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Pelitrexol


CAS No. : 446022-33-9

(Synonyms: AG 2037)

446022-33-9
Price and Availability of CAS No. : 446022-33-9
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1mg $232 In-stock
5mg $580 In-stock
10mg $880 In-stock
50mg $2500 In-stock
100mg $4000 In-stock
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Cat. No. : HY-14530
M.Wt: 463.51
Formula: C20H25N5O6S
Purity: >98 %
Solubility: DMSO : 25 mg/mL (ultrasonic)
Introduction of 446022-33-9 :

Pelitrexol (AG 2037) is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), a purine biosynthetic enzyme. Pelitrexol also inhibits mTORC1 by reducing GTP-bound Rheb level, a mTORC1 obligate activator. Pelitrexol shows robust tumor growth suppression in mice[1]. IC50 & Target: GARFT[1] In Vitro: Pelitrexo (150 nM; 24 h) profoundly inhibits mTORC1 activity by reducing intracellular guanine nucleotides level as well as GTP-bound Rheb protein level in A549 cells[1].
Pelitrexo (0-1000 mM; 16 h) strongly inhibits the phosphorylation level of ribosomal protein S6 (S6RP), S6K1, and Chk1 in a dose-dependent manner in NCI-H460 cells[1].
Pelitrexo (100 nM; 48 h) arrests cell cycle at G1 phase in NCI-H460 cells[1].
In Vivo: Pelitrexo (10 mg/kg, 20 mg/kg; i.p.; every 4 days for 3 weeks) provokes both mTORC1 inhibition and robust tumor growth suppression in mice bearing nonsmall-cell lung cancer (NSCLC) xenografts[1].
Pelitrexo (20 mg/kg; i.p.; every 4 days for 3 weeks) inhibits GARFT-dependent purine biosynthesis and blocks mTORC1 function[1].

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