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PIK-75 HCl

目录号: PC15423 纯度: ≥98%

PI3K亚型p110α抑制剂，PIK-75 是一种 DNA-PK 和 PI3K 抑制剂，抑制 DNA-PK，p110α 和 p110γ，IC50 分别为 2, 5.8 和 76 nM。PIK-75 抑制 p110α 效果比抑制 p110β (IC50=1.3 μM) 高 200 多倍。

CAS No. :372196-77-5

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PC15423-100mg	100mg	¥2255.00	请登录
PC15423-10mM (in 1mL DMSO)	10mM(in1mLDMSO)	¥777.00	请登录

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中文名称	PIK-75 HCl
中文别名	2-甲基-5-硝基苯磺酸 [(6-溴咪唑并[1,2-A]吡啶-3-基)亚甲基]甲基肼盐酸盐;PIK-75 抑制剂
英文名称	PIK-75 HCl
英文别名	PIK-75 Hydrochloride;PFK-15;PIK-75;PIK-75 (hydrochloride);PIK-75, HYDROCHLORIDE SALT;PIK-75, hydrochloride salt (PIK 75 hydrochloride);PIK 75;2-Methyl-5-nitrobenzenesulfonic acid [(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]methylhydrazide hydrochloride;7GH4IC9PLL;(E)-N'-((6-bromoimidazo[1,2-a]pyridin-3-yl)methylene)-N,2-dimethyl-5-nitrobenzenesulfonohydrazide hydrochloride;N'-[(1E)-(6-bromoimidazo[1,2-a]pyridin-3-yl)methylene]-N,2-dimethyl-5-nitrobenzenesulfonohydrazide hydrochloride;ABP000105;s1205
Cas No.	372196-77-5
分子式	C₁₆H₁₅BrClN₅O₄S
分子量	488.74
包装储存	Sealed and stored at 4℃，, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	PI3K亚型p110α抑制剂，PIK-75 是一种 DNA-PK 和 PI3K 抑制剂，抑制 DNA-PK，p110α 和 p110γ，IC50 分别为 2, 5.8 和 76 nM。PIK-75 抑制 p110α 效果比抑制 p110β (IC50=1.3 μM) 高 200 多倍。

生物活性

PIK-75 hydrochloride is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC₅₀s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC₅₀=1.3 μM). PIK-75 hydrochloride induces apoptosis.

性状

Solid

IC50 & Target[1][2]

DNA-PK

2 nM (IC₅₀)

p110α

5.8 nM (IC₅₀)

p110γ

76 nM (IC₅₀)

p110δ

510 nM (IC₅₀)

p110β

1.3 μM (IC₅₀)

hsVPS34

2.6 μM (IC₅₀)

PI3KC2β

1 μM (IC₅₀)

PI3KC2α

10 μM (IC₅₀)

mTORC1

1 μM (IC₅₀)

mTORC2

10 μM (IC₅₀)

ATM

2.3 μM (IC₅₀)

ATR

21 μM (IC₅₀)

PI4KIIIβ

50 μM (IC₅₀)

体外研究(In Vitro)

PIK-75 also inhibits p110δ, PI3KC2β, mTORC1, ATM, hsVPS34, PI3KC2α, mTORC2, ATR and PI4KIIIβ with IC₅₀s of 510 nM, ~1 μM, ~1 μM, 2.3 μM, 2.6 μM, ~10 μM, ~10 μM, 21 μM, ~50 μM, respectively.
PIK-75 alone blocks Thr 308 phosphorylation in L6 myotubes and 3T3-L1 adipocytes with IC₅₀ values of 1.2 and 1.3 μM, respectively.
PIK-75 (1-1000 nM; 5 min) blocks the phosphorylation of PKB induced by insulin on both Ser473and Thr308 in CHO-IR cells in a dose-dependent manner, with an IC₅₀ of 78 nM.
PIK-75 (0.1-1000 nM; 48 hours) inhibits the proliferation and survival of pancreatic cancer cells through apoptotic cell death.
PIK-75 (0.1-1000 nM) also reduces the colony formation of pancreatic cancer MIA PaCa-2 and AsPC-1 cells.

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

Cell Viability Assay

Cell Line:	Human pancreatic cancer cells (MIA PaCa-2 or AsPC-1)
Concentration:	0.1, 0.3, 1, 3, 10, 30, 100, 300, and 1000 nM
Incubation Time:	48 hours
Result:	Submicromolar concentration was sufficient to inhibit the proliferation of pancreatic cancer, MIA PaCa-2 and AsPC-1 cells after 48-h treatment.

Western Blot Analysis

Cell Line:	Overnight-starved CHO-IR cells
Concentration:	1, 10, 100, 1000 nM
Incubation Time:	5 minutes
Result:	Blocked the phosphorylation of PKB induced by insulin (1 nM, 10 min) on both Ser473and Thr308 in a dose-dependent manner.

体内研究(In Vivo)

PIK-75 (2 mg/kg) potentiates anticancer activity of Gemcitabine (20 mg/kg) in vivo. Gemcitabine (20 mg/kg) or PIK-75 (2 mg/kg) alone reduces the tumor growth to similar degree. Beneficial effect of PIK-75/Gemcitabine is evident as this combination markedly reduces the tumor growth in vivowithout affecting the body weights of mice.

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

Animal Model:	Mice bearing tumors of MIA PaCa-2
Dosage:	2 mg/kg; or combination with Gemcitabine (20 mg/kg)
Administration:	Administered injection; 5 times per week. 25 days
Result:	Reduced the tumor growth and enhanced the antitumor effect.

运输条件

Room temperature or refrigerated transportation.

储存方式

Sealed and stored at 4℃，, away from moisture

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

参考文献

[1]. Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47. [Information]

[2]. Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58. [Information]

[3]. Duong HQ, et al. Inhibition of NRF2 by PIK-75 augments sensitivity of pancreatic cancer cells to gemcitabine. Int J Oncol. 2014 Mar;44(3):959-69. [Information]

[4]. Hayakawa M, Kawaguchi K, Kaizawa H, et al. Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. Bioorg Med Chem. 2007;15(17):5837-5844. [Information]

溶解度数据

体外研究:

DMSO : 11 mg/mL (22.51 mM; Need ultrasonic)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0461 mL	10.2304 mL	20.4608 mL
5 mM	0.4092 mL	2.0461 mL	4.0922 mL
10 mM	0.2046 mL	1.0230 mL	2.0461 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1.1 mg/mL (2.25 mM); Clear solution

此方案可获得 ≥ 1.1 mg/mL (2.25 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 11.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 1.1 mg/mL (2.25 mM); Clear solution

此方案可获得 ≥ 1.1 mg/mL (2.25 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 11.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1.1 mg/mL (2.25 mM); Clear solution

此方案可获得 ≥ 1.1 mg/mL (2.25 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 11.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

搜索质检报告(COA)

产品使用指南

Data Sheet

[1]. Knight ZA, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47. [Information]

[2]. Chaussade C, et al. Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling. Biochem J. 2007 Jun 15;404(3):449-58. [Information]

[3]. Duong HQ, et al. Inhibition of NRF2 by PIK-75 augments sensitivity of pancreatic cancer cells to gemcitabine. Int J Oncol. 2014 Mar;44(3):959-69. [Information]

[4]. Hayakawa M, Kawaguchi K, Kaizawa H, et al. Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors. Bioorg Med Chem. 2007;15(17):5837-5844. [Information]

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

PIK-75 HCl

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