CI 972 (anhydrous)

Names

[ CAS No. ]:
115787-68-3

[ Name ]:
CI 972 (anhydrous)

[Synonym ]:
ci 972

Biological Activity

[Description]:

CI 972 anhydrous is a potent, orally active, and competitive inhibitor of purine nucleoside phosphorylase (PNP) (Ki=0.83 μM) under development as a T cell-selective immunosuppressive agent[1][2].

[Related Catalog]:

Signaling Pathways >> Cell Cycle/DNA Damage >> Nucleoside Antimetabolite/Analog
Research Areas >> Inflammation/Immunology

[Target]

Ki: 0.83 μM (PNP)[1]


[In Vivo]

CI 972 anhydrous (5-150 mg/kg; p.o.) produces dose-dependent elevation of plasma inosine one hour after administration to rats[1].

[References]

[1]. Gilbertsen RB, et al. Biochemical and pharmacological properties of CI-972, a novel 9-deazaguanine analog purine nucleoside phosphorylase (PNP) inhibitor. Adv Exp Med Biol. 1991;309A:41-4.

[2]. Gilbertsen RB,et al. Selective in vitro inhibition of human MOLT-4 T lymphoblasts by the novel purine nucleoside phosphorylase inhibitor, CI-972. Biochem Biophys Res Commun. 1991 Aug 15;178(3):1351-8.

Chemical & Physical Properties

[ Boiling Point ]:
602.2ºC at 760mmHg

[ Molecular Formula ]:
C11H12ClN5OS

[ Molecular Weight ]:
297.76400

[ Flash Point ]:
318ºC

[ Exact Mass ]:
297.04500

[ PSA ]:
142.55000

[ LogP ]:
2.38120

[ Vapour Pressure ]:
1.87E-14mmHg at 25°C

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds