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Purity: ≥98%
PF-04979064 is a novel, potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, Oncologists have focused a lot of their research on PI3K, AKT, and mTOR, three important kinases from the PI3K signaling pathway, to treat a variety of cancers. A tricyclic imidazo[1,5]naphthyridine series lead optimization effort was conducted in order to find a structurally distinct back-up candidate to PF-04691502, which is currently being tested for the treatment of solid tumors in phase I/II clinical trials. The combination of structure-based drug design and physical property-based optimization led to the development of the potent and specific PI3K/mTOR dual kinase inhibitor PF-04979064.
Targets |
PI3Kα (Ki = 0.13 nM); PI3Kγ (Ki = 0.111 nM); PI3Kδ (Ki = 0.122 nM); mTOR (Ki = 1.42 nM)
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ln Vitro |
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].
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ln Vivo |
The in vivo PK profile of PF-04979064 in rats shows progress, showing Vdss=5.23 L/kg, Cl=19.3 mL/min/kg, T1/2=1.85 h, and F%=61%[1].
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References |
Molecular Formula |
C24H26N6O3
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Molecular Weight |
446.5016
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Exact Mass |
446.2066
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Elemental Analysis |
C, 64.56; H, 5.87; N, 18.82; O, 10.75
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CAS # |
1220699-06-8
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Related CAS # |
1220699-06-8
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Appearance |
Solid powder
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SMILES |
CC1=NC=C(C=C1)C2=NC3=C4C(=CN=C3C=C2)N(C(=O)N4C5CCN(CC5)C(=O)[C@H](C)O)C
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InChi Key |
GACQNUHFDBEIQH-HNNXBMFYSA-N
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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
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Chemical Name |
1-[1-[(2S)-2-hydroxypropanoyl]piperidin-4-yl]-3-methyl-8-(6-methylpyridin-3-yl)imidazo[4,5-c][1,5]naphthyridin-2-one
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Synonyms |
PF-04979064; PF 04979064; PF04979064
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~10 mg/mL (~22.4 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.24 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (2.24 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (2.24 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2396 mL | 11.1982 mL | 22.3964 mL | |
5 mM | 0.4479 mL | 2.2396 mL | 4.4793 mL | |
10 mM | 0.2240 mL | 1.1198 mL | 2.2396 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.