135503-67-2

135503-67-2 structure

Name: LY 254155
Chemical Name: N-[[5-[2-(2-amino-1,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]-pyrimidin-6-yl)ethyl]-2-thienyl]carbonyl]-L-glutamic acid
CAS Number: 135503-67-2
Molecular Formula: C₁₉H₂₃N₅O₆S
Molecular Weight: 449.48100
Catalog: Signaling Pathways Cell Cycle/DNA Damage Antifolate
Create Date: 2017-05-19 21:36:40
Modify Date: 2024-01-13 15:14:47
LY 254155, an antifolate, inhibits hGARFT and binds to mFBP with Kis of 2.1±0.2 and 1.7±0.1 nM, respectively.

Name	N-[[5-[2-(2-amino-1,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]-pyrimidin-6-yl)ethyl]-2-thienyl]carbonyl]-L-glutamic acid
Synonyms	N-[[5-[2-[2-Amino-1,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl)ethyl]-thien-2-yl]carbonyl]-L-glutamic Acid

Description	LY 254155, an antifolate, inhibits hGARFT and binds to mFBP with Kis of 2.1±0.2 and 1.7±0.1 nM, respectively.
Related Catalog	Signaling Pathways >> Cell Cycle/DNA Damage >> Antifolate Research Areas >> Cancer
Target	Ki: 2.1±0.2 (hGARFT ), 1.7± 0.1 nM (mFBP)[1]
In Vitro	LY 254155 inhibits recombinant human monofunctional glycinamide ribonucleotide formyltransferase (hGARFT) and binds to membrane folate-binding protein (mFBP) [1].
In Vivo	LY 254155 is active against a broad panel of murine and human xenograft solid tumors. LY 254155 (5, 10, 20, and 40 mg/kg) inhibits murine C3H carcinoma growth in C3H mice, with % inhibition of tumor growth is 49%, 71%, 90%, and 94%, respectively[1].
Animal Admin	Mice[1] C3H mice are used. LY 254155 is dosed on days 1, 4, 7, and 10 (4 treatment days). Cumulative dose is calculated using the formula (daily dose×number of treatment days). Doses are administered in mg of LY 254155 per kg of mouse weight (5, 10, 20, and 40 mg/kg), and 10 mice are inoculated at each dosing level, including a no-compound control group. % inhibition of tumor growth is calculated[1].
References	[1]. Habeck LL, et al. A novel class of monoglutamated antifolates exhibits tight-binding inhibition of humanglycinamide ribonucleotide formyltransferase and potent activity against solid tumors. Cancer Res. 1994 Feb 15;54(4):1021-6.