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).
For research use only. We do not sell to patients.
- CAS No.: 3094174-82-7
- Formula: C29H35N5O4
- Molecular Weight:517.62
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
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JAK2 1.17 nM (IC50) |
In Vitro
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. Further protocols information, click here.
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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.
In Vivo
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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Molecular Weight 517.62
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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How to Choose the Right Model Animal
Choosing the right model animal is a validity-driven decision in which the species, strain, sex, age, genetic background, disease-induction method, outcome measures, and welfare burden must match the scientific question rather than laboratory tradition or convenience. A model should be selected by judging face validity, construct validity, and predictive validity: whether it resembles the human phenotype, whether it reproduces relevant mechanisms, and whether results are likely to predict human biology or treatment response. Animal studies often fail to translate because of species differences, weak disease resemblance, poor experimental design, inadequate reporting, publication bias, and underuse of randomization, blinding, and sample-size justification. Unresolved questions include how to rank competing models objectively, how much human-disease complexity must be reproduced for a given objective, and when non-animal systems such as organoids, ex vivo tissue, or computational models
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)