| Identification | Back Directory | [Name]
K-7174 | [CAS]
191089-59-5 | [Synonyms]
K-7174
K7174; K 7174
K-7174(FREE BASE)
1H-1,4-Diazepine, hexahydro-1,4-bis[(4E)-5-(3,4,5-trimethoxyphenyl)-4-penten-1-yl]- | [Molecular Formula]
C33H48N2O6 | [MOL File]
191089-59-5.mol | [Molecular Weight]
568.74 |
| Chemical Properties | Back Directory | [Boiling point ]
689.9±55.0 °C(Predicted) | [density ]
1.074±0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [form ]
Oil | [pka]
9.60±0.10(Predicted) | [color ]
Colorless to light yellow |
| Hazard Information | Back Directory | [Uses]
K-7174 is an orally active proteasome and GATA inhibitor. K-7174 is a cell adhesion inhibitor. K-7174 induces cell apoptosis. K-7174 shows antitumor activities, it can be used for the research of cancer[1][2][3]. | [in vivo]
K-7174 (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 (75 mg/kg; i.p. once daily for 14 days) inhibits the tumor growth in vivo[3].
K-7174 (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
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| 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.
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| 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. Proved oral administration is more effective than intraperitoneal injection.
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| [References]
[1] Umetani M, et al. A novel cell adhesion inhibitor, K-7174, reduces the endothelial VCAM-1 induction by inflammatory cytokines, acting through the regulation of GATA. Biochem Biophys Res Commun. 2000 Jun 7;272(2):370-4. DOI:10.1006/bbrc.2000.2784
[2] Imagawa S, et al. A GATA-specific inhibitor (K-7174) rescues anemia induced by IL-1beta, TNF-alpha, or L-NMMA. FASEB J. 2003 Sep;17(12):1742-4. DOI:10.1096/fj.02-1134fje
[3] Kikuchi J, et al. The novel orally active proteasome inhibitor K-7174 exerts anti-myeloma activity in vitro and in vivo by down-regulating the expression of class I histone deacetylases. J Biol Chem. 2013 Aug 30;288(35):25593-602. DOI:10.1074/jbc.M113.480574 |
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| Company Name: |
Musechem
|
| Tel: |
+1-800-259-7612 |
| Website: |
www.musechem.com |
| Company Name: |
Biorbyt Ltd.
|
| Tel: |
+44 (0)1223 859 353 |
| Website: |
http://www.biorbyt.com |
|