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Chemical Structure| 936091-26-8 Chemical Structure| 936091-26-8
Chemical Structure| 936091-26-8

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CAS No.: 936091-26-8

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Fedratinib (TG-101348) is a potent, selective, ATP-competitive, and orally active JAK2 inhibitor with IC50 values of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35-fold and 334-fold selectivity over JAK1 and JAK3, respectively. It induces cancer cell apoptosis and has potential for myeloproliferative disorders research.

Synonyms: SAR 302503; TG 101348; TG-101348

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Product Details of [ Fedratinib ]

CAS No. :936091-26-8
Formula : C27H36N6O3S
M.W : 524.68
SMILES Code : O=S(C1=CC=CC(NC2=NC(NC3=CC=C(C=C3)OCCN4CCCC4)=NC=C2C)=C1)(NC(C)(C)C)=O
Synonyms :
SAR 302503; TG 101348; TG-101348
MDL No. :MFCD12922515
InChI Key :JOOXLOJCABQBSG-UHFFFAOYSA-N
Pubchem ID :16722836

Safety of [ Fedratinib ]

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of [ Fedratinib ]

epigenetics
RTK
JAK-STAT

Isoform Comparison

Biological Activity

Target

  • JAK2

    JAK2 (V617F), IC50:3 nM

    JAK2, IC50:3 nM

In Vitro:

Cell Line
Concentration Treated Time Description Reference
RAW264.7 cells 10 μM 4 h To evaluate the effect of Fedratinib on JAK/STAT3/FOXO3 signaling, results showed that Fedratinib inhibited JAK2 and STAT3 phosphorylation and promoted M2 macrophage polarization. PMC11025230
Human CD14+ monocytes 500 nM 24 h To investigate the effects of JAK2 inhibition on monocyte response, the production of TNFα and IL-10 was measured. JAK2 inhibition resulted in decreased production of TNFα and increased IL-10 production after a second LPS stimulus. PMC8635809
HMO6 cells 20 μM 24 h To investigate the inhibitory effect of Fedratinib on the JAK2/STAT3 signaling pathway, results showed that Fedratinib significantly downregulated the activation level of JAK2/STAT3 PMC8864012
CHME5 cells 20 μM 24 h To investigate the inhibitory effect of Fedratinib on the JAK2/STAT3 signaling pathway, results showed that Fedratinib significantly downregulated the activation level of JAK2/STAT3 PMC8864012
Human T cells 1 μM 5 days Inhibition of JAK2 reduced CD83 expression on allo-stimulated CD4+ T cells PMC10011883
CD14+ monocytes 500 nM 24 h JAK2 inhibition partially prevents the activation of LPS-upregulated genes and the expression of tolerance-related genes. PMC8635809
LX-2 cells 50 ng/mL 24 h To investigate the effect of FGF19 on the polarization of LX-2 cells toward the iCAF phenotype, results showed that FGF19 induced the iCAF phenotype via the FGFR4-JAK2-STAT3 signaling pathway. PMC10460854

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
Mice C3H/HeJ AA mouse model Systemic administration 50 mg/kg 12 weeks Fedratinib failed to restore hair regrowth in C3H/HeJ AA mice, indicating that JAK2-selective inhibitors are ineffective in treating AA. PMC8119218
Nude mice Brain metastasis model Oral 100 mg/kg Once every two days for 4 weeks To investigate the inhibitory effect of Fedratinib on brain metastasis of A549-F3 cells, results showed that Fedratinib significantly reduced the incidence of brain metastasis and the luminescence intensity of metastatic foci PMC8864012
Mice Experimental Autoimmune Encephalomyelitis (EAE) model Intraperitoneal injection 90 mg/kg Injected on days 7, 10, 12, 14, 17, 19, 21, 24, 26 Fedratinib significantly reduced EAE disease severity and decreased the number of CD4+ T cells producing IL-17A and GM-CSF in the CNS. PMC8431781
BALB/c nude mice colorectal cancer liver metastasis model oral 10 mg/kg daily until the termination of experiment To evaluate the inhibitory effect of Fisogatinib on FGF19-induced liver metastasis, results showed that Fisogatinib significantly suppressed FGF19-induced liver metastasis and extended the survival of mice. PMC10460854

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01437787 Hematopoietic Neoplasm Phase 3 Completed - -
NCT01585623 Solid Tumor Phase 1 Completed - United States, Georgia ... More >> Investigational Site Number 840004 Augusta, Georgia, United States, 30912 United States, Michigan Investigational Site Number 840001 Detroit, Michigan, United States, 48201 United States, Pennsylvania Investigational Site Number 840002 Philadelphia, Pennsylvania, United States, 19111 Less <<
NCT01836705 Neoplasm Malignant Phase 1 Completed - United States, California ... More >> Investigational Site Number 840003 Los Angeles, California, United States, 90048 United States, Georgia Investigational Site Number 840007 Augusta, Georgia, United States, 30912 United States, Michigan Investigational Site Number 840002 Detroit, Michigan, United States, 48201 United States, Missouri Investigational Site Number 840001 St Louis, Missouri, United States, 63110 United States, Ohio Investigational Site Number 840004 Cincinnati, Ohio, United States, 45267-0542 United States, Pennsylvania Investigational Site Number 840005 Philadelphia, Pennsylvania, United States, 19111 United States, Texas Investigational Site Number 840006 San Antonio, Texas, United States, 78229 Investigational Site Number 840008 San Antonio, Texas, United States, 78229 Belgium Investigational Site Number 056001 Bruxelles, Belgium, 1200 Investigational Site Number 056002 Gent, Belgium, 9000 Less <<
NCT01420770 Hematopoietic Neoplasm Phase 2 Completed - United States, California ... More >> Investigational Site Number 840001 San Francisco, California, United States, 94143 United States, Michigan Investigational Site Number 840003 Ann Arbor, Michigan, United States, 48109-0759 United States, Minnesota Investigational Site Number 840006 Rochester, Minnesota, United States, 55905 United States, Ohio Investigational Site Number 840007 Canton, Ohio, United States, 44718 Less <<
NCT01692366 Myelofibrosis Phase 2 Completed - Japan ... More >> Investigational Site Number 392010 Akita-Shi, Japan Investigational Site Number 392002 Bunkyo-Ku, Japan Investigational Site Number 392006 Bunkyo-Ku, Japan Investigational Site Number 392004 Sendai-Shi, Japan Investigational Site Number 392008 Shinjuku-Ku, Japan Investigational Site Number 392009 Shinjuku-Ku, Japan Investigational Site Number 392003 Suita-Shi, Japan Less <<
NCT01420783 Hematopoietic Neoplasm Phase 2 Completed - -
NCT03723148 - - - United States, New Jersey ... More >> Celgene Summit, New Jersey, United States, 07901 Less <<
NCT00724334 Myelofibrosis Phase 1 Phase 2 Completed - United States, California ... More >> Investigational Site Number 840103 La Jolla, California, United States, 92093 Investigational Site Number 840102 Stanford, California, United States, 94305 United States, Massachusetts Investigational Site Number 840105 Boston, Massachusetts, United States, 02115 United States, Michigan Investigational Site Number 840106 Ann Arbor, Michigan, United States, 48109-0759 United States, Minnesota Investigational Site Number 840104 Rochester, Minnesota, United States, 55905 United States, Texas Investigational Site Number 840101 Houston, Texas, United States, 77030 Less <<
NCT02596347 - Unknown - United States, Colorado ... More >> National Jewish Health Recruiting Denver, Colorado, United States, 80206 Contact: Gina M Atnes, BA ?? 303-398-1679 ?? mondellog@njhealth.org ?? Principal Investigator: Li Li, MD Less <<
NCT01763190 Renal Impairment Phase 1 Completed - United States, Florida ... More >> Investigational Site Number 840002 Orlando, Florida, United States, 32809 United States, Minnesota Investigational Site Number 840003 St. Paul, Minnesota, United States, 55144 United States, Tennessee Investigational Site Number 840001 Knoxville, Tennessee, United States, 37920 Less <<
NCT01762462 Hepatic Impairment Phase 1 Completed - United States, Florida ... More >> Investigational Site Number 840003 Miami, Florida, United States, 33014 Investigational Site Number 840002 Orlando, Florida, United States, 32809 United States, Tennessee Investigational Site Number 840001 Knoxville, Tennessee, United States, 37920 Less <<
NCT01523171 Hematopoietic Neoplasm Phase 2 Completed - -
NCT00631462 Myelofibrosis Phase 1 Completed - United States, California ... More >> UCSD Moores Cancer Center San Diego, California, United States, 92093 Stanford Comprehensive Cancer Center Stanford, California, United States, 94305 United States, Massachusetts Dana Farber Cancer Institute Boston, Massachusetts, United States, 02115 United States, Michigan University of Michigan Comprehensive Cancer Center Ann Arbor, Michigan, United States, 48109 United States, Minnesota Mayo Clinic, Rochester Rochester, Minnesota, United States, 55905 United States, Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 Less <<
NCT03755518 Primary Myelofibrosis ... More >> Thrombocytosis Less << Phase 3 Not yet recruiting October 31, 2022 -
NCT03983161 Healthy Volunteers|Hepatic Imp... More >>airment Less << PHASE1 COMPLETED 2023-01-05 University Of Miami Miller Sch... More >>ool Of Medicine, Miami, Florida, 33136, United States|Orlando Clinical Research Center OCRC, Orlando, Florida, 32809, United States|Volunteer Research Group and New Orleans Center for Clinical Research - Knoxville, Knoxville, Tennessee, 37920, United States Less <<
NCT05883904 Primary Myelofibrosis|Post-pol... More >>ycythemia Vera Myelofibrosis|Post-essential Thrombocythemia Myelofibrosis Less << RECRUITING 2025-01-26 Ematologia FONDAZIONE IRCCS CA... More >>' GRANDA, OSPEDALE MAGGIORE POLICLINICO, Milano, Italy Less <<
NCT04446650 Primary Myelofibrosis PHASE1|PHASE2 ACTIVE_NOT_RECRUITING 2025-10-31 Local Institution - 021, Suwa,... More >> Nagano, 392-8510, Japan|Local Institution - 001, Bunkyo-ku, Tokyo, 113-8431, Japan|Local Institution - 002, Aomori, 030-8553, Japan|Local Institution - 004, Bunkyo-ku, 113-8677, Japan|Local Institution - 006, Chuo, 409-3898, Japan|Local Institution - 015, Fukuoka, 812-8582, Japan|Local Institution - 018, Hitachi, Ibaraki, 317-0077, Japan|Local Institution - 005, Isehara City, Kanagawa, 259-1193, Japan|Local Institution - 010, Kamogawa, 296-8602, Japan|Local Institution - 017, Kitakyushu, 806-8501, Japan|Local Institution - 020, Kumamoto, 8628655, Japan|Local Institution - 013, Maebashi, 371-8511, Japan|Local Institution - 012, Miyazaki, 889-1692, Japan|Local Institution - 009, Nagasaki-shi, 8528511, Japan|Local Institution - 011, Osaka-Sayama, 589-8511, Japan|Local Institution - 016, Osaka, 545-8586, Japan|Local Institution - 014, Sapporo, 003-0006, Japan|Local Institution - 007, Shinagawa-ku, Tokyo, 141-8625, Japan|Local Institution - 008, Shinjuku City, 162-8666, Japan|Local Institution - 003, Shinjyuku-ku, 160-0023, Japan|Local Institution - 019, Takamatsu, 760-0017, Japan Less <<
NCT06073847 Primary Myelofibrosis|Post-pol... More >>ycythemia Vera Myelofibrosis|Post-essential Thrombocythemia Myelofibrosis Less << RECRUITING 2027-12-20 Bristol-Myers Squibb YH, Seoul... More >>, 06178, Korea, Republic of|Local Institution - 0001, Seoul, 06234, Korea, Republic of|Novotech Laboratory Korea Co., Ltd., Seoul, 06234, Korea, Republic of Less <<
NCT05051553 Healthy Volunteers PHASE1 COMPLETED 2022-04-08 Syneos Health Clinical Researc... More >>h Services, Llc, Miami, Florida, 33136, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.91mL

0.38mL

0.19mL

9.53mL

1.91mL

0.95mL

19.06mL

3.81mL

1.91mL

References

 

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