| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| ln Vitro |
PI3Kα-IN-9 (compound 27) (0-8 μM; 72 hours; cancer cell line) inhibits proliferation and triggers apoptosis [1]. Compound 27 (PI3Kα-IN-9) (0-8 μM; MGC-803 cells) suppresses the expression of p-AKT, p-P70S6 K, PI3K downstream proteins, and PI3Kα protein [1]. Finding the viability of cells[1]
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|---|---|
| ln Vivo |
Compound 27, also known as PI3Kα-IN-9, has a high degree of bioavailability (130%) and good stability (T1/2>10 hours) when administered orally and intravenously to male Sprague-Dawley rats (1–10 mg/kg) for a 24-hour period[1]. Compound 27, orally administered at a dose of 30 mg/kg every day for three weeks to male BALB/c nude mice, possesses low cytotoxicity and antitumor activity [1].
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| Cell Assay |
Cell viability detection[1]
Cell Types: MGC-803 (gastric cancer), SKOV-3 (ovarian cancer), PC-3 (prostate cancer), MCF-7 (breast cancer), MDA-MB-231 (triple negative) breast cancer), HepG2 (liver cancer), RPMI8226 (multiple myeloma), K562 (chronic myeloid leukemia), U251 (glioma), and MOLT-4 (acute lymphoblastic leukemia) cell lines Tested Concentrations: 0-2 μM for Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited the growth of various cancer cells with IC50 values ranging from 0.43 to 1.33 μM. Apoptosis analysis [1] Cell Types: MGC-803 Cell Tested Concentrations: 0, 2, 4 and 8 μM Incubation Duration: 36 hrs (hours) Experimental Results: The percentage of apoptotic cells increased from 12.07% to 61.69% in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Male BALB/c nude mice [1]
Doses: 30 mg/kg Route of Administration: Oral administration; one time/day for 3 weeks Experimental Results: Inhibition of tumor growth, tumor The growth inhibition (TGI) rate was 41.5%. |
| References |
| Molecular Formula |
C18H21N7O3
|
|---|---|
| Molecular Weight |
383.404442548752
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| Exact Mass |
383.17
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| CAS # |
2715287-67-3
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| PubChem CID |
164886635
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| Appearance |
White to off-white solid powder
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| LogP |
1.3
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
3
|
| Heavy Atom Count |
28
|
| Complexity |
491
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O1C2=CC=C(C3=NC(N4CCOCC4)=NC(N4CCOCC4)=N3)C=C2N=C1N
|
| InChi Key |
LOQNSAZUXOBMAX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H21N7O3/c19-16-20-13-11-12(1-2-14(13)28-16)15-21-17(24-3-7-26-8-4-24)23-18(22-15)25-5-9-27-10-6-25/h1-2,11H,3-10H2,(H2,19,20)
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| Chemical Name |
5-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)-1,3-benzoxazol-2-amine
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.6082 mL | 13.0412 mL | 26.0824 mL | |
| 5 mM | 0.5216 mL | 2.6082 mL | 5.2165 mL | |
| 10 mM | 0.2608 mL | 1.3041 mL | 2.6082 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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