[CAS NO. 1449240-68-9] K145hydrochloride

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PRODUCTS SPECIFICATIONS [1449240-68-9]

Catalog

HY-15779A

Brand

MCE

CAS

1449240-68-9

DESCRIPTION [1449240-68-9]

Overview

MDL	MFCD28160629
Molecular Weight	384.92
Molecular Formula	C18H25ClN2O3S
SMILES	O=C(N(CCN)C/1=O)SC1=C/CCC2=CC=C(OCCCC)C=C2.[H]Cl

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

6 Publications Citing Use of MCE

Summary

K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC ₅₀ of 4.3 µM and a K _i of 6.4 µM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity ^[1] .

IC50 & Target

IC50: 4.3 µM (SphK2) ^[1]
Ki: 6.4 µM (SphK2) ^[1]

In Vitro

K145 (0-10 µM; 24-72 hours; U937 cells) treatment significantly inhibits the growth of U937 cells in a concentration-dependent manner ^[1] .
K145 (10 µM; 24 hours; U937 cells) treatment significantly induces apoptosis in U937 cells ^[1] .
K145 (4-8 µM; 3 hours; U937 cells) treatment decreases the phosphorylation of ERK and Akt ^[1] .
Treatment with K145 (10 µM) causes a decrease of total cellular S1P without significant effects on ceramide levels ^[1] .

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

Cell Viability Assay ^[1]

Cell Line:	U937 cells
Concentration:	0 µM, 4 µM, 6 µM, 8 µM, 10 µM
Incubation Time:	24 hours, 48 hours, 72 hours
Result:	Significantly inhibited the growth of U937 cells in a concentration-dependent manner.

Apoptosis Analysis ^[1]

Cell Line:	U937 cells
Concentration:	10 µM
Incubation Time:	24 hours
Result:	Significantly induced apoptosis in U937 cells.

Western Blot Analysis ^[1]

Cell Line:	U937 cells
Concentration:	4 µM, 8 µM
Incubation Time:	3 hours
Result:	Phosphorylated ERK and Akt were decreased.

In Vivo

K145 (50 mg/kg; oral gavage; daily; for 15 days; BALB/c-nu mice) treatment significantly inhibits the growth of U937 tumors in nude mice ^[1] .

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

Animal Model:	BALB/c-nu mice injected with U937 cells ^[1]
Dosage:	50 mg/kg
Administration:	Oral gavage; daily; for 15 days
Result:	Inhibited the growth of U937 tumors at 50 mg/kg dose and no apparent toxicity was observed.

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 : 126.7 mg/mL ( 329.16 mM ; Need ultrasonic and warming)

DMSO : 50 mg/mL ( 129.90 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5979 mL	12.9897 mL	25.9794 mL
5 mM	0.5196 mL	2.5979 mL	5.1959 mL
10 mM	0.2598 mL	1.2990 mL	2.5979 mL

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

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 0.83 mg/mL (2.16 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 0.83 mg/mL (2.16 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 0.83 mg/mL (2.16 mM); Clear solution

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

References

[1] Liu K, et al. Biological characterization of 3-(2-amino-ethyl)-5-[3-(4-butoxyl-phenyl)-propylidene]-thiazolidine-2,4-dione (K145) as a selective sphingosine kinase-2 inhibitor and anticancer agent. PLoS One. 2013;8(2):e56471.