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).
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- No. CAS: 1391923-59-3
- Fòrmula: C19H21N7O3S
- Peso molecular:427.48
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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PI3Kα 0.03 μM (IC50) |
mTOR 0.01 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A2780 | IC50 |
0.23 μM
Compound: 10; SPR519
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Antiproliferative activity against human A2780 cells after 48 hrs by MTT assay
Antiproliferative activity against human A2780 cells after 48 hrs by MTT assay
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[PMID: 32897703] |
| PC-3 | EC50 |
0.48 μM
Compound: 10; SPR519
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Antiproliferative activity against human PC-3 cells after 48 hrs by MTT assay
Antiproliferative activity against human PC-3 cells after 48 hrs by MTT assay
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[PMID: 32897703] |
| SK-OV-3 | EC50 |
0.5 μM
Compound: 10; SPR519
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Antiproliferative activity against human SK-OV-3 cells after 48 hrs by MTT assay
Antiproliferative activity against human SK-OV-3 cells after 48 hrs by MTT assay
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[PMID: 32897703] |
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.
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Cell Line:A2780 human ovarian cancer cells
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Concentration:0.001-20 µM
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Incubation Time:48 h
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Result:Inhibited A2780 cell proliferation with an EC50 of 0.23 µM.
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Cell Line:PC3 human prostate cancer cells
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Concentration:0.001-20 µM
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Incubation Time:48 h
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Result:Inhibited PC3 cell proliferation with an EC50 of 0.48 µM.
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Cell Line:SKOV3 human ovarian cancer cells
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Concentration:0.001-20 µM
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Incubation Time:48 h
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Result:Inhibited SKOV3 cell proliferation with an EC50 of 0.50 µM.
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.
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Animal Model:CD1 nude mice (female; subcutaneous SKOV-3 ovarian cancer xenografts, tumors grown to 120-130 mm3 before treatment)[1]
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Dosage:2.5 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:p.o.; once daily; 27 days
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Result:Induced considerable dose-dependent tumor growth inhibition starting 3 days after treatment initiation across all doses.
Reduced tumor volume.
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Animal Model:CD1 nude mice (female; subcutaneous HCT116 colon cancer xenografts, tumors grown to 120-130 mm3 before treatment)[1]
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Dosage:2.5 mg/kg; 5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:p.o.; once daily; 21 days
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Result:Induced considerable dose-dependent tumor growth inhibition starting 3 days after treatment initiation across all doses.
Reduced tumor volume.
Chemical Information
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No. CAS 1391923-59-3
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Peso molecular 427.48
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Fòrmula C19H21N7O3S
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SMILES
O=C(C1=CC=C(OC2=NC(=NC(=N2)N3CCOCC3)C=4SC(=NC4)N)C=C1)N(C)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SPR519 Related Classifications
HY-156484 Related Classifications
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