K145 hydrochloride
目录号 : KM9108 CAS No. : 1449240-68-9 纯度 : 98%

K145 hydrochloride 是一种选择性的,具有底物竞争性和口服活性的 SphK2 抑制剂,IC50 为 4.3 µM,Ki 为 6.4 µM。K145 hydrochloride 对 SphK1 和其他蛋白激酶没有活性。K145 hydrochloride 可诱导细胞凋亡,并具有强大的抗肿瘤活性。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
50mg
In-stock
100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

Other Forms of Rapamycin:

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生物活性

K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity.

体外研究

K145 (0-10 µM; 24-72 hours; U937 cells) treatment significantly inhibits the growth of U937 cells in a concentration-dependent manner.
K145 (10 µM; 24 hours; U937 cells) treatment significantly induces apoptosis in U937 cells.
K145 (4-8 µM; 3 hours; U937 cells) treatment decreases the phosphorylation of ERK and Akt.
Treatment with K145 (10 µM) causes a decrease of total cellular S1P without significant effects on ceramide levels.

Cell Viability Assay

Cell Line: U937 cells
Concentration: 0 µM, 4 µM, 6 µM, 8 µM, 10 µM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Significantly inhibited the growth of U937 cells in a concentration-dependent manner.

Apoptosis Analysis

Cell Line: U937 cells
Concentration: 10 µM
Incubation Time: 24 hours
Result: Significantly induced apoptosis in U937 cells.

Western Blot Analysis

Cell Line: U937 cells
Concentration: 4 µM, 8 µM
Incubation Time: 3 hours
Result: Phosphorylated ERK and Akt were decreased.
体内研究

K145 (50 mg/kg; oral gavage; daily; for 15 days; BALB/c-nu mice) treatment significantly inhibits the growth of U937 tumors in nude mice.

Animal Model: BALB/c-nu mice injected with U937 cells
Dosage: 50 mg/kg
Administration: Oral gavage; daily; for 15 days
Result: Inhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed.
分子式
C18H25ClN2O3S
分子量
384.92
CAS号
1449240-68-9
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: 

H2O : 126.7 mg/mL (329.16 mM; Need ultrasonic and warming)

DMSO : 50 mg/mL (129.90 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5979 mL 12.9897 mL 25.9794 mL
5 mM 0.5196 mL 2.5979 mL 5.1959 mL
10 mM 0.2598 mL 1.2990 mL 2.5979 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: ≥ 0.83 mg/mL (2.16 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (2.16 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 8.3 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: ≥ 0.83 mg/mL (2.16 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (2.16 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 8.3 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: ≥ 0.83 mg/mL (2.16 mM); Clear solution

    此方案可获得 ≥ 0.83 mg/mL (2.16 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 8.3 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
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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