2. PI3K/Akt/mTOR
  3. PI3K mTOR
  4. SPR519

SPR519 是一种选择性的、具有口服活性的双重 PI3Kα/mTOR 激酶抑制剂，对 PI3Kα 的 IC50 为 0.03 μM，对 mTOR 的 IC50 为 0.01 μM。SPR519 在卵巢癌和结肠癌异种移植模型中显示出抗癌作用。SPR519 可用于实体瘤 (卵巢癌、结肠癌) 的研究。

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SPR519

SPR519 Chemical Structure

CAS No. : 1391923-59-3

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SPR519 相关抗体

Top Publications Citing Use of Products

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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mTOR mTORC1 mTORC2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

IC50 & Target[1]

PI3Kα

0.03 μM (IC50)

mTOR

0.01 μM (IC50)

体外研究
(In Vitro)

SPR519 (0.001-10 µM; 15 min) 对纯化的 PI3Kα 酶具有抑制作用，其 IC50 为 0.03 µM[1]。
SPR519 以 0.01 µM 的 IC50 抑制纯化的 mTOR 酶[1]。
SPR519 (0.001-20 µM; 48 h) 可抑制卵巢癌 A2780 细胞的增殖，其 EC50 为 0.23 µM[1]。
SPR519 (0.001-20 µM; 48 h) 可抑制前列腺癌细胞 PC3 的增殖，其 EC50 为 0.48 µM[1]。
SPR519 (0.001-20 µM; 48 h) 可抑制卵巢癌细胞 SKOV3 的增殖，其 EC50 为 0.50 µM[1]。

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

SPR519 相关抗体:

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.
药代动力学
(Parmacokinetics)
Species Dose Route AUC Cmax Tmax T1/2
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
体内研究
(In Vivo)

SPR519 (2.5-10 mg/kg；口服；每日 1 次；连续 27 天) 在每日口服 2.5 mg/kg、连续 27 天的低剂量下，即可对携带 SKOV-3 卵巢癌异种移植物的雌性 CD1 裸小鼠产生显著的、剂量依赖性肿瘤生长抑制作用[1]。
SPR519 (2.5-20 mg/kg；口服；每日 1 次；连续 21 天) 对携带 HCT116 结肠癌异种移植物的雌性 CD1 裸鼠可产生显著的、剂量依赖性肿瘤生长抑制作用[1]。

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.
分子量

427.48

Formula

C19H21N7O3S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SPR519 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SPR5191391923-59-3SPR 519SPR-519PI3KmTORPhosphoinositide 3-kinaseMammalian target of RapamycinCYP2C19ovarian cancercolon cancerA2780 human ovarian cancer cellCYP3A4SKOV3 human ovarian cancer cellPC3 human prostate cancer cellhERG potassium channelsPI3KαInhibitorinhibitorinhibit

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目录号：
HY-156484
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