[CAS NO. 1025687-58-4] FostamatinibDisodium

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PRODUCTS SPECIFICATIONS [1025687-58-4]

Catalog

HY-13038

Brand

MCE

CAS

1025687-58-4

DESCRIPTION [1025687-58-4]

Overview

MDL	MFCD15146370
Molecular Weight	624.42
Molecular Formula	C23H24FN6Na2O9P
SMILES	COC1=CC(NC2=NC=C(C(NC3=NC(N4COP(O[Na])(O[Na])=O)=C(C=C3)OC(C)(C)C4=O)=N2)F)=CC(OC)=C1OC

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

7 Publications Citing Use of MCE

Summary

Fostamatinib Disodium (R788 Disodium) is the oral prodrug of the active compound R406 ^[1] . R406 is an orally available and competitive Syk/FLT3 inhibitor with a K _i of 30 nM and an IC ₅₀ of 41 nM ^[2] . R406 also inhibits Lyn (IC ₅₀ =63 nM) and Lck (IC ₅₀ =37 nM) ^[3] .

IC50 & Target

Syk, FLT3 ^[2]

In Vivo

Fostamatinib (R788) is highly bioavailable, and rapidly absorbed in Louvain rats. R406 following a single oral dose of R788 10 mg/kg or 20 mg/kg: AUC _{0-16 hrs} = 10618 ng*h/mL and 30650 ng*h/mL respectively; C _max =2600 ng/mL and 6500 ng/mL respectively (observed at 1 hour); t _1/2 =4.2 hours. The prodrug was not detected in plasma suggesting R788 is completely converted to R406 ^[1] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT05509582	National Heart, Lung, and Blood Institute (NHLBI)\|National Institutes of Health Clinical Center (CC)	Immune Mediated Anemia\|Immune Mediated Thrombocytopenia\|Chronic GVHD	November 28, 2022	Phase 2
NCT04543279	Washington University School of Medicine\|Rigel Pharmaceuticals	Myelofibrosis	May 3, 2021	Phase 2
NCT01242514	AstraZeneca	Rheumatoid Arthritis	January 2011	Phase 3
NCT01197534	AstraZeneca	Rheumatoid Arthritis	September 2010	Phase 3
NCT01563978	AstraZeneca	Rheumatoid Arthritis	April 2012	Phase 2
NCT01197521	AstraZeneca	Rheumatoid Arthritis	September 2010	Phase 3
NCT00446095	Rigel Pharmaceuticals	Lymphoma	April 2007	Phase 1\|Phase 2
NCT01355354	AstraZeneca	Healthy Volunteers\|Rheumatoid Arthritis	June 2011	Phase 1
NCT01569074	AstraZeneca	Rheumatoid Arthritis	April 2012	Phase 2
NCT01222455	AstraZeneca	Hepatic Impairment\|Healthy Volunteers\|Pharmacokinetics\|Amount of R406 in Blood	October 2010	Phase 1
NCT00805467	AstraZeneca	Rheumatoid Arthritis	August 2008	Phase 2
NCT01725230	AstraZeneca	Rheumatoid Arthritis	November 2012	Phase 1
NCT02077192	Rigel Pharmaceuticals	Immune Thrombocytopenic Purpura	July 2014	Phase 3
NCT01245790	AstraZeneca	Rheumatoid Arthritis\|Renal Impairment	November 2010	Phase 1
NCT03246074	Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins\|Rigel Pharmaceuticals\|Allegheny Singer Research Institute (also known as Allegheny Health Network Research Institute)	Ovarian Cancer	April 3, 2018	Phase 1
NCT04904276	Rigel Pharmaceuticals	ITP\|Immune Thrombocytopenia	May 18, 2021
NCT01197755	AstraZeneca	Rheumatoid Arthritis	September 2010	Phase 3
NCT02076399	Rigel Pharmaceuticals	Immune Thrombocytopenic Purpura	July 14, 2014	Phase 3
NCT01499303	AstraZeneca	Diffuse Large B-Cell Lymphoma	December 2011	Phase 2
NCT01311622	AstraZeneca	Rheumatoid Arthritis\|Healthy Subjects	March 2011	Phase 1
NCT04132050	Kissei Pharmaceutical Co., Ltd.	Idiopathic Thrombocytopenic Purpura	December 24, 2019	Phase 3
NCT02076412	Rigel Pharmaceuticals	Immune Thrombocytopenic Purpura	January 2015	Phase 3
NCT02092961	AstraZeneca	Rheumatoid Arthritis	February 2011	Phase 2
NCT01682408	AstraZeneca	Pharmacokinetics	September 2012	Phase 1
NCT01336218	AstraZeneca	Rheumatoid Arthritis\|Healthy Volunteers	April 2011	Phase 1
NCT00326339	Rigel Pharmaceuticals	Rheumatoid Arthritis	August 2006	Phase 2
NCT05502783	National Heart, Lung, and Blood Institute (NHLBI)\|National Institutes of Health Clinical Center (CC)	Immune Mediated Anemia\|Immune Mediated Thrombocytopenia\|Chronic GVHD	November 28, 2022	Phase 2
NCT03991780	Imperial College London	Renal Transplant Rejection	May 8, 2019	Phase 1\|Phase 2
NCT00665626	Rigel Pharmaceuticals	Rheumatoid Arthritis	May 2008	Phase 2
NCT01309854	AstraZeneca	Rheumatoid Arthritis\|Healthy Volunteers\|Pharmacokinetics\|Pioglitazone\|Drug-drug Interaction\|Amount of Pioglitazone in Blood	March 2011	Phase 1
NCT05030675	M.D. Anderson Cancer Center\|National Cancer Institute (NCI)	Refractory Chronic Myelomonocytic Leukemia\|Refractory Myelodysplastic Syndrome	August 13, 2021	Phase 1
NCT01208155	AstraZeneca	Bioavailability\|Pharmacokinetics	September 2010	Phase 1
NCT01276262	AstraZeneca	Scientific Terminology Rheumatoid Arthritis, Healthy Female Volunteers, Pharmacokinetics, Oral Contraceptive, Drug-drug Interaction\|Laymen Terminology Level of Oral Contraceptive in Blood, Oral Contraceptive, Rheumatoid Arthritis, Drug -Drug Interaction	March 2011	Phase 1
NCT04138927	Rigel Pharmaceuticals	Warm Antibody Autoimmune Hemolytic Anemia	October 30, 2019	Phase 3
NCT01608542	AstraZeneca	Healthy Japanese Volunteers	June 2012	Phase 1
NCT02612558	Rigel Pharmaceuticals	Warm Antibody Autoimmune Hemolytic Anemia	July 2016	Phase 2
NCT01264770	AstraZeneca	Rheumatoid Arthritis	January 2011	Phase 2
NCT01387308	AstraZeneca	Healthy	August 2011	Phase 1
NCT02433236	Rigel Pharmaceuticals	IGA Nephropathy	September 2015	Phase 2
NCT04579393	National Heart, Lung, and Blood Institute (NHLBI)\|National Institutes of Health Clinical Center (CC)	Coronavirus Disease 2019	October 8, 2020	Phase 2
NCT00752999	Rigel Pharmaceuticals	Systemic Lupus Erythematosus	November 2008	Phase 2
NCT04629703	Rigel Pharmaceuticals	Covid19\|SARS (Severe Acute Respiratory Syndrome)\|SARS Pneumonia\|SARS-Associated Coronavirus as Cause of Disease Classified Elsewhere\|Pneumonia\|Pneumonia, Viral	February 22, 2021	Phase 3
NCT04924660	Sean Collins\|National Institutes of Health (NIH)\|National Heart, Lung, and Blood Institute (NHLBI)\|Vanderbilt University Medical Center	COVID-19\|SARS-CoV-2 Infection\|Coronavirus Infection	July 15, 2021	Phase 2\|Phase 3
NCT00923481	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	Head and Neck Neoplasms\|Pheochromocytoma\|Colorectal Neoplasms\|Carcinoma, Non-Small-Cell Lung\|Carcinoma, Renal Cell	April 2009	Phase 2
NCT00665925	Rigel Pharmaceuticals	Rheumatoid Arthritis	May 2008	Phase 2
NCT05040698	Holdsworth House Medical Practice\|Rigel Pharmaceuticals	Hidradenitis Suppurativa	October 1, 2021	Phase 2
NCT02611063	Stefanie Sarantopoulos, MD, PhD.\|Duke University	Hematological Malignancies	January 2016	Phase 1
NCT05613296	Gruppo Italiano Malattie EMatologiche dell´Adulto	ITP - Immune Thrombocytopenia\|Chronic ITP\|Refractory ITP	December 2022
NCT03764618	Rigel Pharmaceuticals	Warm Antibody Autoimmune Hemolytic Anemia	April 24, 2019	Phase 3
NCT01598571	AstraZeneca	Healthy	May 2012	Phase 1
NCT04581954	Imperial College London\|Imperial College Healthcare NHS Trust\|Rigel Pharmaceuticals\|Novartis	Coronavirus\|Covid19\|Pneumonia	October 2, 2020	Phase 1\|Phase 2
NCT02112838	Rigel Pharmaceuticals	IGA Nephropathy	October 2014	Phase 2
NCT01640054	AstraZeneca	Rheumatoid Arthritis	July 2012	Phase 2
NCT03363334	Rigel Pharmaceuticals	Immune Thrombocytopenic Purpura
NCT00798096	Rigel Pharmaceuticals	T Cell Lymphoma	March 2009	Phase 2
NCT05593770	NEAT ID Foundation	COVID-19\|SARS-CoV2 Infection\|Coronavirus Infection	October 27, 2022	Phase 2\|Phase 3
NCT00706342	Rigel Pharmaceuticals	Purpura, Thrombocytopenic, Idiopathic	January 2007	Phase 2

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 20.83 mg/mL ( 33.36 mM ; ultrasonic and warming and heat to 60°C)

H ₂ O : ≥ 1 mg/mL ( 1.60 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6015 mL	8.0074 mL	16.0149 mL
5 mM	0.3203 mL	1.6015 mL	3.2030 mL
10 mM	0.1601 mL	0.8007 mL	1.6015 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

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

Solubility: ≥ 2.5 mg/mL (4.00 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (4.00 mM); Clear solution

* All of the co-solvents are available by MCE.