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Chemical Structure| 901119-35-5 Chemical Structure| 901119-35-5

Structure of Fostamatinib
CAS No.: 901119-35-5

Chemical Structure| 901119-35-5

Fostamatinib

CAS No.: 901119-35-5

Fostamatinib (R788) is the oral prodrug of R406. R406 is a potent, orally active, ATP-competitive inhibitor of Syk/FLT3 with a Ki of 30 nM and an IC50 of 41 nM. R406 also inhibits Lyn (IC50 = 63 nM) and Lck (IC50 = 37 nM).

Synonyms: R788

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Cat. No.: A115345 Purity: 98%

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Product Details of Fostamatinib

CAS No. :901119-35-5
Formula : C23H26FN6O9P
M.W : 580.46
SMILES Code : O=P(O)(OCN1C2=NC(NC3=NC(NC4=CC(OC)=C(OC)C(OC)=C4)=NC=C3F)=CC=C2OC(C)(C)C1=O)O
Synonyms :
R788
MDL No. :MFCD16628163

Safety of Fostamatinib

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Fostamatinib

RTK

Isoform Comparison

Biological Activity

Target
  • Syk

    Syk, IC50:41 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Kidney tubular epithelial cell line (P cells) 200 nM 48 h To evaluate the effect of R406 (active metabolite of Fostamatinib) on MUC1 protein levels; results showed R406 significantly reduced MUC1 abundance on the plasma membrane and increased its intracellular distribution PMC7691435
MWCL.1 cells 1 μM 3 days To evaluate the effect of Fostamatinib on the viability of MWCL-1 cells, results showed that 1 μM Fostamatinib significantly reduced cell viability after 3 days, inducing cell cycle arrest and apoptosis. PMC4737551
BCWM.1 cells 1 μM 3 days To evaluate the effect of Fostamatinib on the viability of BCWM.1 cells, results showed that 1 μM Fostamatinib significantly reduced cell viability after 3 days, inducing cell cycle arrest and apoptosis. PMC4737551
EBV+ B-cell lymphoma PTLD lines 0-10 μM 96 h Induces apoptosis and cell cycle arrest while decreasing downstream PI3K/Akt signaling PMC4008139
Bone marrow monocytes 10 ng/ml GM-CSF and 10 ng/ml IL-3 5 days To evaluate the effect of Fostamatinib on GM-CSF/IL-3 stimulated bone marrow monocyte colony formation, results showed that Fostamatinib reduced GM-CSF/IL-3 stimulated bone marrow monocyte colony formation. PMC4759214
Ly6Chigh monocytes 30 ng/ml M-CSF 16 h To evaluate the effect of Fostamatinib on monocyte to macrophage differentiation, results showed that Fostamatinib blocked M-CSF stimulated monocyte to macrophage differentiation. PMC4759214

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6J mice Ischemia/reperfusion (I/R)-induced acute lung injury model Oral 3 g/kg Once daily for 10 days To evaluate the effect of R788 on MUC1 levels in vivo; results showed R788 significantly reduced MUC1 abundance in lung epithelial cells PMC7691435
Mice Silicosis mouse model Oral gavage 80 mg/kg Once daily for two weeks To investigate the effect of Fostamatinib on p-SYK levels and pulmonary fibrosis in a silicosis mouse model. Results showed that Fostamatinib significantly inhibited p-SYK levels and effectively alleviated silica-induced alveolitis and pulmonary fibrosis. PMC9098425
Non-obese diabetic mice MWCL-1 cell xenograft model Intraperitoneal injection 80 mg/kg Three times a week for 45 days To evaluate the anti-tumor activity of Fostamatinib in the MWCL-1 cell xenograft model, results showed that Fostamatinib significantly slowed tumor growth. PMC4737551
Mice Apoe-/- mice on high cholesterol diet Oral 0.3% (w/w) Continued for 8 weeks To evaluate the effect of Fostamatinib on high cholesterol diet-induced atherosclerosis, results showed that Fostamatinib reduced the formation of atherosclerotic plaques and decreased the number of Ly6Chigh monocytes and macrophages. PMC4759214

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT05613296 ITP - Immune Thrombocytopenia|... More >>Chronic ITP|Refractory ITP Less << UNKNOWN 2025-12-23 -
NCT05904093 Sickle Cell Disease|Hb-SS Dise... More >>ase|Hemoglobin S|Disease Sickle Cell Anemia|Sickle Cell Disorders|Hemoglobin Beta Thalassemia Disease Less << PHASE1 RECRUITING 2026-05-14 National Institutes of Health ... More >>Clinical Center, Bethesda, Maryland, 20892, United States Less <<
NCT01499303 Diffuse Large B-Cell Lymphoma PHASE2 COMPLETED 2025-10-13 Research Site, Huntsville, Ala... More >>bama, United States|Research Site, Denver, Colorado, United States|Research Site, New Haven, Connecticut, United States|Research Site, Sarasota, Florida, United States|Research Site, Atlanta, Georgia, United States|Research Site, Iowa City, Iowa, United States|Research Site, Baltimore, Maryland, United States|Research Site, Boston, Massachusetts, United States|Research Site, Rochester, Minnesota, United States|Research Site, St. Louis, Missouri, United States|Research Site, Hackensack, New Jersey, United States|Research Site, New York, New York, United States|Research Site, Rochester, New York, United States|Research Site, Columbus, Ohio, United States|Research Site, Nashville, Tennessee, United States|Research Site, Houston, Texas, United States|Research Site, San Antonio, Texas, United States|Research Site, Charlottesville, Virginia, United States|Research Site, Seattle, Washington, United States|Research Site, London, United Kingdom|Research Site, Southampton, United Kingdom Less <<
NCT05040698 Hidradenitis Suppurativa PHASE2 COMPLETED 2023-01-27 Holdsworth House Medical Pract... More >>ice, Sydney, New South Wales, 2010, Australia Less <<
NCT05030675 Refractory Chronic Myelomonocy... More >>tic Leukemia|Refractory Myelodysplastic Syndrome Less << PHASE1 COMPLETED 2024-08-08 M D Anderson Cancer Center, Ho... More >>uston, Texas, 77030, United States Less <<
NCT03991780 Renal Transplant Rejection PHASE1|PHASE2 ACTIVE_NOT_RECRUITING 2025-10-15 Imperial College NHS Healthcar... More >>e Trust, London, W12 0HS, United Kingdom Less <<
NCT04904276 ITP|Immune Thrombocytopenia TERMINATED 2022-11-17 Advanced Research, Tamarac, Fl... More >>orida, 33321, United States|Simmons Cancer Institute at Southern Illinois University, Springfield, Illinois, 62702, United States|University of Kansas Medical Center, Kansas City, Kansas, 66160, United States|Saint Agnes Hospital, Baltimore, Maryland, 21229, United States|The Center for Cancer and Blood Disorders, Bethesda, Maryland, 20817, United States|Maryland Oncology Hematology, P.A, Clinton, Maryland, 20735, United States|Maryland Oncology Hematology, P.A, Columbia, Maryland, 21044, United States|Maryland Oncology Hematology, P.A, Rockville, Maryland, 20850, United States|Maryland Oncology Hematology, P.A, Silver Spring, Maryland, 20904, United States|Boston Medical Center, Boston, Massachusetts, 02118, United States|Washington University, Saint Louis, Missouri, 63130, United States|Regional Cancer Care Associates, LLC, Little Silver, New Jersey, 07739, United States|New York Medical College Westchester Medical Center, Valhalla, New York, 10532, United States|New York Medical College, Valhalla, New York, 10595, United States Less <<
NCT06071520 Primary Immune Thrombocytopeni... More >>a Less << COMPLETED 2023-06-30 Hospital Puerta del Mar, Cadiz... More >>, Cádiz, 11009, Spain|Hospital Universitario de Jerez de la Frontera, Jerez De La Frontera, Cádiz, 11407, Spain|Hospital de Puerto Real, Puerto Real, Cádiz, 11510, Spain|Hospital de Riotinto, Minas de Riotinto, Huelva, 21660, Spain|Hospital de la Serranía de Ronda, Ronda, Málaga, 29400, Spain|Hospital de la Merced de Osuna, Osuna, Sevilla, 41640, Spain|Hospital Universitario Virgen de las Nieves, Granada, 18014, Spain|Hospital Universitario San Cecilio, Granada, 18016, Spain|Hospital Universitario Juan Ramón Jiménez, Huelva, 21005, Spain|Hospital Universitario de Jaén, Jaén, 23007, Spain|Hospital Regional Universitario de Málaga, Málaga, 29010, Spain|Hospital Virgen de la Victoria, Málaga, 29010, Spain|Hospital Universitario Virgen Macarena, Sevilla, 41009, Spain|Hospital Universitario Virgen del Rocío, Sevilla, 41013, Spain Less <<
NCT01222455 Hepatic Impairment|Healthy Vol... More >>unteers|Pharmacokinetics|Amount of R406 in Blood Less << PHASE1 COMPLETED 2025-06-11 Research Site, Orlando, Florid... More >>a, United States Less <<
NCT01640054 Rheumatoid Arthritis PHASE2 TERMINATED 2025-07-13 Research Site, Hongkong, Shati... More >>n, Hong Kong|Research Site, Hong Kong, Hong Kong|Research Site, Fukuoka-shi, Fukuoka, Japan|Research Site, Kitakyushu-shi, Fukuoka, Japan|Research Site, Sapporo-shi, Hokkaido, Japan|Research Site, Kato-shi, Hyogo, Japan|Research Site, Sendai-shi, Miyagi, Japan|Research Site, Nagasaki-shi, Nagasaki, Japan|Research Site, Omura-shi, Nagasaki, Japan|Research Site, Sasebo-shi, Nagasaki, Japan|Research Site, Okayama-shi, Okayama, Japan|Research Site, Tomigusuku-shi, Okinawa, Japan|Research Site, Hamamatsu-shi, Shizuoka, Japan|Research Site, Itabashi-ku, Tokyo, Japan|Research Site, Shinjuku-ku, Tokyo, Japan|Research Site, Anyang-si, Gyeonggi-do, Korea, Republic of|Research Site, Gwangju, Korea, Republic of|Research Site, Incheon, Korea, Republic of|Research Site, Seoul, Korea, Republic of|Research Site, Kaohsiung, Taiwan|Research Site, Taichung, Taiwan|Research Site, Taipei, Taiwan|Research Site, Bangkok, Thailand|Research Site, Singapore, Thailand|Research Site, Hanoi, Vietnam|Research Site, Ho Chi Minh, Vietnam Less <<

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