ChemicalBook CAS DataBase List 1309444-75-4

1309444-75-4

Name	K145
CAS	1309444-75-4
Molecular Formula	C18H24N2O3S
MDL Number	MFCD28167726
Molecular Weight	348.46
MOL File	1309444-75-4.mol

Chemical Properties

solubility	Soluble in DMSO
form	Powder

Hazard Information

Biological Activity

K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with IC50 of 4.3 μM and Ki of 6.4 μM.It is inactive against SphK1 and other protein kinases,it induces apoptosis and has potent antitumor activity.

in vitro

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

Cell Viability Assay

< td class="col2"> U937 cells td>

Cell Line:
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

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

Western Blot Analysis < /p>

Cell Line:	U937 cells
Concentration:	4 μM, 8 μM
Incubation Time: < /td>	3 hours
Result:	Phosphorylated ERK and Akt wer e 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.

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

target

IC50: 4.3 μM (SphK2)
Ki: 6.4 μM (SphK2)

Supplier

ShangHai Caerulum Pharma Discovery Co., Ltd.

Telephone18149758185 18149758185

Websitehttp://www.caerulumpharma.com

LETOPHARM LIMITED

Telephone+86-21-5821 5861

Websitehttp://www.letopharm.com

SPIRO PHARMA

Telephone

Websitehttp://www.spiropharma.com.cn

Beijing Solarbio Science & Tecnology Co., Ltd.

Telephone010-50973130 4009686088

Websitehttp://www.solarbio.com

Amadis Chemical Company Limited

Telephone571-89925085

Websitehttp://www.amadischem.com

Beijing Jin Ming Biotechnology Co., Ltd.

Telephone010-60605840 18892239720

Websitehttp://www.jm-bio.com/

Angel Pharmatech, Ltd.

Telephone 17317130613

Websitehttp://www.angelpharmatech.com

Fan De(Beijing) Biotechnology Co., Ltd.

Telephone 15911056312

Websitehttp://www.bio-fount.com/

Absin Bioscience Inc.

Telephone021-38015121 15000105423

Websitehttps://www.absin.cn/

Chunchuang (Wuhan) Technology Co., Ltd

Telephone 15342225168

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList1427518/0.htm

MedBioPharmaceutical Technology Inc

Telephone021-69568360 18916172912

Websitehttp://www.med-bio.cn/

Beijing Jin Ming Biotechnology Co., Ltd.

Telephone010-60605840 15801484223;

Websitehttp://www.jm-bio.com/

InvivoChem

Telephone 13549236410

Websitehttps://www.invivochem.cn/

TargetMol Chemicals Inc.

Telephone 4008200310

Websitehttps://www.targetmol.cn/

ATK CHEMICAL COMPANY LIMITED

Telephone+undefined-21-51877795

Websitehttp://www.atkchemical.com

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