C2CCN(C([C@@H](O)C)=O)CC2)N(C)C3=C1C4=NC(C5=CC=C(C)N=C5)=CC=C4N=C3

Appearance: Solid powder

Purity: >98% (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:

Product Data:
Product Data
Instruction:
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Biological target: 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
In vitro activity: Integration of structure-based drug design and physical properties-based optimization yielded a potent and selective PI3K/mTOR dual kinase inhibitor PF-04979064. This manuscript discusses the lead optimization for the tricyclic series, which both improved the in vitro potency and addressed a number of ADMET issues including high metabolic clearance mediated by both P450 and aldehyde oxidase (AO), poor permeability, and poor solubility. Reference: ACS Med Chem Lett. 2012 Nov 7;4(1):91-7. https://pubmed.ncbi.nlm.nih.gov/24900568/
In vivo activity: Male C57BL/6 mice were randomly divided into sham, model, and PI3K inhibitor groups. Mice were exposed to PM2.5 for 4 weeks to establish an in vivo COPD model. In mice with COPD induced by PM2.5, the PI3K inhibitor PF-04979064 suppressed protein expression of PI3K, p-AKT, and p-mTOR to increase apoptosis of alveolar epithelial cells and reduce autophagy. Reference: J Int Med Res. 2020 Jul;48(7):300060520927919. https://pubmed.ncbi.nlm.nih.gov/32715876/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 10.0 22.40

Preparing Stock Solutions

The following data is based on the product molecular weight 446.51 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. Cheng H, Li C, Bailey S, Baxi SM, Goulet L, Guo L, Hoffman J, Jiang Y, Johnson TO, Johnson TW, Knighton DR, Li J, Liu KK, Liu Z, Marx MA, Walls M, Wells PA, Yin MJ, Zhu J, Zientek M. 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. doi: 10.1021/ml300309h. PMID: 24900568; PMCID: PMC4027523. 2. Zhang F, Ma H, Wang ZL, Li WH, Liu H, Zhao YX. The PI3K/AKT/mTOR pathway regulates autophagy to induce apoptosis of alveolar epithelial cells in chronic obstructive pulmonary disease caused by PM2.5 particulate matter. J Int Med Res. 2020 Jul;48(7):300060520927919. doi: 10.1177/0300060520927919. PMID: 32715876; PMCID: PMC7385846.
In vitro protocol: 1. Cheng H, Li C, Bailey S, Baxi SM, Goulet L, Guo L, Hoffman J, Jiang Y, Johnson TO, Johnson TW, Knighton DR, Li J, Liu KK, Liu Z, Marx MA, Walls M, Wells PA, Yin MJ, Zhu J, Zientek M. 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. doi: 10.1021/ml300309h. PMID: 24900568; PMCID: PMC4027523.
In vivo protocol: 1. Zhang F, Ma H, Wang ZL, Li WH, Liu H, Zhao YX. The PI3K/AKT/mTOR pathway regulates autophagy to induce apoptosis of alveolar epithelial cells in chronic obstructive pulmonary disease caused by PM2.5 particulate matter. J Int Med Res. 2020 Jul;48(7):300060520927919. doi: 10.1177/0300060520927919. PMID: 32715876; PMCID: PMC7385846.

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1: Zhong Z, Wang T, Zang R, Zang Y, Feng Y, Yan S, Geng C, Zhu N, Wang Q. Dual PI3K/mTOR inhibitor PF-04979064 regulates tumor growth in gastric cancer and enhances drug sensitivity of gastric cancer cells to 5-FU. Biomed Pharmacother. 2023 Dec 29;170:116086. doi: 10.1016/j.biopha.2023.116086. Epub ahead of print. PMID: 38159377.


2: Zhang F, Ma H, Wang ZL, Li WH, Liu H, Zhao YX. The PI3K/AKT/mTOR pathway regulates autophagy to induce apoptosis of alveolar epithelial cells in chronic obstructive pulmonary disease caused by PM2.5 particulate matter. J Int Med Res. 2020 Jul;48(7):300060520927919. doi: 10.1177/0300060520927919. PMID: 32715876; PMCID: PMC7385846.


3: Cheng H, Li C, Bailey S, Baxi SM, Goulet L, Guo L, Hoffman J, Jiang Y, Johnson TO, Johnson TW, Knighton DR, Li J, Liu KK, Liu Z, Marx MA, Walls M, Wells PA, Yin MJ, Zhu J, Zientek M. 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. doi: 10.1021/ml300309h. PMID: 24900568; PMCID: PMC4027523.