SPR519 

SPR519 is a selective, orally active dual PI3Kα/mTOR kinase inhibitor, with an IC₅₀ of 0.03 μM against PI3Kα and an IC₅₀ of 0.01 μM against mTOR. SPR519 exhibits anticancer effects in ovarian cancer and colon cancer xenograft models. SPR519 can be used for the research of solid tumors (ovarian cancer, colon cancer)^[1].

SPR519 (0.001-10 µM; 15 min) inhibits purified PI3Kα enzyme with an IC₅₀ of 0.03 µM^[1].
SPR519 inhibits purified mTOR enzyme with an IC₅₀ of 0.01 µM^[1].
SPR519 (0.001-20 µM; 48 h) inhibits A2780 human ovarian cancer cell proliferation with an EC₅₀ of 0.23 µM^[1].
SPR519 (0.001-20 µM; 48 h) inhibits PC3 human prostate cancer cell proliferation with an EC₅₀ of 0.48 µM^[1].
SPR519 (0.001-20 µM; 48 h) inhibits SKOV3 human ovarian cancer cell proliferation with an EC₅₀ of 0.50 µM^[1].

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

SPR519 (2.5-10 mg/kg; p.o.; once daily; for 27 consecutive days) exerts significant, dose-dependent tumor growth inhibition in female CD1 nude mice bearing SKOV-3 ovarian cancer xenografts, even at the low dose of 2.5 mg/kg administered orally once daily for 27 consecutive days^[1].
SPR519 (2.5-20 mg/kg; p.o.; once daily; for 21 consecutive days) exerts significant, dose-dependent tumor growth inhibition in female CD1 nude mice bearing HCT116 colon cancer xenografts^[1].

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

427.48

C₁₉H₂₁N₇O₃S

1391923-59-3

O=C(C1=CC=C(OC2=NC(=NC(=N2)N3CCOCC3)C=4SC(=NC4)N)C=C1)N(C)C

Room temperature in continental US; may vary elsewhere.

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

• [1]. Mahajan D, et al. Discovery and Development of SPR519 as a Potent, Selective, and Orally Bioavailable Inhibitor of PI3Kα and mTOR Kinases for the Treatment of Solid Tumors. J Med Chem. 2020;63(19):11121-11130.