[CAS NO. 446022-33-9] Pelitrexol
PRODUCTS SPECIFICATIONS [446022-33-9]
DESCRIPTION [446022-33-9]
Overview
| MDL | MFCD13194949 |
|---|---|
| Molecular Weight | 463.51 |
| Molecular Formula | C20H25N5O6S |
| SMILES | O=C(O)CC[C@@H](C(O)=O)NC(C1=CC(C)=C(CC[C@H](CN2)CC3=C2N=C(N)NC3=O)S1)=O |
1 Publications Citing Use of MCE
Summary
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Cycle Analysis [1]
| Cell Line: | NCI-H460 NSCLC |
| Concentration: | 100 nM |
| Incubation Time: | 4, 8, 24, 48 hours |
| Result: | Resulted 63% cells accumulation in G1 phase of the cell cycle. |
Cell Cycle Analysis [1]
| Cell Line: | NCI-H460 NSCLC |
| Concentration: | 0, 10, 30, 100, 300, 1000 nM |
| Incubation Time: | 16 hours |
| Result: | Inhibits the level of p-S6RP, p-S6K1, and p-Chk1. |
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Xenograft model of nonsmall-cell lung cancer (NSCLC) in mice [1] |
| Dosage: | 10 mg/kg, 20 mg/kg |
| Administration: | Intraperitoneal injection; every 4 days for 3 weeks for group 1; administrated at 1, 4, 7 days for group 2 |
| Result: |
Inhibited tumor growth by 64% and 69% at 10 mg/kg and 20 mg/kg, respectively in group 1.
Inhibited mTORC1-dependent phosphorylation of S6K1, S6RP and CAD at 20 mg/kg in group 2. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT00090701 | Pfizer |
Lung Neoplasms
|
September 2004 | Phase 2 |
| NCT00017524 | University of Alabama at Birmingham|National Cancer Institute (NCI) |
Unspecified Adult Solid Tumor, Protocol Specific
|
March 2001 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 25 mg/mL ( 53.94 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1575 mL | 10.7873 mL | 21.5745 mL |
| 5 mM | 0.4315 mL | 2.1575 mL | 4.3149 mL |
| 10 mM | 0.2157 mL | 1.0787 mL | 2.1575 mL |