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^[1].

PI3Kα-IN-31 (compound B10) (0-1000 nM; 30 min pre-incubation, 1 h reaction) selectively inhibits purified PI3Kα^H1047R, PI3Kα^E542K, and PI3Kα^E545K 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.

PI3Kα-IN-31 (compound B10) (25-50 mg/kg; p.o.; daily; 20 days) dose-dependently inhibits MCF-7 breast cancer xenograft growth in NOD-SCID mice, achieving 86.29% and 97.17% TGI, respectively, with good in vivo tolerance^[1].

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

631.94

C₂₉H₁₉ClF₅N₅O₄

3115133-30-4

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Zheng ZB, et al. 1,2-Dihydropyrrolo[1,2-a]pyrazine-3(4H)-one Derivatives and Their Uses, CN, CN121045188A, 2025-12-02.