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

Product information

CAS Number: 135503-67-2

Molecular Weight: 449.48

Formula: C19H23N5O6S

Chemical Name: (2S)-2-{[5-(2-{2-amino-4-oxo-3H,4H,5H,6H,7H,8H-pyrido[2,3-d]pyrimidin-6-yl}ethyl)thiophen-2-yl]formamido}pentanedioic acid

Smiles: NC1NC(=O)C2CC(CNC=2N=1)CCC1=CC=C(S1)C(=O)N[C@@H](CCC(O)=O)C(O)=O

InChiKey: GQCXGHHHNACOGE-ACGXKRRESA-N

InChi: InChI=1S/C19H23N5O6S/c20-19-23-15-11(16(27)24-19)7-9(8-21-15)1-2-10-3-5-13(31-10)17(28)22-12(18(29)30)4-6-14(25)26/h3,5,9,12H,1-2,4,6-8H2,(H,22,28)(H,25,26)(H,29,30)(H4,20,21,23,24,27)/t9?,12-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

LY 254155 inhibits recombinant human monofunctional glycinamide ribonucleotide formyltransferase (hGARFT) and binds to membrane folate-binding protein (mFBP) .

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.

Products are for research use only. Not for human use.