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Cat. No.: HY-156484

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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

Storage:

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

SPR519 Chemical Structure

CAS No.: 1391923-59-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

PI3Kα

0.03 μM (IC₅₀)

mTOR

0.01 μM (IC₅₀)

All PI3K Isoforms :

All mTOR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.23 μM Compound: 10; SPR519	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	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	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.

Cell Proliferation Assay^[1]

Cell Line:

A2780 human ovarian cancer cells
Concentration:

0.001-20 µM
Incubation Time:

48 h
Result:

Inhibited A2780 cell proliferation with an EC₅₀ of 0.23 µM.

Cell Proliferation Assay^[1]

Cell Line:

PC3 human prostate cancer cells
Concentration:

0.001-20 µM
Incubation Time:

48 h
Result:

Inhibited PC3 cell proliferation with an EC₅₀ of 0.48 µM.

Cell Proliferation Assay^[1]

Cell Line:

SKOV3 human ovarian cancer cells
Concentration:

0.001-20 µM
Incubation Time:

48 h
Result:

Inhibited SKOV3 cell proliferation with an EC₅₀ of 0.50 µM.

Parmacokinetics

Species	Dose	Route	AUC	C_max	T_max	T_1/2
Mice^[1]	1 mg/kg	p.o.	26858 nM·h	5014 nM	1.33 h	2.66 h
Mice^[1]	3 mg/kg	p.o.	32146 nM·h	6903 nM	1.50 h	2.74 h
Mice^[1]	10 mg/kg	p.o.	76365 nM·h	12558 nM	1.67 h	2.52 h

In Vivo

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.

Animal Model:

CD1 nude mice (female; subcutaneous SKOV-3 ovarian cancer xenografts, tumors grown to 120-130 mm³ before treatment)^[1]
Dosage:

2.5 mg/kg; 5 mg/kg; 10 mg/kg
Administration:

p.o.; once daily; 27 days
Result:

Induced considerable dose-dependent tumor growth inhibition starting 3 days after treatment initiation across all doses.
Reduced tumor volume.

Animal Model:

CD1 nude mice (female; subcutaneous HCT116 colon cancer xenografts, tumors grown to 120-130 mm³ before treatment)^[1]
Dosage:

2.5 mg/kg; 5 mg/kg; 10 mg/kg; 20 mg/kg
Administration:

p.o.; once daily; 21 days
Result:

Induced considerable dose-dependent tumor growth inhibition starting 3 days after treatment initiation across all doses.
Reduced tumor volume.

Chemical Information

CAS No. 1391923-59-3
Molecular Weight 427.48
Formula C₁₉H₂₁N₇O₃S
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[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. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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SPR519

All PI3K Isoforms

All mTOR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

SPR519 Related Classifications

HY-156484 Related Classifications