JAK2-IN-9
JAK2-IN-9 is an orally active selective JAK2 inhibitor with a human IC50 of 5 nM. JAK2-IN-9 inhibits JAK2 kinase activity, blocks JAK2 phosphorylation, and suppresses the activation of the downstream JAK2-STAT signaling pathway. JAK2-IN-9 inhibits the phosphorylation of STAT3, STAT5 and AKT in cancer cells. JAK2-IN-9 induces cancer cell apoptosis (apoptosis) and cell cycle arrest. JAK2-IN-9 can be used for the research of myeloproliferative neoplasms.
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- CAS No.: 2568842-26-0
- Formule: C20H24N6O2S
- Masse moléculaire:412.51
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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
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Activité biologique
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JAK2 5 nM (IC50) |
p-STAT3 |
STAT5 |
Akt |
JAK2-IN-9 (compound A8) potently inhibits recombinant JAK2 with an IC50 of 5 nM, and exhibits high selectivity for JAK1, JAK3, TYK2 and FLT3[1].
JAK2-IN-9 exhibits high selectivity at the kinome-wide level, with a selectivity of 50-fold or higher against off-target kinases including LCK, LYN and FAK when tested at 1 μM[1].
JAK2-IN-9 inhibits the proliferation of SET-2 cells with an IC50 of 44.3 nM; it also inhibits the proliferation of Ba/F3 JAK2V617F cells with an IC50 of 25.3 nM[1].
JAK2-IN-9 (10-1000 nM) dose-dependently inhibits the phosphorylation of JAK2 and the phosphorylation of its downstream signaling proteins STAT3, STAT5 and AKT in Ba/F3 JAK2V617F cells[1].
JAK2-IN-9 (0.5-16 nM; 24 h) induces concentration-dependent G0/G1 cell cycle arrest in Ba/F3 JAK2V617F cells[1].
JAK2-IN-9 (20-320 nM; 2 h) induces dose-dependent apoptosis in Ba/F3 JAK2V617F cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3 JAK2V617F cells
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Concentration:0.5, 2, 4, 8, 16 nM
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Incubation Time:24 h
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Result:Induced a concentration-dependent G0/G1 phase cell cycle arrest.
Induced statistically significant G0/G1 phase cell cycle arrest at 16 nM.
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Cell Line:Ba/F3 JAK2V617F cells
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Concentration:20, 40, 80, 160, 320 nM
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Incubation Time:2 h
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Result:Induced significant apoptosis in a dose-dependent manner.
Induced statistically significant apoptosis at concentrations ≥ 40 nM.
Induced highly significant apoptosis at concentrations ≥ 80 nM.
| Species | Dose | Route | Cmax | Tmax | T1/2 | CLz | AUC0-t | Bioavailability |
|---|---|---|---|---|---|---|---|---|
| Rat[1] | 5 mg/kg | p.o. | 121.4 ng/mL | 1.4 h | 5.2 h | 17.7 L/h/kg | 3517.9 ng·h/mL | 41.1 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2568842-26-0
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Masse moléculaire 412.51
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Formule C20H24N6O2S
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SMILES
C=CS(=O)(NCC1=CC=C(NC2=NC=C(C)C(C3=CN(C(C)C)N=C3)=N2)C=C1)=O
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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-9 Related Classifications
HY-155746 Related Classifications
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