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Fedratinib (TG101348)
Catalog No.S2736 Synonyms: SAR302503
For research use only.
Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Fedratinib also inhibits FMS-like tyrosine kinase 3 (FLT3) and RET (c-RET) with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. Phase 2.
CAS No. 936091-26-8
Selleck's Fedratinib (TG101348) has been cited by 67 publications
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Biological Activity
| Description | Fedratinib (SAR302503, TG101348) is a selective inhibitor of JAK2 with IC50 of 3 nM in cell-free assays, 35- and 334-fold more selective for JAK2 versus JAK1 and JAK3. Fedratinib also inhibits FMS-like tyrosine kinase 3 (FLT3) and RET (c-RET) with IC50 of 15 nM and 48 nM, respectively. Fedratinib has potential antineoplastic activity. Fedratinib inhibits proliferation and induces apoptosis. Phase 2. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| In vitro |
TG-101348 also significantly inhibits JAK2 V617F, Flt3, and Ret with IC50 of 3 nM, 15 nM, and 48 nM, respectively. TG101348 has an IC50 ~300-fold higher for the closely related JAK3 and is a less potent inhibitor of the JAK1 and TYK2 family members. TG101348 inhibits proliferation of a human erythroblast leukemia (HEL) cell line that harbors the JAK2V617F mutation, as well as a murine pro-B cell line expressing human JAK2V617F (Ba/F3 JAK2V617F), with IC50 of 305 nM and 270 nM, respectively. TG-101348 also inhibits proliferation of parental Ba/F3 cells to a comparable level, with IC50 of ~420 nM. TG101348 treatment reduces STAT5 phosphorylation at concentrations that parallel the concentrations required to inhibit cell proliferation. TG101348 induces apoptosis in both HEL and Ba/F3 JAK2V617F cells in a dose-dependent manner. TG101348 does not show proapoptotic activity in control normal human dermal fibroblasts at concentrations up to 10 μM, and the antiproliferative IC50 against fibroblasts is >5 μM. [1] TG101348 treatment decreases GATA-1 expression, which is associated with erythroid-skewing of JAK2V617F+ progenitor differentiation, and inhibits STAT5 as well as GATA S310 phosphorylation. [2] TG101348 inhibits the proliferation of HMC-1.1 (KITV560G) cells, with somewhat lower potency than HMC-1.2 (KITD816V, KITV560G) cells, with IC50 of 740 nM and 407 nM, respectively. [3] |
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| Cell Data |
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| Assay |
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| In vivo |
TG101348 has potential for efficacious treatment of JAK2V617F-associated myeloproliferative diseases (MPD). In treated animals, there is a statistically significant reduction in hematocrit and leukocyte count, a dose-dependent reduction/elimination of extramedullary hematopoiesis, and, at least in some instances, evidence for attenuation of myelofibrosis, correlated with surrogate endpoints, including reduction/elimination of JAK2V617F disease burden, suppression of endogenous erythroid colony formation, and in vivo inhibition of JAK-STAT signal transduction. There are no apparent toxicities and no effect on T cell number. [1] Oral administration of TG101348 (120 mg/kg) significantly inhibits PV progenitor erythroid differentiation in vivo. [2] |
Protocol (from reference)
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Solubility (25°C)
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In vitro |
DMSO |
100 mg/mL
(190.59 mM) |
| Water |
Insoluble
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| Ethanol |
Insoluble
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Chemical Information
| Molecular Weight | 524.68 | ||
|---|---|---|---|
| Formula | C27H36N6O3S |
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| CAS No. | 936091-26-8 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | CC1=CN=C(N=C1NC2=CC(=CC=C2)S(=O)(=O)NC(C)(C)C)NC3=CC=C(C=C3)OCCN4CCCC4 | ||
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Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT04955938 | Recruiting | Drug: Ivosidenib|Drug: Enasidenib|Drug: Fedratinib | IDH Mutation|IDH1 Mutation|IDH2 Gene Mutation|Blood Cancer|Myeloproliferative Neoplasm | University of Chicago | October 29 2021 | Phase 1 |
| NCT05051553 | Not yet recruiting | Drug: Fedratinib | Healthy Volunteers | Bristol-Myers Squibb | September 21 2021 | Phase 1 |
| NCT04702464 | Completed | Drug: Fedratinib|Drug: Fluconazole | Healthy Volunteers | Celgene|Impact Biomedicines Inc. a wholly owned subsidiary of Celgene Corporation | January 12 2021 | Phase 1 |
| NCT03983161 | Recruiting | Drug: Fedratinib | Healthy Volunteers|Hepatic Impairment | Celgene|Impact Biomedicines Inc. a wholly owned subsidiary of Celgene Corporation | July 15 2019 | Phase 1 |
| NCT03983239 | Completed | Drug: Fedratinib|Drug: Rifampin|Drug: Efavirenz | Healthy Volunteers | Celgene|Impact Biomedicines Inc. a wholly owned subsidiary of Celgene Corporation | June 21 2019 | Phase 1 |
| NCT02596347 | Completed | Procedure: Blood draw|Procedure: bronchoscopy | Chronic Beryllium Disease (CBD)|Beryllium Sensitization (BeS) | National Jewish Health | April 2015 | -- |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
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