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LY 254155

Names

[ CAS No. ]:
135503-67-2

[ Name ]:
LY 254155

[Synonym ]:
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

Biological Activity

[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.


[Related Small Molecules]

Levomefolic acid | Folinic acid (Calcium) | Pralatrexate | Calcium Levofolinate | Calcium N5-methyltetrahydrofolate | Diaveridine | LY309887

Chemical & Physical Properties

[ Molecular Formula ]:
C19H23N5O6S

[ Molecular Weight ]:
449.48100

[ Exact Mass ]:
449.13700

[ PSA ]:
215.74000

[ LogP ]:
1.78850

Related Compounds