2. PI3K/Akt/mTOR Cell Cycle/DNA Damage Autophagy Apoptosis
  3. PI3K mTOR DNA-PK Autophagy Apoptosis
  4. PI-103 Hydrochloride

PI-103 Hydrochloride 

目录号: HY-10115A 纯度: 98.00%
COA 产品使用指南

摩尔计算器

PI-103 Hydrochloride 是一种有效的 PI3K 和 mTOR 抑制剂，抑制 p110α，p110β，p110δ，p110γ，mTORC1 和 mTORC2，IC50 分别为 8 nM，88 nM，48 nM，150 nM，20 nM 和 83 nM。PI-103 Hydrochloride 也可抑制DNA-PK，IC50 为 2 nM。PI-103 Hydrochloride 诱导自噬 (autophagy)。

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PI-103 Hydrochloride Chemical Structure

PI-103 Hydrochloride Chemical Structure

CAS No. : 371935-79-4

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1089
In-stock
5 mg ￥990
In-stock
10 mg ￥1550
In-stock
50 mg ￥3464
In-stock
100 mg ￥4201
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of PI-103 Hydrochloride:

PI-103 Hydrochloride 相关抗体

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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

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy[1][2][3][4].

IC50 & Target[1]

p110α

2 nM (IC50)

p110β

3 nM (IC50)

p110δ

3 nM (IC50)

p110γ

15 nM (IC50)

mTORC1

20 nM (IC50)

mTORC2

83 nM (IC50)

DNA-PK

23 nM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
Sf9 IC50
0.003 μM
Compound: 2
Inhibition of GST-tagged human p110-beta expressed in SF9/Baculovirus system by SPA
Inhibition of GST-tagged human p110-beta expressed in SF9/Baculovirus system by SPA
[PMID: 17601739]
Sf9 IC50
0.0036 μM
Compound: 2
Inhibition of GST-tagged bovine p110-alpha expressed in SF9/Baculovirus system by SPA
Inhibition of GST-tagged bovine p110-alpha expressed in SF9/Baculovirus system by SPA
[PMID: 17601739]
Sf9 IC50
0.01 μM
Compound: 2
Inhibition of glu-tagged PI3K C2-beta expressed in SF9/Baculovirus system by SPA
Inhibition of glu-tagged PI3K C2-beta expressed in SF9/Baculovirus system by SPA
[PMID: 17601739]
Sf9 IC50
0.25 μM
Compound: 2
Inhibition of His-tagged human p110gamma expressed in SF9/Baculovirus system by SPA
Inhibition of His-tagged human p110gamma expressed in SF9/Baculovirus system by SPA
[PMID: 17601739]
体外研究
(In Vitro)

PI-103 exhibits antiproliferative properties in a panel of human cancer cell lines[1]. PI-103 is essentially cytostatic for cell lines and induced cell cycle arrest in the G1 phase. In blast cells, PI-103 inhibits leukemic proliferation, the clonogenicity of leukemic progenitors and induces mitochondrial apoptosis, especially in the compartment containing leukemic stem cells [2]. PI-103 potently inhibits both the rapamycin-sensitive (mTORC1, IC50=20 nM) and rapamycin-insensitive (mTORC2, IC50=83 nM) complexes of the protein kinase mTOR[4].

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

PI-103 Hydrochloride 相关抗体:
体内研究
(In Vivo)

PI-103 shows therapeutic activity against a range of human tumor xenografts, exhibiting inhibition of angiogenesis, invasion, and metastasis, as well as direct antiproliferative effects[1]. PI-103 induces immunosuppression promoting in vivo tumor growth and inhibiting apoptosis. Tumors from PI-103-treated mice shows higher levels of cyclin D1 and more proliferating cells[3].

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

384.82

Formula

C19H17ClN4O3
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 4.1 mg/mL (10.65 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5986 mL 12.9931 mL 25.9862 mL
5 mM 0.5197 mL 2.5986 mL 5.1972 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 98.00%

COA (273 KB) LCMS (268 KB)

产品使用指南 (1538 KB)
参考文献
Kinase Assay
[4]

IC50 values are measured using either a standard thin-layer chromatography (TLC) assay for lipid kinase activity or a high-throughput membrane capture assay. Kinase reactions are performed by preparing a reaction mixture containing kinase, inhibitor (2% DMSO final concentration), buffer (25 mM HEPES, pH 7.4, 10 mM MgCl2), and freshly sonicated phosphatidylinositol (100 μg/mL). Reactions are initiated by the addition of ATP containing 10 μCi of γ-32P-ATP to a final concentration 10 or 100 μM, and allowed to proceed for 20 minutes at room temperature. For TLC analysis, reactions are then terminated by the addition of 105 μL 1N HCl followed by 160 μL CHCl3:MeOH (1:1). The biphasic mixture is vortexed, briefly centrifuged, and the organic phase transferred to a new tube using a gel loading pipette tip precoated with CHCl3. This extract is spotted on TLC plates and developed for 3-4 hours in a 65:35 solution of n-propanol:1M acetic acid. The TLC plates are then dried, exposed to a phosphorimager screen, and quantitated. For each compound, kinase activity is typically measured at 10-12 inhibitor concentrations representing two-fold dilutions from the highest concentration tested (100 μM). For compounds showing significant activity, IC50 determinations are repeated two to four times, and the reported value is the average of these independent measurements[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

For proliferation assays, MOLM14, OCI-AmL3 and MV4-11 cells are cultured during 48 h at 105 cells/mL, in triplicate, in 10% FCS, without or with 0.1 or 1 μM PI-103, and then pulsed 6 h with 1μCi (37 kBq) [3H]-thymidine. The amounts of radioactivity are determined after trichloracetic acid precipitation[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Mice[3]
Five to six month old males of either FVB/N strain or nude BALB/c strain are injected subcutaneously with one million cells in PBS. When tumor reaches between 50 and 100 mm3, mice are treated with 10 mg/kg or 70 mg/kg of PI-103 and/or 50 mg/kg sorafenib by IP injection daily. Control mice are treated with the same volume of DMSO. Tumor size and mice weight is monitored every 2 days. When mice are sacrificed, tumors are dissected and processed[3].

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

PI-103 Hydrochloride 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5986 mL 12.9931 mL 25.9862 mL 64.9654 mL
5 mM 0.5197 mL 2.5986 mL 5.1972 mL 12.9931 mL
10 mM 0.2599 mL 1.2993 mL 2.5986 mL 6.4965 mL
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:

PI-103371935-79-4PI103PI 103PI3KmTORDNA-PKAutophagyApoptosisPhosphoinositide 3-kinaseMammalian target of RapamycinDNA-dependent protein kinaseInhibitorinhibitorinhibit

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