[CAS NO. 18550-98-6] 3PO

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PRODUCTS SPECIFICATIONS [18550-98-6]

Catalog

SLK-S7639

Brand

Selleck

CAS

18550-98-6

DESCRIPTION [18550-98-6]

Overview

MDL	-
Molecular Weight	210.23
Molecular Formula	C13H10N2O
SMILES	O=C(C1=CC=NC=C1)/C=C/C2=CC=CN=C2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	4.7567 mL	23.7835 mL	47.5670 mL
5 mM	0.9513 mL	4.7567 mL	9.5134 mL
10 mM	0.4757 mL	2.3783 mL	4.7567 mL
50 mM	0.0951 mL	0.4757 mL	0.9513 mL

Description

3PO (3-(3-pyridinyl)-1-(4-pyridinyl)-2-propen-1-one) is a small-molecule inhibitor of with an IC50 of 22.9 μM for recombinant human PFKFB3 protein and does not inhibit PFK-1 activity. It suppresses glucose uptake, and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.

Targets

PFKFB3 ^[2]

22.9 μM

In vitro

3PO is an inhibitor of the PFKFB3 isozyme primarily through competition with Fru-6-P and does not inhibit purified PFK-1 activity. 3PO markedly attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines (IC50, 1.4-24 μmol/L) and is selectively cytostatic to ras-transformed human bronchial epithelial cells relative to normal human bronchial epithelial cells. 3PO can cause G2-M phase arrest.

In vivo

i.p. administration of 3PO (0.07 mg/g) to tumor-bearing mice markedly reduces the intracellular concentration of Fru-2,6-BP, glucose uptake, and growth of established tumors in vivo. It suppresses tumorigenic growth of breast adenocarcinoma, leukemia, and lung adenocarcinoma cells in vivo. The PK properties of 3PO are examined in C57Bl/6 mice intravenously administered 3PO: clearance CL=2312 mL/min/kg, T=0.3 hr, C=113 ng/ml, AUC=36 ng/hr/ml. 3PO is reported to have potent activity against a highly relevant mouse model of leukemia.

References

[1] Clem B, et al. Mol Cancer Ther. 2008, 7(1):110-20.
[2] Clem BF, et al. Mol Cancer Ther. 2013, 12(8):1461-70.