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A12B4C3

Names

[ CAS No. ]:
1005129-80-5

[ Name ]:
A12B4C3

[Synonym ]:
4a,7a-Dihydro-2-(1-hydroxyundecyl)-1-[(4-nitrophenyl)amino]-6-phenyl-1H-pyrrolo[3,4-b]pyridine-5,7(2H,6H)-dione
2-(1-hydroxyundecyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7-(2H,4aH)dione
A12B4C3

Biological Activity

[Description]:

A12B4C3 is a potent human polynucleotide kinase/phosphatase (hPNKP) inhibitor with an IC50 value of 0.06 μM. A12B4C3 has antiproliferative activity against cancer cells. A12B4C3 can also enhance the radiosensitivity of certain cancer cells[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Others >> Others

[Target]

IC50: 0.06 μM (hPNKP)[1]


[In Vitro]

A12B4C3 (0-10 μM) strongly inhibits hPNKP phosphatase activity[1]. A12B4C3 (0-100 μM; 72 h) reduces A549 and MDA-MB-231 cell proliferation in a dose dependent manner[1]. A12B4C3 (1 μM; 24 h) increases the radiosensitivity of A549 cells[1]. Cell Proliferation Assay[1] Cell Line: A549 and MDA-MB-231 Concentration: 0, 1, 5, 10, 50 and 100 μM Incubation Time: 72 h Result: Reduced cell proliferation in a dose dependent manner, and up to ~50% at 100 μM. Cell Proliferation Assay[1] Cell Line: A549 and MDA-MB-231 (incubated with A12B4C3 for 2h then irradiated 0-10 Gy) Concentration: 1 μM Incubation Time: 24 h Result: Almost doubled the radiosensitivity of A549 cells.

[References]

[1]. Freschauf GK, et al. Identification of a small molecule inhibitor of the human DNA repair enzyme polynucleotide kinase/phosphatase. Cancer Res. 2009 Oct 1;69(19):7739-46.

Chemical & Physical Properties

[ Molecular Formula ]:
C30H38N4O5

[ Molecular Weight ]:
534.64700

[ Exact Mass ]:
534.28400

[ PSA ]:
118.70000

[ LogP ]:
6.21110

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301

[ Precautionary Statements ]:
P301 + P310

[ RIDADR ]:
UN 2811 6.1 / PGIII

Related Compounds

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