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Rabacfosadine

Name: Rabacfosadine
Brand: TargetMol
SKU: T16716
Price: 129 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T16716Cas No. 859209-74-8

Alias VDC-1101, GS-9219

Rabacfosadine (GS-9219) is a novel dual pre-drug of the acyclic nucleotide phosphonate PMEG to tumor lymphocytes for the study of lymphoma.

Rabacfosadine

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Purity: 99.37%

Catalog No. T16716Alias VDC-1101, GS-9219Cas No. 859209-74-8

Rabacfosadine (GS-9219) is a novel dual pre-drug of the acyclic nucleotide phosphonate PMEG to tumor lymphocytes for the study of lymphoma.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$129	In Stock	In Stock
5 mg	$322	In Stock	In Stock
10 mg	$479	In Stock	In Stock
25 mg	$768	In Stock	In Stock
50 mg	$1,060	-	In Stock
100 mg	$1,390	-	In Stock
200 mg	$1,870	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.37%

ee:100%

Appearance:Oil

Color:White

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COA CSFC HNMR LCMS

Product Introduction

Bioactivity

Description	Rabacfosadine (GS-9219) is a novel dual pre-drug of the acyclic nucleotide phosphonate PMEG to tumor lymphocytes for the study of lymphoma.
In vitro	Rebaarsen inhibits the proliferation of mitogen-stimulated T and B lymphocytes as determined by BrdUrd binding assay (EC50 135 and 42 nM, respectively). GS-9219 showed strong antiproliferative activity against activated lymphocytes and hematopoietic tumor cell lines. Labafaxadine is converted to its active metabolite, PMEG diphosphate, by enzymatic hydrolysis, deamination and phosphorylation in lymphocytes. In this paper, we investigated the ability of rabafaxadine to inhibit the proliferation of activated lymphocytes and hematopoietic tumor cells. To compare the activity of GS-9219 in dividing and non-dividing cells, the activity of Rabacfosadine in these cell populations was assessed using the metabolism-based XTT sodium assay rather than the BrdUrd assay.The results of the XTT assay showed that the EC50 values of Rabacfosadine differed from those in quiescent (EC50=17.2 μM) and proliferating cells (EC50=135 nM). ) in quiescent cells (EC50=17.2 μM) and proliferating cells (EC50=135 nM) with a 127-fold difference in EC50 values. These results suggest that Rabatadine has a great selectivity for actively replicating lymphoblastoid cells [1].
In vivo	Rabatadine has potent single-agent activity in dogs with lymphoma by a mechanism of action different from that of doxorubicin. Dogs are treated alternately with rabafenacin (1.0 mg/kg, i.v., weeks 0, 6, and 12) and doxorubicin (30 mg/m2, i.v., weeks 3, 9, and 15). Dogs that achieved a complete response (CR) were evaluated at monthly follow-up visits. Complete clinicopathologic evaluations were performed every 21 days and remission and adverse events (AEs) were assessed. Acute AEs (occurring within 21 days of the first dose of each drug) were compared between labradine and doxorubicin in 46 dogs with at least 1 dose of each drug [2].
Synonyms	VDC-1101, GS-9219

Chemical Properties

Molecular Weight	526.53
Formula	C₂₁H₃₅N₈O₆P
Cas No.	859209-74-8
Smiles	C(COCP(N[C@H](C(OCC)=O)C)(N[C@H](C(OCC)=O)C)=O)N1C=2C(=C(NC3CC3)N=C(N)N2)N=C1
Relative Density.	1.50 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 80 mg/mL (151.94 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.27 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.8992 mL	9.4961 mL	18.9923 mL	94.9614 mL
5 mM	0.3798 mL	1.8992 mL	3.7985 mL	18.9923 mL
10 mM	0.1899 mL	0.9496 mL	1.8992 mL	9.4961 mL
20 mM	0.0950 mL	0.4748 mL	0.9496 mL	4.7481 mL
50 mM	0.0380 mL	0.1899 mL	0.3798 mL	1.8992 mL
100 mM	0.0190 mL	0.0950 mL	0.1899 mL	0.9496 mL

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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

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc