| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
PI3Kα
PI3Kα (phosphoinositide 3-kinase alpha). PI3Kα-IN-11 is a potent inhibitor of PI3Kα. |
|---|---|
| ln Vitro |
HCT116-WT and HCT116-MUT (H1047R) cell lines can be inhibited with IC50 values of 1.1 and 0.73 μM, respectively.
PI3Kα-IN-11 is a potent PI3Kα inhibitor with anticancer activity. By inhibiting PI3Kα, it blocks the PI3K/AKT/mTOR signaling pathway, leading to reduced cell survival, proliferation, and metabolism. |
| ln Vivo |
No detailed in vivo activity data are publicly available for PI3Kα-IN-11. As a potent PI3Kα inhibitor, its in vivo effects would be expected to be related to the inhibition of PI3K signaling, which could lead to reduced tumor growth.
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| Enzyme Assay |
In vitro kinase assays for PI3Kα-IN-11 are performed to evaluate its inhibitory activity against PI3Kα. The kinase is incubated with lipid substrates and ATP in the presence of varying concentrations of the compound. The inhibition of kinase activity is measured, and IC50 values are calculated.
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| Cell Assay |
In vitro cell-based assays are conducted to evaluate the effects of PI3Kα-IN-11 on PI3K/AKT/mTOR signaling and cell viability. Cells are treated with the compound, and AKT phosphorylation and the phosphorylation of downstream targets are measured by Western blotting. Cell viability and proliferation are assessed using standard assays such as MTT or CCK-8.
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| Animal Protocol |
No detailed in vivo animal study protocols are publicly available for PI3Kα-IN-11. In vivo studies would be conducted in animal models, such as tumor xenograft models, to evaluate the antitumor efficacy of the compound.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for PI3Kα-IN-11. The compound is soluble in DMSO.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for PI3Kα-IN-11. As a PI3Kα inhibitor, its toxicity profile would be expected to be related to its mechanism of action.
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| References |
[1]. Sabbah DA, et al.N-Phenyl-4-hydroxy-2-quinolone-3-carboxamides as selective inhibitors of mutant H1047R phosphoinositide-3-kinase (PI3Kα). Bioorg Med Chem. 2012 Dec 15;20(24):7175-83.
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| Additional Infomation |
PI3Kα-IN-11 is a potent PI3Kα inhibitor with anticancer activity. It is a valuable research tool for studying the role of PI3K signaling in cancer and for developing targeted anticancer therapies. The compound is not approved for human therapeutic use and is strictly for research purposes.
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| Molecular Formula |
C17H14N2O3
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|---|---|
| Molecular Weight |
294.30
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| Exact Mass |
294.1
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| CAS # |
300803-79-6
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| PubChem CID |
54680441
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
622.4±55.0 °C at 760 mmHg
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| Flash Point |
330.2±31.5 °C
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| Vapour Pressure |
0.0±1.9 mmHg at 25°C
|
| Index of Refraction |
1.667
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| LogP |
1.04
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
22
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| Complexity |
480
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1C2=C(C=CC=C2)C(O)=C(C(NCC2=CC=CC=C2)=O)C1=O
|
| InChi Key |
WKAZEVUZAKRWHB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H14N2O3/c20-15-12-8-4-5-9-13(12)19-17(22)14(15)16(21)18-10-11-6-2-1-3-7-11/h1-9H,10H2,(H,18,21)(H2,19,20,22)
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| Chemical Name |
N-benzyl-4-hydroxy-2-oxo-1H-quinoline-3-carboxamide
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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 (33.98 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3979 mL | 16.9895 mL | 33.9789 mL | |
| 5 mM | 0.6796 mL | 3.3979 mL | 6.7958 mL | |
| 10 mM | 0.3398 mL | 1.6989 mL | 3.3979 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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