Fedratinib (TG101348) dihydrochloride hydrate
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
Size | Price | Stock |
---|---|---|
500mg | $750 | To Be Confirmed |
1g | $1250 | To Be Confirmed |
5g | $3160 | To Be Confirmed |
Cat #: V16212 CAS #: 1374744-69-0 Purity ≥ 99%
Description: Fedratinib dihydrochloride hydrate (SAR302503 or TG101348) is a novel, potent, selective, orally bioavailable, small-molecule and ATP-competitive inhibitor of janus kinase 2 (JAK2) with the inhibition constant IC50 of 3 nM.
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Molecular Weight (MW) | 615.62 |
---|---|
Molecular Formula | C27H40Cl2N6O4S |
CAS No. | 1374744-69-0 |
SMILES Code | O=S(C1=CC=CC(NC2=NC(NC3=CC=C(OCCN4CCCC4)C=C3)=NC=C2C)=C1)(NC(C)(C)C)=O.[H]Cl.[H]Cl.[H]O[H] |
Synonyms | TG101348; TG-101348; TG 101348; Fedratinib dihydrochloride hydrate; SAR302503; SAR-302503; SAR 302503; |
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 | 1.6244 mL | 8.1219 mL | 16.2438 mL | 32.4876 mL |
5mM | 0.3249 mL | 1.6244 mL | 3.2488 mL | 6.4975 mL |
10mM | 0.1624 mL | 0.8122 mL | 1.6244 mL | 3.2488 mL |
20mM | 0.0812 mL | 0.4061 mL | 0.8122 mL | 1.6244 mL |
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Method for preparing in vivo formulation:
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Tween 80,mix and clarify, next add
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