PIK-75 hydrochloride - CAS:372196-77-5

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PIK-75 hydrochloride

目录号 : KM9134 CAS No. : 372196-77-5 纯度 : 98%

Data Sheet 产品使用指南

PIK-75 hydrochloride 是一种可逆的 DNA-PK 和 p110α-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)。

规格	价格	是否有货
10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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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.

体外研究

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.

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

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.

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.

分子式

C₁₆H₁₅BrClN₅O₄S

分子量

488.74

CAS号

372196-77-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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°C) (insoluble)

配制储备液

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

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。-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。

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。
2.

请依序添加每种溶剂： 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。
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。

科研文献

纯度： 98%

Data Sheet

产品使用指南

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*

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

浓度

体积

浓度

体积

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Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 2 篇科研文献

The molarity calculator equation

The dilution calculator equation