PI3Kα-IN-34
PI3Kα-IN-34 is a selective PI3Kα inhibitor. PI3Kα-IN-34 releases NO in cells in a concentration-dependent manner. PI3Kα-IN-34 induces Apoptosis. PI3Kα-IN-34 can be used for research on colorectal cancer and breast cancer.
For research use only. We do not sell to patients.
- Formula: C24H30N8O7S
- Molecular Weight:574.61
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
712 nM
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Antiproliferative activity against human MCF-7 cells assessed by MTT assay after 48 h of incubation.
Antiproliferative activity against human MCF-7 cells assessed by MTT assay after 48 h of incubation.
|
42679149 |
| MDA-MB-231 | IC50 |
21 nM
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Antiproliferative activity against human MDA-MB-231 cells assessed by MTT assay after 48 h of incubation.
Antiproliferative activity against human MDA-MB-231 cells assessed by MTT assay after 48 h of incubation.
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42679149 |
| A549 | IC50 |
1444 nM
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Antiproliferative activity against human A549 cells assessed by MTT assay after 48 h of incubation.
Antiproliferative activity against human A549 cells assessed by MTT assay after 48 h of incubation.
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42679149 |
| HeLa | IC50 |
260 nM
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Antiproliferative activity against human HeLa cells assessed by MTT assay after 48 h of incubation.
Antiproliferative activity against human HeLa cells assessed by MTT assay after 48 h of incubation.
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42679149 |
| HepG2 | IC50 |
264 nM
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Antiproliferative activity against human HepG2 cells assessed by MTT assay after 48 h of incubation.
Antiproliferative activity against human HepG2 cells assessed by MTT assay after 48 h of incubation.
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42679149 |
| 4T1 | IC50 |
76 nM
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Antiproliferative activity against murine 4T1 cells assessed by MTT assay after 48 h of incubation.
Antiproliferative activity against murine 4T1 cells assessed by MTT assay after 48 h of incubation.
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42679149 |
| CT26 | IC50 |
10 nM
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Antiproliferative activity against murine CT26 colon cancer cells assessed by MTT assay after 48 h of incubation.
Antiproliferative activity against murine CT26 colon cancer cells assessed by MTT assay after 48 h of incubation.
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42679149 |
| HEK-293T | IC50 |
5371 nM
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Antiproliferative activity against human embryonic kidney HEK-293T cells assessed by MTT assay after 48 h of incubation.
Antiproliferative activity against human embryonic kidney HEK-293T cells assessed by MTT assay after 48 h of incubation.
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42679149 |
| L929 | IC50 |
>10000 nM
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Antiproliferative activity against murine L929 cells assessed by MTT assay after 48 h of incubation.
Antiproliferative activity against murine L929 cells assessed by MTT assay after 48 h of incubation.
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42679149 |
In Vitro
PI3Kα-IN-34 (Compound 5K) (48 h) exhibits significant antiproliferative activity against CT26 cells, MCF7 cells, and MDA-MB-231 cells, with IC50 values of 10 nM, 712 nM, and 21 nM, respectively[1].
PI3Kα-IN-34 (10-20 nM; 24 h) causes CT26 cells to accumulate in G2/M phase in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CT26 cells, MCF7 cells, and MDA-MB-231 cells
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Concentration:Serial concentrations
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Incubation Time:48 h
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Result:Exhibits significant antiproliferative activity against CT26 cells, MCF7 cells, and MDA-MB-231 cells, with IC50 values of 10 nM, 712 nM, and 21 nM, respectively
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Cell Line:CT26
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Concentration:10, 20 nM
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Incubation Time:24 h
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Result:Revealed a dose-dependent accumulation in the G2/M phase, increasing from 2.45% (control) to 27.9% (20 nM).
Induced a decrease in the proportion of cells in the S phase from 52.0% (control) to
23.8% (20 nM).
In Vivo
PI3Kα-IN-34 (12.5-50 mg/kg; tail intravenous bolus injection; single dose) has a single-dose intravenous LD50 of 30.3 mg/kg in healthy mice, with no observed adverse effects at non-lethal doses[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (Female, 6-8 weeks old)[1]
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Dosage:10 mg/kg
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Administration:tail intravenous injection; every 2 days
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Result:Exhibited effective in vivo tumor growth inhibition with no substantial mouse body weight loss and no detectable toxic effects on the heart, liver, spleen, lung, or kidney.
Showed pronounced nuclear shrinkage, loss of cellularity, and extensive necrotic areas in tumor tissue via hematoxylin and eosin staining.
Induced significant tumor cell apoptosis confirmed by TUNEL staining.
Reduced p-Akt levels significantly and elevated 3-nitrotyrosine levels in tumor lysates via Western blot analysis.
Decreased Ki-67 expression markedly in treated tumor tissue via flow cytometric analysis.
Showed no abnormalities in alanine transaminase, aspartate transaminase, blood urea nitrogen, creatine kinase, or lactate dehydrogenase markers via biochemical blood analysis.
Chemical Information
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Molecular Weight 574.61
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Formula C24H30N8O7S
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SMILES
[O-][N+]1=C(C(OC[C@@H]2CCCN2C3=NC(N4CCOCC4)=NC(N5CCOCC5)=N3)=NO1)S(=O)(C6=CC=CC=C6)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PI3Kα-IN-34 Related Classifications
HY-189148 Related Classifications
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