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KP372-1

目录号: PC15525 纯度: ≥98%
特异性Akt抑制剂,KP372-1 is a specific Akt inhibitor that blocks proliferation and induces apoptosis of thyroid cancer cells with an IC50 value of 30-60 nM in vitro.
CAS No. :1374996-60-7
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中文名称
KP372-1
英文名称
KP372-1
英文别名
KP372-1
Cas No.
1374996-60-7
分子式
C10N6OH4
分子量
224.18
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

KP372-1 is an Akt inhibitor that inhibits proliferation and induces apoptosis and anoikis. KP372-1 is also an NQO1 redox cycling agent that causes DNA damage (including DNA breakage) by generating ROS. KP372-1 can be used in cancer research (such as head and neck squamous cell carcinoma (HNSCC) and pancreatic cancer).

性状

Solid

体外研究(In Vitro)

KP372-1 (0.0625, 0.125, 0.25, 0.5, 1.0 μM; 48 h) inhibits growth of JMARc42 and Tu167c2 cells with IC50s of 200 and 100 nM, respectively.
KP372-1 (125 nM; 24 h) induces Tu167c2 cells apoptosis and induces anoikis in the JMARc42 cells.
KP372-1 (125 nM; 30 min) blocks Akt, thereby decreasing the phosphorylation of the S6 ribosomal protein in both Tu167 and JMAR cells.
KP372-1 (0.250, 0.5, 1.0 μM; 30 min) inhibits Akt kinase activity with an IC50 of 250 nM in JMAR cells.

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

Cell Proliferation Assay

Cell Line: JMARc42 and Tu167c2 cells
Concentration: 0.0625, 0.125, 0.25, 0.5, 1.0 μM
Incubation Time: 48 h
Result: Showed antiproliferative activity.

Apoptosis Analysis

Cell Line: Tu167c2 and JMARc42 cells
Concentration: 125 nM
Incubation Time: 24 h
Result: Induced approximately 90% of cells apoptosis.

Western Blot Analysis

Cell Line: Tu167 and JMAR cells
Concentration: 125 nM
Incubation Time: 30 min
Result: Induced a small but consistent decrease in Akt phosphorylation with a concomitant marked decrease in S6 phosphorylation.
Inhibited the EGF induced phosphorylation of Aktser473 in Tu167 and AktThr308 in JMAR.

Western Blot Analysis

Cell Line: JMAR cells
Concentration: 0.250, 0.5, 1.0 μM
Incubation Time: 30 min
Result: Significantly blocked Akt kinase activity in a dose-dependent fashion, with an IC50 of 250 nM.
体内研究(In Vivo)

KP372-1(10, 20 mg/kg; i.v.; single daily for 33 days) induces NADH oxidation and impairs tumor growth in vivo without apparent toxicity.

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

Animal Model: Nude mice (H1299 xenografts model).
Dosage: 10, 20 mg/kg
Administration: Tailvein injection; single daily for 33 days
Result: Affected tumor metabolism and suppressed tumor growth.
运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
溶解度数据
体外研究: 

DMSO : 17.86 mg/mL (39.83 mM; Need ultrasonic)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2304 mL 11.1518 mL 22.3035 mL
5 mM 0.4461 mL 2.2304 mL 4.4607 mL
10 mM 0.2230 mL 1.1152 mL 2.2304 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。-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。

搜索质检报告(COA)

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。

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