PI3Kα-IN-31
PI3Kα-IN-31 is an orally active and selective PI3Kα inhibitor. PI3Kα-IN-31 shows potent preference for mutant PI3Kα over wild-type PI3Kα. PI3Kα-IN-31 exerts antiproliferative effects in PI3Kα-mutant cancer cells. PI3Kα-IN-31 suppresses tumor growth in xenograft models. PI3Kα-IN-31 can be used for the research of breast cancer.
For research use only. We do not sell to patients.
- CAS No.: 3115133-30-4
- Formula: C29H19ClF5N5O4
- Molecular Weight:631.94
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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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PI3Kα 87.35 nM (IC50) |
p110α-H1047R 14.2 nM (IC50) |
p110α-E542K 24.58 nM (IC50) |
p110α-E545K 31.88 nM (IC50) |
PI3Kα-IN-31 (compound B10) (0-1000 nM; 30 min pre-incubation, 1 h reaction) selectively inhibits purified PI3KαH1047R, PI3KαE542K, and PI3KαE545K mutant enzymes with IC50 values of 14.2 nM, 24.58 nM, and 31.88 nM, respectively, and exhibits weaker inhibitory activity against wild-type PI3Kα with an IC50 of 87.35 nM[1].
PI3Kα-IN-31 (0-10 μM; 96 h) potently inhibits the proliferation of T-47D and MCF-7 breast cancer cells harboring PI3Kα mutations with IC50 values of 9.7 nM and 18.6 nM respectively, and shows no significant inhibition of SKBR3 cells with wild-type PI3Kα[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD-SCID (female, 4-6 weeks old, subcutaneous inoculation of MCF-7 cells)[1]
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Dosage:25 mg/kg; 50 mg/kg
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Administration:p.o.; daily; 20 days
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Result:Reached average tumor volumes of 333.6 mm3 and 210.5 mm3 on day 12 at doses of 25 mg/kg and 50 mg/kg, respectively.
Achieved tumor growth inhibition (TGI) rates of 86.29% and 97.17% at doses of 25 mg/kg and 50 mg/kg, respectively.
Showed no significant body weight loss or other adverse reactions during the study period.
Chemical Information
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CAS No. 3115133-30-4
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Molecular Weight 631.94
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Formula C29H19ClF5N5O4
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SMILES
O=C(C1=CC(NC(C2=CC(NC(C3=CC(F)=CC(C(F)(F)F)=C3)=O)=C4N2CC(NC4C5=CC(F)=CC=C5Cl)=O)=O)=CC=C1)N
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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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