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Sirpiglenastat

Name: Sirpiglenastat
Brand: TargetMol
SKU: T62560
Price: 313 USD
Availability: InStock
Rating: 5 (10 reviews)

(Synonyms: DRP-104) Copy Product Info

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Synonyms: DRP-104

Catalog No. T62560 Copy Product Info

Purity: 98.37%

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Sirpiglenastat (DRP-104) belongs to glutamine antagonist prodrugs and is a broad-spectrum glutamine metabolism inhibitor with tumor-selective activation, good tolerability, and oral activity. This compound is used in therapeutic research on various solid tumors.

Cas No. 2079939-05-0

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Pack Size	Price	USA Stock	Global Stock
1 mg	$313	In Stock	In Stock
5 mg	$943	In Stock	In Stock
10 mg	$1,270	In Stock	In Stock
25 mg	$1,880	In Stock	In Stock
50 mg	$2,530	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$917	In Stock	In Stock

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Batch Information

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Purity:98.37%

Appearance:Solid

Color:Yellow

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COA HPLC HNMR

Product Introduction

Bioactivity

Description	Sirpiglenastat (DRP-104) belongs to glutamine antagonist prodrugs and is a broad-spectrum glutamine metabolism inhibitor with tumor-selective activation, good tolerability, and oral activity. This compound is used in therapeutic research on various solid tumors.
In vitro	Methods:Sirpiglenastat was incubated in HY19636 pancreatic ductal adenocarcinoma cells at a concentration of 25 μM for 24 hours, validated by metabolomic analysis. Results: Sirpiglenastat extensively inhibited glutamine metabolic pathways, inducing cellular metabolic crisis.[1] Methods:Cell viability assays were used to validate Sirpiglenastat in vitro activity in head and neck squamous cell carcinoma (HNSCC) cell lines (CAL27, CAL33, HN12, SCC47, Detroit 562), with cells incubated with serial concentrations of Sirpiglenastat (DRP-104) for 72 hours. Results: Sirpiglenastat effectively inhibited HNSCC cell proliferation, with a growth inhibition concentration 50 (GI₅₀) comparable to DON, indicating that this prodrug can be effectively activated in HNSCC cells.[2]
In vivo	Methods: The in vivo activity of Sirpiglenastat was validated in a head and neck squamous cell carcinoma (HNSCC) subcutaneous xenograft model in SCID/NSG mice. Sirpiglenastat was administered by subcutaneous injection at a dose of 3 mg/kg on a 5 days on/2 days off schedule for 4 weeks, with vehicle diluent as the solvent control. Results: Sirpiglenastat significantly inhibited tumor growth, reduced tumor weight, and improved survival rates in the model mice. [3]
Synonyms	DRP-104

Chemical Properties

Molecular Weight	441.48
Formula	C₂₂H₂₇N₅O₅
Cas No.	2079939-05-0
Smiles	C([C@@H](C(N[C@H](C(OC(C)C)=O)CCC(C=[N+]=[N-])=O)=O)NC(C)=O)C=1C=2C(NC1)=CC=CC2

Storage & Solubility Information

Storage

Keep away from direct sunlight,Keep away from moisture,Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 90.5 mg/mL (204.99 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2651 mL	11.3255 mL	22.6511 mL	113.2554 mL
5 mM	0.4530 mL	2.2651 mL	4.5302 mL	22.6511 mL
10 mM	0.2265 mL	1.1326 mL	2.2651 mL	11.3255 mL
20 mM	0.1133 mL	0.5663 mL	1.1326 mL	5.6628 mL
50 mM	0.0453 mL	0.2265 mL	0.4530 mL	2.2651 mL
100 mM	0.0227 mL	0.1133 mL	0.2265 mL	1.1326 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Keywords

Glutaminase

Related Tags: Sirpiglenastat chemical structure | Sirpiglenastat in vivo | Sirpiglenastat in vitro | Sirpiglenastat formula | Sirpiglenastat molecular weight