JAK2-IN-15
JAK2-IN-15 is an orally active, potent, selective JAK2 inhibitor (IC50 = 1.17 nM). JAK2-IN-15 can inhibit the AK2-STAT signaling pathway. JAK2-IN-15 significantly improves key pathological indicators such as hematocrit and splenomegaly in an Epoetin beta (HY-114134) (rhEPO)-induced mouse model. JAK2-IN-15 can be used for the study of Polycythemia Vera (PV).
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- CAS No.: 3094174-82-7
- Formule: C29H35N5O4
- Masse moléculaire:517.62
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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JAK2 1.17 nM (IC50) |
JAK2-IN-15 (Compound 2) exhibits potent JAK2 inhibition (IC50 = 1.17 nM)[1].
JAK2-IN-15 (72 h) effectively inhibits the proliferation of HEL (IC50 = 1.88 μM) and SET-2 (IC50 = 9.56 μM) cells carrying the JAK2V617F mutation[1].
JAK2-IN-15 (0.3-10 μM, 72 h) exhibits significant antiproliferative activities against HEL and SET-2 cells with JAK2V617F mutant by inhibiting the JAK2-STAT signaling pathway in a dose-dependent manner[1].
JAK2-IN-15 (100 μM) inhibits only 17 wild-type kinases, exhibiting strong selectivity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEL 92.1.7 cells, SET-2
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Concentration:0.3 μM, 1 μM, 3 μM, 10 μM
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Incubation Time:4 h
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Result:Effectively inhibited phosphorylation of JAK2 (Y1007/8 site), STAT3, STAT5, AKT and ERK.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A model of polycythemia and splenomegaly was created using female BALB/c mice (8-10 weeks old, weighing 17-20 g) by subcutaneous injection of 10 units of recombinant human erythropoietin (rhEPO) daily for 4 consecutive days[1].
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Dosage:25 mg/kg, 50 mg/kg, 75 mg/kg
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Administration:P.o., once daily for 4 days
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Result:Spleen weight decreased.
Dose-dependent inhibition of hematocrit.
Reduction of rhEPO-induced reticulocyte proliferation.
Inhibition of Ter119/CD71 erythroblast expansion in the spleen and bone marrow.
No significant effect on white blood cell count or body weight.
Chemical Information
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CAS No. 3094174-82-7
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Masse moléculaire 517.62
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Formule C29H35N5O4
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SMILES
CC1=C2N=C(NC3=CC=C(C(COC/C=C/COCC4=CC=CC(N2)=C4)=C3)OCCN5CCOCC5)N=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JAK2-IN-15 Related Classifications
HY-178936 Related Classifications
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