2. Cell Cycle/DNA Damage
  3. Antifolate
  4. Pelitrexol

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.

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Pelitrexol Chemical Structure

Pelitrexol Chemical Structure

CAS No. : 446022-33-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 638 In-stock
Solution
10 mM * 1 mL in DMSO USD 638 In-stock
Solid
1 mg USD 232 In-stock
5 mg USD 580 In-stock
10 mg USD 880 In-stock
50 mg USD 2500 In-stock
100 mg USD 4000 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Pelitrexol Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Pelitrexol

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

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

Pelitrexol Related Antibodies

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].

MedChemExpress (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
Molecular Weight

463.51

Formula

C20H25N5O6S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (53.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.49 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.49 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 98.94%

COA (248 KB) LCMS (268 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1575 mL 10.7873 mL 21.5745 mL 53.9363 mL
5 mM 0.4315 mL 2.1575 mL 4.3149 mL 10.7873 mL
10 mM 0.2157 mL 1.0787 mL 2.1575 mL 5.3936 mL
15 mM 0.1438 mL 0.7192 mL 1.4383 mL 3.5958 mL
20 mM 0.1079 mL 0.5394 mL 1.0787 mL 2.6968 mL
25 mM 0.0863 mL 0.4315 mL 0.8630 mL 2.1575 mL
30 mM 0.0719 mL 0.3596 mL 0.7192 mL 1.7979 mL
40 mM 0.0539 mL 0.2697 mL 0.5394 mL 1.3484 mL
50 mM 0.0431 mL 0.2157 mL 0.4315 mL 1.0787 mL
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Pelitrexol Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pelitrexol446022-33-9AG 2037AG2037AG-2037Antifolatechemoenzymatic processoxalamic esterRhebobligate activatorgrowth suppression10-formyltetrahydrofolate:5'-phosphoribosylglycinamide N-formyltransferaseInhibitorinhibitorinhibit

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