PI3Kα-IN-32
PI3Kα-IN-32 (Compound 11f) is a selective, orally active PI3Kα inhibitor, with an IC50 of 26.3 nM against PI3KαH1047R. PI3Kα-IN-32 inhibits AKT phosphorylation. PI3Kα-IN-32 exhibits anticancer activity against breast cancer. PI3Kα-IN-32 can be used in the research of HR+/HER2- breast cancer.
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- CAS. Nr.: 3057582-20-1
- Formel: C20H18F5N5O2S
- Molecular Weight:487.45
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Help & FAQs
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
PI3Kα-H1047R 26.3 nM (IC50) |
PI3Kα 94.6 nM (IC50) |
In Vitro
PI3Kα-IN-32 potently and selectively inhibits the enzymatic activity of the PI3KαH1047R mutant, with an IC50 of 26.3 nM[1].
PI3Kα-IN-32 (maximum 10 μM; 144 h) potently inhibits the proliferation of T47D HR+/HER2- breast cancer cells with an IC50 of 88.8 nM, and is 14.7-fold more selective for SK-BR-3 breast cancer cells expressing wild-type PI3Kα than for the former[1].
PI3Kα-IN-32 inhibits AKT phosphorylation in T47D HR+/HER2- breast cancer cells with an IC50 of 29.0 nM, and shows 5.8-fold selectivity for SK-BR-3 breast cancer cells expressing wild-type PI3Kα over the former[1].
PI3Kα-IN-32 (10 μM) exhibits high selectivity for PI3Kα, shows only weak activity against PI3Kδ and PIK3C3, and has no significant activity against the other 108 tested kinases[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:T47D HR+/HER2- breast cancer cells, SK-BR-3 wild-type PI3Kα breast cancer cells
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Concentration:10 μM (max, serial 4-fold dilutions)
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Incubation Time:144 h
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Result:Inhibited T47D cell proliferation with an IC50 of 88.8 nM.
Inhibited SK-BR-3 cell proliferation with an IC50 of 1307.5 nM, giving a T47D/SK-BR-3 selectivity ratio of 14.7.
Parmacokinetics
In Vivo
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 (female, 6-8 weeks old, subcutaneous inoculation of T47D cells with 17β-estradiol tablet implantation)[1]
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Dosage:50 mg/kg; 100 mg/kg; 150 mg/kg
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Administration:p.o.; QD; 21 days
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Result:Produced 77% tumor growth inhibition (TGI = 0.77) at 50 mg/kg.
Attained complete tumor regression at 100 mg/kg (TGI = 1.06) and 150 mg/kg (TGI = 1.19).
Showed no significant body weight loss at all tested dosages.
Caused no significant changes in plasma insulin levels at 4 h and 24 h post-dose.
Decreased tumor p-AKT (Ser473) levels by over 90% within 4 h of oral administration.
Confirmed dose-dependent inhibition of AKT phosphorylation in tumor tissue after treatment.
Chemical Information
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CAS. Nr. 3057582-20-1
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Molecular Weight 487.45
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Formel C20H18F5N5O2S
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SMILES
OC(C1)(C)CN1C(N=C2)=NC=C2NC(N[C@H](C3=C(C)C4=C(C(F)=CC(F)=C4)S3)C(F)(F)F)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
PI3Kα-IN-32 Related Classifications
HY-183285 Related Classifications
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