Pyrazoloacridine

Pyrazoloacridine (NSC 366140), an intercalating agent with anti-cancer activity, inhibits the activity of topoisomerases 1 and 2. Pyrazoloacridine (NSC 366140) exhibits an IC50 of 1.25 μM in K562 myeloid leukemia cells for 24 h treatment[1][2].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Topoisomerase

Pyrazoloacridine (NSC 366140, PD 115934) exhibits IC50 values of 10.7 μM and 4.5 μM for oxic and hypoxic HCT-8 cells[1]. Pyrazoloacridine (NSC 366140, 2-4 μM) abolishes the catalytic activity of both topo I and topo II in vitro[2]. Pyrazoloacridine (NSC 366140) displays activity against cisplatin- and paclitaxel-resistant ovarian cancer[2]. Pyrazoloacridine (NSC 366140) has been shown to cause delayed DNA fragmentation in MCF-7 breast cancer cells[2]. Pyrazoloacridine (NSC 366140) induces apoptosis in P53-deficient Hep 3B human hepatoma cells[2]. Cell Cytotoxicity Assay[2] Cell Line: K562 Myeloid Leukemia Cells. Concentration: 0-500 μM. Incubation Time: 1 h or 24 h. Result: When K562 cells were incubated with PA for 1 h and then plated in soft agar, an IC50 of -50 μM was observed. In contrast, when cells were incubated for 24 h with PA, the IC50 was 1.25 μM.

[1]. J S Sebolt, et al. Pyrazoloacridines, a new class of anticancer agents with selectivity against solid tumors in vitro. Cancer Res. 1987 Aug 15;47(16):4299-304.

[2]. A A Adjei, et al. Effect of pyrazoloacridine (NSC 366140) on DNA topoisomerases I and II. Clin Cancer Res. 1998 Mar;4(3):683-91.

MOLECULAR FORMULA :

C19-H21-N5-O3

MOLECULAR WEIGHT :

367.45

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

MUTATION DATA

TYPE OF TEST :

Mutation test systems - not otherwise specified

TEST SYSTEM :

Rodent - mouse Leukocyte

DOSE/DURATION :

1320 nmol/L

REFERENCE :

CNREA8 Cancer Research. (Public Ledger Building, Suit 816, 6th & Chestnut Sts., Philadelphia, PA 19106) V.1- 1941- Volume(issue)/page/year: 47,4299,1987