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).
For research use only. We do not sell to patients.
- CAS No.: 1391923-59-3
- Formula: C19H21N7O3S
- Molecular Weight:427.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
[1]|
PI3Kα 0.03 μM (IC50) |
mTOR 0.01 μM (IC50) |
Cellular Effect
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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
|
[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
|
[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
|
[PMID: 32897703] |
In Vitro
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. Further protocols information, click here.
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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.
Parmacokinetics
In Vivo
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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CAS No. 1391923-59-3
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Molecular Weight 427.48
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Formula 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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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Splenic/Portal-Vein Liver Metastasis Xenograft
Splenic and portal-vein liver metastasis xenograft models deliver tumor cells into the portal circulation so that cells reach the liver first and form hepatic metastatic lesions; splenic injection uses the spleen as an access route to the portal system, while direct portal-vein injection introduces cells into the portal vein without requiring splenectomy. The assay detects liver colonization, intrahepatic tumor growth, tumor distribution, treatment response, survival, and liver-metastasis microenvironment changes; readouts include bioluminescence or fluorescence imaging, gross liver nodule counts, liver weight or tumor burden, histology, and survival.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
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Intraperitoneal/Peritoneal Dissemination Xenograft
Intraperitoneal (IP) or peritoneal dissemination xenograft models are based on the introduction of human cancer cells into the peritoneal cavity of immunodeficient mice, where they attach to peritoneal surfaces, form multicellular aggregates or spheroids, and progressively generate disseminated tumor nodules that mimic advanced peritoneal metastatic disease. These models are widely used to study ovarian cancer progression, tumor-microenvironment interactions, and intraperitoneal therapeutic responses, often incorporating bioluminescence or fluorescence imaging to longitudinally monitor tumor burden in vivo. The biological principle relies on the capacity of tumor cells such as SKOV3 or related ovarian carcinoma lines to survive in suspension, aggregate within ascites-like fluid, adhere to mesothelial surfaces, and invade peritoneal organs, thereby recapitulating human peritoneal carcinomatosis patterns observed in advanced disease.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)