K-7174 dihydrochloride

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

191089-60-8

K-7174 dihydrochloride 是具有口服活性的proteasome和GATA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 activeproteasomeandGATAinhibitor. K-7174 dihydrochloride is acell adhesioninhibitor. K-7174 dihydrochloride induces cellapoptosis. K-7174 dihydrochloride shows antitumor activities, it can be used for the research ofcancer^[1]^[2]^[3].

体外研究
(In Vitro)

K-7174 dihydrochloride (10 μM; 1 h) inhibits the adhesion by VCAM-1 and its ligand^[1].
K-7174 dihydrochloride (1-30 μM; 1 h) dose-dependently suppresses the VCAM-1 expression with an IC₅₀value of 14 μM^[1].
K-7174 dihydrochloride (1-30 μM; 1 h) dose-dependently suppresses the induction of VCAM-1 mRNA by TNFα with an IC₅₀value of 9 μM^[1].
K-7174 dihydrochloride (10-20 μM; 24 h) dose-dependently rescues Epo production by Hep3B cells^[2].
K-7174 dihydrochloride (2.5-30 μM; 24 h) inhibits the binding activity of GATA^[2].
K-7174 dihydrochloride (0-25 μM; 72 h) inhibits MM cells growth and induces cell apoptosis^[3].

Cell Viability Assay^[3]

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

Apoptosis Analysis^[3]

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^[2].
K-7174 dihydrochloride (75 mg/kg; i.p. once daily for 14 days) inhibits the tumor growth in vivo^[3].
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^[3].

Animal Model:	ICR mice with IL-β or TNF-α injection^[2]
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^[3]
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^[3]
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.

分子量

641.67

性状

Solid

Formula

C₃₃H₅₀Cl₂N₂O₆

CAS 号

191089-60-8

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)

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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本网站选购。