| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
With IC50 values of 22 nM and 29 nM for MDA361 and PC3 cells, respectively, PKI-179 suppresses cell growth [1]. PKI-179 is active against CYP2C8 (IC50=3 μM) but inactive against a panel of 361 additional kinases, hERG, and cytochrome P450 (CYP) isoforms at concentrations up to >30 μM [1].
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| ln Vivo |
PKI-179 (5-50 mg/kg; taken orally once daily for 40 days) inhibits tumor growth and is well tolerated in nude mice bearing MDA-361 human breast cancer tumors [1]. PKI-179 (50 mg/kg; orally) exerts favorable inhibitory effects on PI3K signaling in nude mice bearing MDA361 tumor xenografts [1]. PKI-179 has good oral bioavailability (98% in nude mice, 46% in rats, 38% in monkeys, and 61% in dogs) and a long half-life (>60 minutes) [1].
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| Animal Protocol |
Animal/Disease Models: Nude mice bearing MDA-361 human breast cancer tumors [1] Doses: 5, 10, 25, 50 mg/kg
Route of Administration: intraperitoneal (ip) injection every 3 days for 4 weeks Experimental Results: Doses exceeding 10 mg /kg, demonstrated significant tumor growth arrest. For all different doses, no significant weight loss was observed in the test animals. |
| References |
[1]. Venkatesan AM, et, al. PKI-179: an orally efficacious dual phosphatidylinositol-3-kinase (PI3K)/mammalian target of rapamycin (mTOR) inhibitor. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5869-73.
[2]. Rehan M. A structural insight into the inhibitory mechanism of an orally active PI3K/mTOR dual inhibitor, PKI-179 using computational approaches. J Mol Graph Model. 2015 Nov;62:226-234. |
| Molecular Formula |
C25H28N8O3
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|---|---|
| Molecular Weight |
488.54162
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| Exact Mass |
488.22844
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| CAS # |
1197160-28-3
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| Related CAS # |
PKI-179 hydrochloride;1463510-35-1
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| SMILES |
C1=C(C=CC(=C1)NC(=O)N=C2C=CNC=C2)C3=NC(=NC(=N3)N4C5CCC4COC5)N6CCOCC6
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| Synonyms |
PK I179; PKI-179; PKI179
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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 : ~100 mg/mL (~204.69 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.12 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 25.0 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.12 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0469 mL | 10.2346 mL | 20.4692 mL | |
| 5 mM | 0.4094 mL | 2.0469 mL | 4.0938 mL | |
| 10 mM | 0.2047 mL | 1.0235 mL | 2.0469 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.
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