127228-54-0

127228-54-0 structure

Name: LY309887
Chemical Name: N-[(5-{2-[(6R)-2-Amino-4-oxo-1,4,5,6,7,8-hexahydropyrido[2,3-d]py rimidin-6-yl]ethyl}-2-thienyl)carbonyl]-L-glutamic acid
CAS Number: 127228-54-0
Molecular Formula: C₁₉H₂₃N₅O₆S
Molecular Weight: 449.48100
Catalog: Signaling Pathways Cell Cycle/DNA Damage Antifolate
Create Date: 2017-04-20 13:19:17
Modify Date: 2024-01-16 16:27:10
LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 6.5 nM, and has antitumor activity.

Name	N-[(5-{2-[(6R)-2-Amino-4-oxo-1,4,5,6,7,8-hexahydropyrido[2,3-d]py rimidin-6-yl]ethyl}-2-thienyl)carbonyl]-L-glutamic acid
Synonyms	LY309887

Description	LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 6.5 nM, and has antitumor activity.
Related Catalog	Signaling Pathways >> Cell Cycle/DNA Damage >> Antifolate Research Areas >> Cancer
Target	Ki: 6.5 nM (GARFT), 1.78 nM (Folate receptor α), 18.2 nM (Folate receptor β)[1]
In Vitro	LY309887 is a potent inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 6.5 nM for human GARFT and also has high affinity at human folate receptor (FR)α and FRβ (Ki, 1.78 nM and 18.2 nM, respectively). LY309887 is signigicantly cytotoxic against the human leukemia cell line CCRF-CEM with IC50 of 9.9 nM[1].
In Vivo	LY309887 (3 mg/kg-100 mg/kg, i.p.) shows complete inhibition on the tumor growth in mice bearing C3H mammary cancer cells[1].
References	[1]. Mendelsohn LG, et al. Biochemistry and pharmacology of glycinamide ribonucleotide formyltransferase inhibitors: LY309887 and lometrexol. Invest New Drugs. 1996;14(3):287-94.