[CAS NO. 191089-60-8] K-7174dihydrochloride

Name: K-7174dihydrochloride
Brand: Arctom Scientific
SKU: AS952229

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PRODUCTS SPECIFICATIONS [191089-60-8]

Distributor

Catalog

AS952229

Brand

Arctom Scientific

CAS

191089-60-8

DESCRIPTION [191089-60-8]

Overview

MDL	-
Molecular Weight	641.67
Molecular Formula	C33H50Cl2N2O6
SMILES	COC1=C(OC)C(OC)=CC(/C=C/CCCN2CCN(CCC/C=C/C3=CC(OC)=C(OC)C(OC)=C3)CCC2)=C1.[H]Cl.[H]Cl

For research use only. We do not sell to patients.

8 Publications Citing Use of MCE

Summary

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 ^[1] ^[2] ^[3] .

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 IC ₅₀ value 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 IC ₅₀ value 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] .

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

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.

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] .

MCE 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 ^[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.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

H ₂ O : 15 mg/mL ( 23.38 mM ; Need ultrasonic and warming)

Preparing
Stock Solutions

Concentration Solvent Mass	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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

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

* All of the co-solvents are available by MCE.

References

Synonyms

1H-1,4-Diazepine, hexahydro-1,4-bis[(4E)-5-(3,4,5-trimethoxyphenyl)-4-penten-1-yl]-, hydrochloride (1:2)

1H-1,4-Diazepine, hexahydro-1,4-bis[5-(3,4,5-trimethoxyphenyl)-4-pentenyl]-, dihydrochloride, (E,E)-