ChemicalBook CAS DataBase List 191089-59-5

191089-59-5

Name	K-7174
CAS	191089-59-5
Molecular Formula	C33H48N2O6
Molecular Weight	568.74
MOL File	191089-59-5.mol

Chemical Properties

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

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

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. Proved oral administration is more effective than intraperitoneal injection.

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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