K-7174 dihydrochloride,98.69%

产品编号:Bellancom-12743A| CAS NO:191089-60-8| 分子式:C33H50Cl2N2O6| 分子量:641.67

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-12743A
1100.00 杭州 北京(现货)
Bellancom-12743A
1650.00 杭州 北京(现货)
Bellancom-12743A
6500.00 杭州 北京(现货)

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K-7174 dihydrochloride

产品介绍 K-7174 dihydrochloride 是具有口服活性的 proteasomeGATA 的抑制剂。K-7174 dihydrochloride 抑制细胞黏附。K-7174 dihydrochloride 诱导细胞凋亡。K-7174 dihydrochloride 具有抗肿瘤活性,可用于癌症的研究。
生物活性

K-7174 dihydrochloride is an orally active proteasome and GATA inhibitor. K-7174 dihydrochloride is a cell adhesion inhibitor. K-7174 dihydrochloride induces cell apoptosis. K-7174 dihydrochloride shows antitumor activities, it can be used for the research of cancer.

体外研究

K-7174 dihydrochloride (10 μM; 1 h) inhibits the adhesion by VCAM-1 and its ligand.
K-7174 dihydrochloride (1-30 μM; 1 h) dose-dependently suppresses the VCAM-1 expression with an IC50 value of 14 μM.
K-7174 dihydrochloride (1-30 μM; 1 h) dose-dependently suppresses the induction of VCAM-1 mRNA by TNFα with an IC50 value of 9 μM.
K-7174 dihydrochloride (10-20 μM; 24 h) dose-dependently rescues Epo production by Hep3B cells.
K-7174 dihydrochloride (2.5-30 μM; 24 h) inhibits the binding activity of GATA.
K-7174 dihydrochloride (0-25 μM; 72 h) inhibits MM cells growth and induces cell apoptosis.

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

Cell Viability Assay

Cell Line: KMS12-BM, U266, and RPMI8226 cell lines
Concentration: 0-25 μM
Incubation Time: 72 h
Result: Inhibited MM cells growth.

Apoptosis Analysis

Cell Line: KMS12-BM, U266, and RPMI8226 cell lines
Concentration: 10 μM
Incubation Time: 48 h
Result: Significantly increased apoptosis of MM cells with the increasing percentage of annexin-V-positive cells.
体内研究
(In Vivo)

K-7174 dihydrochloride (30 mg/kg; i.p. once daily for 9 days) reverses the decreasing of hemoglobin concentrations and reticulocyte counts by IL-1β or TNF-α.
K-7174 dihydrochloride (75 mg/kg; i.p. once daily for 14 days) inhibits the tumor growth in vivo.
K-7174 dihydrochloride (50 mg/kg; p.o. once daily for 14 days) inhibits the tumor growth in vivo and shows a better effect than intraperitoneal injection.

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

Animal Model: ICR mice with IL-β or TNF-α injection
Dosage: 30 mg/kg
Administration: Intraperitoneal injection; 30 mg/kg once daily for 9 days
Result: Increased erythropoietin (Epo) production, reticulocyte counts, and hemoglobin (Hb) concentrations.
Animal Model: NOD/SCID mice with murine xenograft
Dosage: 75 mg/kg
Administration: Intraperitoneal injection; once daily for 14 days
Result: Significantly decreased tumor volume, but showed a significant body weight reduction after 10 days.
Animal Model: NOD/SCID mice with murine xenograft
Dosage: 50 mg/kg
Administration: Oral gavage; once daily for 14 days
Result: Showed an anti-myeloma activity. Porved oral administration is more effective than intraperitoneal injection.
体内研究

K-7174 dihydrochloride (30 mg/kg; i.p. once daily for 9 days) reverses the decreasing of hemoglobin concentrations and reticulocyte counts by IL-1β or TNF-α.
K-7174 dihydrochloride (75 mg/kg; i.p. once daily for 14 days) inhibits the tumor growth in vivo.
K-7174 dihydrochloride (50 mg/kg; p.o. once daily for 14 days) inhibits the tumor growth in vivo and shows a better effect than intraperitoneal injection.

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

Animal Model: ICR mice with IL-β or TNF-α injection
Dosage: 30 mg/kg
Administration: Intraperitoneal injection; 30 mg/kg once daily for 9 days
Result: Increased erythropoietin (Epo) production, reticulocyte counts, and hemoglobin (Hb) concentrations.
Animal Model: NOD/SCID mice with murine xenograft
Dosage: 75 mg/kg
Administration: Intraperitoneal injection; once daily for 14 days
Result: Significantly decreased tumor volume, but showed a significant body weight reduction after 10 days.
Animal Model: NOD/SCID mice with murine xenograft
Dosage: 50 mg/kg
Administration: Oral gavage; once daily for 14 days
Result: Showed an anti-myeloma activity. Porved oral administration is more effective than intraperitoneal injection.
体内研究

K-7174 dihydrochloride (30 mg/kg; i.p. once daily for 9 days) reverses the decreasing of hemoglobin concentrations and reticulocyte counts by IL-1β or TNF-α.
K-7174 dihydrochloride (75 mg/kg; i.p. once daily for 14 days) inhibits the tumor growth in vivo.
K-7174 dihydrochloride (50 mg/kg; p.o. once daily for 14 days) inhibits the tumor growth in vivo and shows a better effect than intraperitoneal injection.

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

Animal Model: ICR mice with IL-β or TNF-α injection
Dosage: 30 mg/kg
Administration: Intraperitoneal injection; 30 mg/kg once daily for 9 days
Result: Increased erythropoietin (Epo) production, reticulocyte counts, and hemoglobin (Hb) concentrations.
Animal Model: NOD/SCID mice with murine xenograft
Dosage: 75 mg/kg
Administration: Intraperitoneal injection; once daily for 14 days
Result: Significantly decreased tumor volume, but showed a significant body weight reduction after 10 days.
Animal Model: NOD/SCID mice with murine xenograft
Dosage: 50 mg/kg
Administration: Oral gavage; once daily for 14 days
Result: Showed an anti-myeloma activity. Porved oral administration is more effective than intraperitoneal injection.
性状Solid
溶解性数据
In Vitro: 

H2O : 15 mg/mL (23.38 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.5584 mL 7.7922 mL 15.5843 mL
5 mM 0.3117 mL 1.5584 mL 3.1169 mL
10 mM 0.1558 mL 0.7792 mL 1.5584 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 (sealed storage, away from moisture)。-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: PBS

    Solubility: 10 mg/mL (15.58 mM); Clear solution; Need ultrasonic

*以上所有助溶剂都可在 西域 网站选购。
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)

参考文献

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