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製品番号: 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).

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 1391923-59-3
分子式: C₁₉H₂₁N₇O₃S
分子量:427.48

保管条件:

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

SPR519 構造式

CAS 番号: 1391923-59-3

容量

価格（税別）

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数量

Amount: USD 0.00

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- Parmacokinetics
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

PI3Kα

0.03 μM (IC₅₀)

mTOR

0.01 μM (IC₅₀)

PI3K アイソフォーム固有の製品をすべて表示 :

mTOR アイソフォーム固有の製品をすべて表示 :

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]

体外実験

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

体内実験

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.

化学情報

CAS 番号 1391923-59-3
分子量 427.48
分子式 C₁₉H₂₁N₇O₃S
SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[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]

Calculators

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

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

Minimum order quantity

100 mg

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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献

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SPR519

PI3K アイソフォーム固有の製品をすべて表示

mTOR アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

SPR519 関連分類

HY-156484 関連分類