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 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 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 | 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。 |
m.cnreagent.com