2. PI3K/Akt/mTOR Apoptosis
  3. PI3K Akt Apoptosis
  4. 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.

PI3Kα-IN-30

PI3Kα-IN-30 Chemical Structure

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PI3Kα-IN-30 Related Antibodies

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Description

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[1].

IC50 & Target[1]

PI3K alpha

2.8 nM (IC50)

In Vitro

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.

PI3Kα-IN-30 Related Antibodies

Western Blot Analysis[1]

Cell Line: T47D cells
Concentration: 0.03, 0.1, 0.3, 1 and 3 μM
Incubation Time: 1 h
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).

Apoptosis Analysis[1]

Cell Line: T47D cells
Concentration: 1 μM
Incubation Time: 48 h
Result: Induced apoptosis in T47D cells at 1 μM, with statistical significance compared to controls.
Parmacokinetics
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 %
In Vivo

PI3Kα-IN-30 (Compound 26) (20-40 mg/kg; p.o.; once daily for 21 consecutive days) effectively inhibits tumor growth in a mouse model of HCC1954 breast cancer xenografts harboring PIK3CA mutations[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c-Nude (6-8 weeks old, 20 females) mice[1]
Dosage: 20 and 40 mg/kg
Administration: p.o.; once daily for 21 consecutive days
Result: Achieved a tumor growth inhibition rate (TGI) of 71.98% at 40 mg/kg.
Molecular Weight

575.61

Formula

C26H28F3N7O3S
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PI3Kα-IN-30 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PI3Kα-IN-30PI3KAktApoptosisPhosphoinositide 3-kinasePKBProtein kinase Bbreast cancerHCC1954PI3KδT47DPI3KαpS6MCF-7PI3KγPI3KβInhibitorinhibitorinhibit

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