Fedratinib (SAR302503)
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
500mg | $440 | In Stock |
1g | $700 | In Stock |
5g | $1770 | In Stock |
Cat #: V0317 CAS #: 936091-26-8 Purity ≥ 98%
Description: Fedratinib (formerly SAR302503 or TG101348; brand name Inrebic) is a novel, potent, selective, orally bioavailable, small-molecule and ATP-competitive inhibitor of janus kinase 2 (JAK2) with an IC50 of 3 nM.
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Molecular Weight (MW) | 524.68 |
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Molecular Formula | C27H36N6O3S |
CAS No. | 936091-26-8 |
SMILES Code | O=S(C1=CC=CC(NC2=NC(NC3=CC=C(OCCN4CCCC4)C=C3)=NC=C2C)=C1)(NC(C)(C)C)=O |
Synonyms | SAR302503; SAR-302503; SAR 302503; Fedratinib; TG101348; TG 101348; TG-101348; |
Protocol | In Vitro | Fedratinib (TG101348) (0.1 μM, 0.3 μM, 1 μM, 3 μM, and 10 μM) induces apoptosis in both HEL and Ba/F3 JAK2V617F cells in a dose-dependent manner. Exposure of these cells to Fedratinib (TG101348) (0.1 μM, 0.3 μM, 1 μM, 3 μM, and 10 μM) reduces STAT5 phosphorylation at concentrations that parallel the concentrations required to inhibit cell proliferation. Fedratinib (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 an IC50 value of approximately 300 nM for either line. Proliferation of parental Ba/F3 cells was inhibited to a comparable level, with an IC50 value of ∼420 nM. |
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In Vivo | Fedratinib (TG101348; 60-120 mg/kg; oral gavage; twice daily; for 42 days; C57Bl/6 mice) trewatment shows a dose-dependent reduction in polycythemia and a marked dose-dependent reduction in splenomegaly of treated animals. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.9059 mL | 9.5296 mL | 19.0592 mL | 38.1185 mL |
5mM | 0.3812 mL | 1.9059 mL | 3.8118 mL | 7.6237 mL |
10mM | 0.1906 mL | 0.9530 mL | 1.9059 mL | 3.8118 mL |
20mM | 0.0953 mL | 0.4765 mL | 0.9530 mL | 1.9059 mL |
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Step Two: Enter the in vivo formulation
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Method for preparing in vivo formulation:
Take
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PEG300, mix and clarify, next add
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Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
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