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PIK-75 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PIK-75 hydrochloride图片
CAS NO:372196-77-5
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
PIK-75 hydrochloride 是一种可逆的DNA-PKp110α-选择性的抑制剂,抑制 DNA-PK,p110α和 p110γ,IC50分别为 2,5.8 和 76 nM。PIK-75 hydrochloride 抑制 p110α 效果比抑制 p110β (IC50=1.3 μM) 高 200 多倍。PIK-75 hydrochloride 诱导凋亡 (apoptosis)。
生物活性

PIK-75 hydrochloride is a reversibleDNA-PKandp110α-selective inhibitor, which inhibitsDNA-PK,p110αand p110γ withIC50s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM)[1][2]. PIK-75 hydrochloride inducesapoptosis[3].

IC50& Target[1]

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[1].
PIK-75 alone blocks Thr 308 phosphorylation in L6 myotubes and 3T3-L1 adipocytes with IC50values of 1.2 and 1.3 μM, respectively[1].
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 IC50of 78 nM[2].
PIK-75 (0.1-1000 nM; 48 hours) inhibits the proliferation and survival of pancreatic cancer cells through apoptotic cell death[3].
PIK-75 (0.1-1000 nM) also reduces the colony formation of pancreatic cancer MIA PaCa-2 and AsPC-1 cells[3].

Cell Viability Assay[3]

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[2]

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[3].

Animal Model:Mice bearing tumors of MIA PaCa-2[3]
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.
分子量

488.74

性状

Solid

Formula

C16H15BrClN5O4S

CAS 号

372196-77-5

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
In Vitro: 

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

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

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.0461 mL10.2304 mL20.4608 mL
5 mM0.4092 mL2.0461 mL4.0922 mL
10 mM0.2046 mL1.0230 mL2.0461 mL
*

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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.

    请依序添加每种溶剂: 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 ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin 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 μL20% 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.

    请依序添加每种溶剂: 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。

*以上所有助溶剂都可在本网站选购。