KP372-1,99.52%

产品编号:Bellancom-15673| CAS NO:1374996-60-7| 分子式:C20H8N12O2| 分子量:448.36

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用,

货号 包装 价格 库存与货期 购买量 操作
Bellancom-15673
2800.00 杭州 北京(现货)

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KP372-1

产品介绍 KP372-1是一种 Akt 抑制剂,能抑制癌细胞增殖并诱导细胞凋亡和失巢凋亡。KP372-1 也是一种 NQO1 氧化还原循环剂,通过产生活性氧 (ROS) 来引起 DNA 损伤 (包括 DNA 断裂)。KP372-1 能有效降低体内肿瘤生长,可用于癌症的研究 (如头颈部鳞状细胞癌和胰腺癌)。
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).

体外研究

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.

西域 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.

西域 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.
体内研究

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.

西域 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.
体内研究

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.

西域 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.
性状Solid
溶解性数据
In Vitro: 

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

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2304 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
*

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。

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
参考文献

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