PI3Kα-IN-30
PI3Kα-IN-30 is an orally active, selective PI3Kα inhibitor with an IC50 of 2.8 nM. PI3Kα-IN-30 inhibits cancer cell proliferation, as well as the phosphorylation of Akt (S473) and pS6 (S240/244). PI3Kα-IN-30 shows low growth inhibitory activity against normal somatic cell lines at a concentration of 30 μM. PI3Kα-IN-30 induces cancer cell apoptosis and exerts anti-tumor efficacy in xenograft models. PI3Kα-IN-30 can be used for the research of breast cancer.
For research use only. We do not sell to patients.
- Formula: C26H28F3N7O3S
- Molecular Weight:575.61
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PI3K alpha 2.8 nM (IC50) |
PI3Kα-IN-30 (Compound 26) (0.001-30 μM; 72 h) potently inhibits the proliferation of T47D, MCF-7, and HCC1954 human breast cancer cell lines, with the strongest activity against T47D cells (IC50 = 0.0084 μM)[1].
PI3Kα-IN-30 (30 μM) shows minimal growth inhibitory effects on normal somatic HK-2, LX-2, and BEAS-2B cells at a concentration of 30 μM[1].
PI3Kα-IN-30 (0.03-3 μM; 1 h) dose-dependently downregulates the PI3K signaling pathway in T47D cells by reducing phosphorylation of Akt and S6[1].
PI3Kα-IN-30 (1 μM; 48 h) induces apoptosis in T47D cells at a concentration of 1 μM after 48 h of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T47D cells
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Concentration:0.03, 0.1, 0.3, 1 and 3 μM
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Incubation Time:1 h
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Result:Dose-dependently reduced the phosphorylation level of Akt (S473) and S6 (S240/244) in T47D cells.
Showed significant inhibition at concentrations as low as 0.03 μM for pAkt(S473) and 0.1 μM for pS6(S240/244).
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Cell Line:T47D cells
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Concentration:1 μM
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Incubation Time:48 h
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Result:Induced apoptosis in T47D cells at 1 μM, with statistical significance compared to controls.
| Species | Dose | Route | Cmax | Tmax | T1/2 | CL | AUC0-t | AUC0-∞ | Vz | MRT0-t | MRT0-∞ | F |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 1 mg/kg | i.v. | 2013 ng/mL | 0.033 h | 0.51 h | 1035 mL/h/kg | 2426 ng·h/mL | 973 ng·h/mL | 761 mL/kg | 0.55 h | 0.57 h | / |
| Rat[1] | 10 mg/kg | p.o. | 1443 ng/mL | 0.51 h | 3.00 h | 3345 mL/h/kg | 3238 ng·h/mL | 3405 ng·h/mL | 15142 mL/kg | 2.20 h | 2.77 h | 34.8 % |
| Mice[1] | 3.4 mg/kg | i.v. | 3323 ng/mL | 0.083 h | 3.11 h | 768 mL/h/kg | 4502 ng·h/mL | 4530 ng·h/mL | 3338 mL/kg | 1.48 h | 1.61 h | / |
| Mice[1] | 15 mg/kg | p.o. | 1940 ng/mL | 2.67 h | 2.61 h | 1277 mL/h/kg | 11375 ng·h/mL | 12220 ng·h/mL | 4749 mL/kg | 3.99 h | 4.46 h | 61.1 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c-Nude (6-8 weeks old, 20 females) mice[1]
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Dosage:20 and 40 mg/kg
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Administration:p.o.; once daily for 21 consecutive days
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Result:Achieved a tumor growth inhibition rate (TGI) of 71.98% at 40 mg/kg.
Chemical Information
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Molecular Weight 575.61
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Formula C26H28F3N7O3S
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SMILES
CC(N=C(NC(N1C[C@H](NC(C2=C(C)C=CC=N2)=O)C[C@H]1C(N)=O)=O)S3)=C3C4=CC=NC(C(C)(C)C(F)(F)F)=C4
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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)
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