JAK2-IN-14
JAK2-IN-14 is an orally active JAK2 inhibitor with an IC50 of 2 nM. JAK2-IN-14 demonstrates 89.5-, 80.5-, and 51-fold selectivity over JAK1, JAK3, and TYK2, respectively. JAK2-IN-14 inhibits STAT5 signaling pathway. JAK2-IN-14 causes tumor cell cycle arrest and apoptosis. JAK2-IN-14 can used for the study of myeloproliferative neoplasms (MPNs).
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- CAS. Nr.: 3087335-24-5
- Formel: C26H33N7O
- Molecular Weight:459.59
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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JAK2 2 nM (IC50) |
JAK1 179 nM (IC50) |
JAK3 161 nM (IC50) |
Tyk2 102 nM (IC50) |
STAT5 |
JAK2-IN-14 (Compound 15au) (0.01-5 μM, 24 h) significantly induces cell cycle arrest at the G2/M phase and cell apoptosis in a dose-dependent manner in BaF3-JAK2V617F and HEL cells[1].
JAK2-IN-14 (0.05-1 μM, 2 h) effectively inhibits the phosphorylation of JAK2 and its downstream signaling molecule STAT5 in BaF3-JAK2V617F and 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:BaF3-JAK2V617F and HEL cells
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Concentration:10, 50, 100, 500 and 1000 nM
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Incubation Time:24 h
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Result:Blocked the progression of tumor cells at the G2/M phase, leading to a decrease in the proportions of cells in the G1/G0 and G2 phases.
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Cell Line:BaF3-JAK2V617F and HEL cells
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Concentration:10, 50, 100, 500 and 1000 nM
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Incubation Time:2 h
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Result:Reduced p-JAK2 and p-STAT5 levels concentration-dependently.
| Species | Dose | Route | Cmax | Tmax | T1/2 | CL/F | AUC0-t |
|---|---|---|---|---|---|---|---|
| Mice[1] | 5 mg/kg | p.o. | 2101.0 ng/mL | 1.0 h | 7.8 h | 1.0 L/h/kg | 5069.7 ng·h/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BaF3-JAK2V617F allogeneic transplantation model established in BALB/c-nude mice[1]
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Dosage:7.5, 15 and 30 mg/kg
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Administration:Oral administration (p.o.), once daily for 13 days
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Result:Demonstrated significant therapeutic efficacy, reducing spleen weight by 24.1%, 26.4%, and 40.5% at doses of 7.5, 15, and 30 mg/kg, respectively
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Animal Model:HEL cells xenograft model was established in 6-week-old male BALB/c nude mice[1]
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Dosage:20 and 40 mg/kg
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Administration:Oral administration (p.o.), once daily for 28 days
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Result:Significantly inhibited subcutaneous tumor growth.
did not induce observable body weight loss during the experimental period.
Chemical Information
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CAS. Nr. 3087335-24-5
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Molecular Weight 459.59
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Formel C26H33N7O
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SMILES
CC1=CN=C(NC2=CC=C(N3CCN(CC4CC4)CC3)C5=C2)N=C1C6=CN(CCCCO5)N=C6
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
JAK2-IN-14 Related Classifications
HY-175684 Related Classifications
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