PI3Kα-IN-29
PI3Kα-IN-29 is a potent, orally active and selective PI3Kα with an IC50 of 2.5 nM. PI3Kα-IN-29 exhibits >400-fold selectivity over PI3Kβ/δ/γ/mTOR. PI3Kα-IN-29 selectively degrades the H1047R mutant p110α protein and inhibits PI3Kα kinase activity. PI3Kα-IN-29 suppresses PI3K/AKT/mTOR signaling, induces G1 arrest, and inhibits migration. PI3Kα-IN-29 inhibits tumor growth in a T47 mouse model. PI3Kα-IN-29 can be used for the research of breast cancer.
For research use only. We do not sell to patients.
- Formula: C20H17N5O4
- Molecular Weight:391.38
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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
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PI3Kα 2.5 nM (IC50) |
PI3Kβ >1000 nM (IC50) |
PI3Kδ >1000 nM (IC50) |
PI3Kγ >1000 nM (IC50) |
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Cell Line:T47D, MCF7
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Concentration:T47D: 0, 100, 500 nM
MCF7: 0, 1.25, 5 µM -
Incubation Time:24 h
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Result:Concentration-dependently induced G1 phase arrest both in T47D and MCF7 celss.
Increased G1 population to 71.8% and 60.2% in T47D at 500 and 100 nM, respectively.
In MCF7 cells, a similar G1 arrest pattern was observed at 1.25 and 5 µM.
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Cell Line:T47D, RKO, HCT116, SKOV3, SKBR3, PC3, MCF10A and MCF7
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Concentration:0, 0.5, 1, 5 μM
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Incubation Time:24 h
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Result:Concentration-dependently suppressed phosphorylation of AKT (Ser473) in all tested cell lines.
Selectively induced degradation of mutant PI3Kα protein (H1047R) in a concentration-dependent manner, with the most pronounced effect in T47D cells.\r
Significant degradation was also observed in other PIK3CA-mutant lines: RKO, HCT116 (colorectal cancer), and SKOV3 (ovarian cancer).
No degradation was observed in wild-type (SKBR3, MCF10A) or E545K-mutant (MCF7) cell lines.
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Cell Line:MCF7
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Concentration:125, 250, 500 nM
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Incubation Time:0, 12, 24 h
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Result:Significantly suppressed MCF7 cell migration, with minimal wound closure observed even at low concentrations after 24 h.
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Cell Line:T47D, MCF7
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Concentration:0, 0.1, 0.5, 1, 2 μM
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Incubation Time:24 h
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Result:Upregulated p27 expression, and downregulated E-cadherin expression.
Demonstrated concentration-dependent suppression of retino-blastoma (RB) protein phosphorylation, with concomitant RB degradation observed at higher concentrations.
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Cell Line:MCF7
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Concentration:125, 250, 500 nM, 1 and 2 μM
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Incubation Time:14 days
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Result:Concentration-dependently inhibited colony formation in MCF7 cells.
Achieved near‑complete suppression at higher concentrations (≥1 µM).
PI3Kα-IN-29 (500, 1000, and 1500 mg/kg, i.g., single dose) demonstrates a favorable safety profile in ICR mice[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 mice subcutaneously inoculated with T47D cells[1]
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Dosage:50 and 100 mg/kg
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Administration:p.o., once daily for 21 days
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Result:Achieved 70.7% and 52.3% tumor growth inhibition (TGI) at 100 and 50 mg/kg, respectively.
Showed a marked tumor regression at 100 mg/kg.
Showed no significant changes in body weight and no apparent histopatho-logical abnormalities.
Dose-dependently reduced Ki67 expression and phosphorylation of AKT.
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Animal Model:ICR mice[1]
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Dosage:500, 1000, and 1500 mg/kg
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Administration:i.g., single dose
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Result:Revealed no significant body weight loss roup throughout the 14-day period.
Showed no inflammatory infiltration or organ-specific lesions in all major organs.
Chemical Information
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Molecular Weight 391.38
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Formula C20H17N5O4
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SMILES
C[C@H](OC1=CC=C2C3=NC(C4=CC5=C(C=C4)OC(N)=N5)=CN3COC2=C1)C(N)=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-29 Related Classifications
HY-179623 Related Classifications
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