| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
mTOR 0.42 nM (IC50) PI3Kα 8 nM (IC50) PI3Kβ 24 nM (IC50) PI3Kγ 74 nM (IC50) PI3Kδ 77 nM (IC50) E545K 14 nM (IC50) H1047R 77 nM (IC50)
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|---|---|
| ln Vitro |
PKI-179 reduces the growth of cells, exhibiting IC50 values for MDA361 and PC3 cells of 22 nM and 29 nM, respectively[1]. At dosages up to >30 μM, PKI-179 exhibits inhibitory activity against a panel of 361 different kinases, hERG, and cytochrome P450 (CYP) isoforms; nevertheless, it does exhibit activity for CYP2C8 (IC50=3 μM)[1].
|
| ln Vivo |
In nude mice bearing MDA-361 human breast cancer tumors, PKI-179 (5-50 mg/kg; po once daily for 40 days) reduces the tumor growth and is well tolerated[1]. Good suppression of PI3K signaling is observed in nude mice containing MDA361 tumor xenografts when PKI-179 (50 mg/kg; po) is administered[1]. PKI-179 has a high half-life (>60 min) and good oral bioavailability (98% in naked mouse, 46% in rat, 38% in monkey, and 61% in dog)[1].
|
| 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: Ip every 3 days for 4 weeks Experimental Results: demonstrated pronounced tumor growth arrest when dosed above 10 mg/kg. No significant weight loss of tested animals was observed for all different dosages. |
| 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 |
C25H29CLN8O3
|
|---|---|
| Molecular Weight |
525.00
|
| CAS # |
1463510-35-1
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| Related CAS # |
PKI-179;1197160-28-3
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
| SMILES |
N(C1C=CC(C2N=C(N3CCOCC3)N=C(N3C4COCC3CC4)N=2)=CC=1)C(=O)NC1=CC=NC=C1.Cl
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: 20 mg/mL (38.10 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.38 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 12.5 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: ≥ 1.25 mg/mL (2.38 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 12.5 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 | 1.9048 mL | 9.5238 mL | 19.0476 mL | |
| 5 mM | 0.3810 mL | 1.9048 mL | 3.8095 mL | |
| 10 mM | 0.1905 mL | 0.9524 mL | 1.9048 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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