SML0040

Lometrexol hydrate

≥95% (HPLC), powder, GARFTase inhibitor

• Sinônimo(s): LY 264618 hydrate, N-[4-[2-[(6R)-2-amino-3,4,5,6,7,8-hexahydro-4-oxopyrido[2,3-d]pyrimidin-6-yl]ethyl]benzoyl]-L-glutamic acid hydrate
• Fórmula empírica (Notação de Hill): C₂₁H₂₅N₅O₆ · xH₂O
• Número CAS: 106400-81-1
• Peso molecular: 443.45 (anhydrous basis)
• Código UNSPSC: 12352200
• ID de substância PubChem: 329825110
• NACRES: NA.77

Propriedades

• Nome do produto: Lometrexol hydrate, ≥95% (HPLC)
• Nível de qualidade: 100
• Ensaio: ≥95% (HPLC)
• Formulário: powder
• cor: white to light yellow
• solubilidade: DMSO: ≥5 mg/mL
• temperatura de armazenamento: 2-8°C
• cadeia de caracteres SMILES: O.NC1=NC(=O)C2=C(NC[C@H](CCc3ccc(cc3)C(=O)N[C@@H](CCC(O)=O)C(O)=O)C2)N1
• InChI: 1S/C21H25N5O6.H2O/c22-21-25-17-14(19(30)26-21)9-12(10-23-17)2-1-11-3-5-13(6-4-11)18(29)24-15(20(31)32)7-8-16(27)28;/h3-6,12,15H,1-2,7-10H2,(H,24,29)(H,27,28)(H,31,32)(H4,22,23,25,26,30);1H2/t12-,15+;/m1./s1
• chave InChI: AEFQSKJUVDZANQ-YLCXCWDSSA-N

Descrição

Aplicação

Lometrexol hydrate was used to compare the biological activity of potent inhibitor of human GARFTase.

Ações bioquímicas/fisiológicas

Glycinamide Ribonucleotide Formyltransferase (GARFTase) is a folate-dependent enzyme required for de novo purine synthesis. Lometrexate is a potent inhibitor of GARFTase, but does not interfere with enzymes involved in the synthesis of folate. Lometrexerol has been tested clinically for the treatment of various cancers as an anti-folate like agent, similar to methotrexate. Treatment with lometrexol rapidly decreases ATP and GTP levels, cell cycle arrest and induces apoptosis. Although depletion of nucleotide pools induces p53 expression, lometrexol is cytotoxic in both wild-type and mutant p53 expressing tumor cells. Lometrexol is cytotoxic in CCRF-CEm leukemia cells with an IC50 of 2.9 nM.

Informações de segurança

• Pictogramas: GHS06
• Palavra indicadora: Danger
• Frases de perigo: H301
• Declarações de precaução: P264 - P270 - P301 + P310 - P405 - P501
• Classificações de perigo: Acute Tox. 3 Oral
• Código de classe de armazenamento: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable