WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H525950
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.
Hodoodo Cat#: H525950
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
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:
Biological target: | |
In vitro activity: | |
In vivo activity: |
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.
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: | |
In vitro protocol: | |
In vivo protocol: |
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.