JAK2-IN-13
JAK2-IN-13 is a potent and orally active JAK2 inhibitor with an IC50 of 54.7 nM. JAK2-IN-13 downregulates the expressions of p-STAT3 and p-STAT5. JAK2-IN-13 exhibits good bioavailability and potent inhibition of rhEPO-induced extramedullary erythropoiesis and polycythemia vera. JAK2-IN-13 can be used for the study of myeloproliferative neoplasms.
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- Fòrmula: C25H28ClN5O2
- Peso molecular:465.98
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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JAK2 54.7 nM (IC50) |
STAT3 |
STAT5 |
JAK2-IN-13 (Compound 11) (0.011-25 μM, 72 h) shows potent inhibitory activity against HEL and SET-2 cells, with IC50 values of 0.57 μM and 1.07 μM, respectively[1].
JAK2-IN-13 (0-10 μM, 3 h) significantly inhibits downstream signal pathways of JAK2 and downregulates p-STAT3 and p-STAT5 expression in HEL cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEL cells
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Concentration:0, 0.3, 1, 5, 10 μM
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Incubation Time:3 h
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Result:Dose-dependent downregulated p-STAT3 and p-STAT5 expressions.
Significantly inhibited the phosphorylation of STAT3 and STAT5 at 10 μM for 4 h.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:rhEPO-induced polycythemia model established in female BALB/c mice (8−10 weeks, 17−20 g)[1]
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Dosage:50, 75 and 100 mg/kg
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Administration:Oral administration (p.o.), once daily for 4 days
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Result:Suppressed the increase in reticulocyte counts and hematocrit expansion induced by rhEPO and alleviated splenomegaly.
Inhibited the expansion of Ter119/CD71 erythroblasts in both the spleen and bone marrow.
Had no significant impact on white blood cell counts and body weight.
Chemical Information
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Peso molecular 465.98
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Fòrmula C25H28ClN5O2
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SMILES
CC1=CN=C(NC(C=C2)=CC3=C2OCCN4CCCC4)N=C1NC5=CC(Cl)=CC(COC3)=C5
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JAK2-IN-13 Related Classifications
HY-174988 Related Classifications
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