Rabacfosadine (Synonyms: GS-9219; VDC-1101)

Cat. No.: HY-13640 Purity: 99.26%: FAQs
Data Sheet SDS COA Handling Instructions

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Rabacfosadine (GS-9219), a novel proagent of the nucleotide analogue PMEG, is designed as a cytotoxic agent that preferentially targets lymphoid cells.

For research use only. We do not sell to patients.

Rabacfosadine Chemical Structure

CAS No. : 859209-74-8

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5 mg	USD 390	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 580	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 930	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1280	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1680	In-stock	Estimated Time of Arrival: December 31
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Other Forms of Rabacfosadine:

Rabacfosadine succinate Get quote

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Biological Activity
Protocol
Purity & Documentation
References
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Description

Rabacfosadine (GS-9219), a novel proagent of the nucleotide analogue PMEG, is designed as a cytotoxic agent that preferentially targets lymphoid cells.

Cellular Effect

Cell Line	Type	Value	Description	References
CCRF-CEM	IC₅₀	0.48 μM Compound: 2, GS-9219	Antiproliferative activity against human CCRF-CEM after 72 hrs by XTT assay Antiproliferative activity against human CCRF-CEM after 72 hrs by XTT assay	[PMID: 21664011]
HeLa S3	IC₅₀	2.15 μM Compound: 2, GS-9219	Antiproliferative activity against human HeLaS3 after 72 hrs by XTT assay Antiproliferative activity against human HeLaS3 after 72 hrs by XTT assay	[PMID: 21664011]
HL-60	IC₅₀	0.78 μM Compound: 2, GS-9219	Antiproliferative activity against human HL60 after 72 hrs by XTT assay Antiproliferative activity against human HL60 after 72 hrs by XTT assay	[PMID: 21664011]

In Vitro

In lymphocytes, Rabacfosadine (GS-9219) is converted to its active metabolite, 9-(2-phosphonylmethoxyethyl)guanine (PMEG) diphosphate, via enzymatic hydrolysis, deamination, and phosphorylation. GS-9219 has substantial antiproliferative activity against activated lymphocytes and hematopoietic tumor cell lines. The ability of Rabacfosadine to inhibit the proliferation of activated lymphocytes and of tumor cells of hematopoietic origin is investigated. Rabacfosadine inhibits the proliferation of mitogen-stimulated T and B lymphocytes with EC₅₀ values of 135 and 42 nM, respectively, as determined by BrdUrd incorporation. To compare the activity of GS-9219 in dividing and nondividing cells, Rabacfosadine is evaluated in these populations using a metabolism-based sodium XTT assay instead of BrdUrd assays. Results from the XTT assay shows a 127-fold difference between the EC₅₀ values of Rabacfosadine in quiescent (EC₅₀=17.2 μM) and proliferating (EC₅₀=135 nM) cells. These results indicate a substantial selectivity of Rabacfosadine toward actively replicating lymphoblasts^[1].

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

In Vivo

Rabacfosadine (RAB) has substantial single-agent activity in dogs with lymphoma, and a different mechanism of action than Doxorubicin (DOX). Open-label, multicenter prospective clinical trial. Dogs receive alternating Rabacfosadine (1.0 mg/kg IV weeks 0, 6, 12) and Doxorubicin (30 mg/m² IV weeks 3, 9, 15). Dogs that achieved complete response (CR) are followed by monthly evaluations. Complete clinicopathological evaluation and assessment of remission and adverse event (AEs) are performed every 21 days. Acute AEs, occurring within 21 days after administration of the first dose of each agent, are compared between Rabacfosadine and Doxorubicin in 46 dogs receiving at least 1 dose of each agent^[2].

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

Clinical Trial

Molecular Weight

526.53

Formula

C₂₁H₃₅N₈O₆P

CAS No.

859209-74-8

Appearance

Solid

Color

Light yellow to yellow

SMILES

CCOC([C@H](C)NP(N[C@@H](C)C(OCC)=O)(COCCN1C=NC2=C(NC3CC3)N=C(N)N=C12)=O)=O

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

In Vitro:

DMSO : 100 mg/mL (189.92 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	1.8992 mL	9.4961 mL	18.9923 mL
5 mM	0.3798 mL	1.8992 mL	3.7985 mL
10 mM	0.1899 mL	0.9496 mL	1.8992 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 2.5 mg/mL (4.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (4.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.75 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.26%

Select Batch:

Data Sheet (283 KB) SDS (252 KB)

COA (255 KB) HNMR (308 KB) LCMS (100 KB)

Handling Instructions (2659 KB)

References

[1]. Reiser H, et al. GS-9219--a novel acyclic nucleotide analogue with potent antineoplastic activity in dogs with spontaneous non-Hodgkin's lymphoma. Clin Cancer Res. 2008 May 1;14(9):2824-32. [Content Brief]

[2]. Thamm DH, et al. Alternating Rabacfosadine/Doxorubicin: Efficacy and Tolerability in Na?ve Canine Multicentric Lymphoma. J Vet Intern Med. 2017 May;31(3):872-878. [Content Brief]

Kinase Assay ^[1]	Twenty million PHA-stimulated T cells are incubated with 10 μM[¹⁴C]GS-9219 for 24 h. Cells are washed once with tissue culture medium and twice with PBS, incubated in 80% methanol overnight, and centrifuged at 14,000 rpm for 15 min to remove denatured proteins. The methanol extracts are lyophilized and dissolved in the high-performance liquid chromatography (HPLC) loading buffer. A portion of each sample is used for scintillation counting to calculate the total pmoles, and the rest is used for HPLC analysis to calculate the ratio of metabolites. HPLC analysis is done by gradient elution using a Phenomenex Prodigy column (5 μm, ODS3 150×4 mm), where buffer A is 25 mM K₂HPO₄ (pH 6.0) and 5 mM Tetrabutylammonium bromide and buffer B is 25 mM K₂HPO₄ (pH 6.0), 70% Acetonitrile, and 5 mM Tetrabutylammonium bromide^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Dogs^[2] Dogs are given alternating doses of Rabacfosadine and Doxorubicin every 3 weeks. Rabacfosadine is administered at a dosage of 1.0 mg/kg as a 30-minute IV infusion on weeks 0, 6, and 12. Doxorubicin is administered at a dosage of 30 mg/m² (1.0 mg/kg for dogs weighing <15 kg) as an approximately 20-minute IV infusion on weeks 3, 9, and 15. Concurrent cytotoxic chemotherapy of any kind and concurrent corticosteroids are not allowed. A CBC is performed 1 week after the first Rabacfosadine and Doxorubicin treatments (weeks 1 and 4). All dogs have a physical examination with lymph node measurements, owner history, CBC, serum biochemistry profile (SBC), and urinalysis performed at each chemotherapy visit. Thoracic radiographs are recommended at week 15 and approximately every 2 months thereafter in responding dogs. Dose delays, reductions, or both, and supportive treatment for AEs are carried out at the discretion of the attending clinician. Dogs that experienced a complete response (CR) are followed with monthly physical examinations after week 15 until relapse, when they are considered off study. Dogs that experienced partial response (PR) or stable disease (SD) at week 15 are considered off study and censored from analysis at that time. At the time of study withdrawal, dogs are eligible for additional treatment at the discretion of the attending clinician. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Reiser H, et al. GS-9219--a novel acyclic nucleotide analogue with potent antineoplastic activity in dogs with spontaneous non-Hodgkin's lymphoma. Clin Cancer Res. 2008 May 1;14(9):2824-32. [Content Brief] [2]. Thamm DH, et al. Alternating Rabacfosadine/Doxorubicin: Efficacy and Tolerability in Na?ve Canine Multicentric Lymphoma. J Vet Intern Med. 2017 May;31(3):872-878. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.8992 mL	9.4961 mL	18.9923 mL	47.4807 mL
	5 mM	0.3798 mL	1.8992 mL	3.7985 mL	9.4961 mL
	10 mM	0.1899 mL	0.9496 mL	1.8992 mL	4.7481 mL
	15 mM	0.1266 mL	0.6331 mL	1.2662 mL	3.1654 mL
	20 mM	0.0950 mL	0.4748 mL	0.9496 mL	2.3740 mL
	25 mM	0.0760 mL	0.3798 mL	0.7597 mL	1.8992 mL
	30 mM	0.0633 mL	0.3165 mL	0.6331 mL	1.5827 mL
	40 mM	0.0475 mL	0.2374 mL	0.4748 mL	1.1870 mL
	50 mM	0.0380 mL	0.1899 mL	0.3798 mL	0.9496 mL
	60 mM	0.0317 mL	0.1583 mL	0.3165 mL	0.7913 mL
	80 mM	0.0237 mL	0.1187 mL	0.2374 mL	0.5935 mL
	100 mM	0.0190 mL	0.0950 mL	0.1899 mL	0.4748 mL

Rabacfosadine 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:

Rabacfosadine859209-74-8GS-9219 VDC-1101GS9219GS 9219VDC1101VDC 1101VDC-1101Nucleoside Antimetabolite/AnalogInhibitorinhibitorinhibit

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