1. Cell Cycle/DNA Damage
  2. Antifolate

LY 254155 

Cat. No.: HY-14523
Handling Instructions

LY 254155, an antifolate, inhibits hGARFT and binds to mFBP with Kis of 2.1±0.2 and 1.7±0.1 nM, respectively.

For research use only. We do not sell to patients.

LY 254155 Chemical Structure

LY 254155 Chemical Structure

CAS No. : 135503-67-2

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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.

IC50 & 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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2248 mL 11.1240 mL 22.2479 mL
5 mM 0.4450 mL 2.2248 mL 4.4496 mL
10 mM 0.2225 mL 1.1124 mL 2.2248 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

449.48

Formula

C₁₉H₂₃N₅O₆S

CAS No.

135503-67-2

SMILES

O=C1C2=C(NCC(CCC(S3)=CC=C3C(N[[email protected]@H](CCC(O)=O)C(O)=O)=O)C2)N=C(N)N1

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
LY 254155
Cat. No.:
HY-14523
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LY 254155

Cat. No.: HY-14523