JAK2-IN-24
JAK2-IN-24 is an orally active JAK2 inhibitor with an IC50 < 0.003 μM. JAK2-IN-24 blocks the JAK/STAT signaling pathway. JAK2-IN-24 inhibits JAK1 and JAK3 tyrosine kinases. JAK2-IN-24 inhibits pSTAT5 levels in mouse spleen in the TEL-JAK2 implantation model. JAK2-IN-24 inhibits tumor growth. JAK2-IN-24 can be used in research on myeloproliferative neoplasms.
For research use only. We do not sell to patients.
- CAS No.: 1220516-48-2
- Formula: C16H16FN9
- Molecular Weight:353.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
JAK2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BaF3 | IC50 |
0.24 μM
|
Inhibition of pSTAT5 in BaF3 TEL-TYK2 cells by Western blot.
Inhibition of pSTAT5 in BaF3 TEL-TYK2 cells by Western blot.
|
24359159 |
| SET-2 | IC50 |
0.030 μM
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Inhibition of pSTAT5 in SET-2 cells at 1 h by Western blot.
Inhibition of pSTAT5 in SET-2 cells at 1 h by Western blot.
|
24359159 |
| SET-2 | IC50 |
0.054 μM
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Inhibition of pSTAT5 in SET-2 cells at 24 h by Western blot.
Inhibition of pSTAT5 in SET-2 cells at 24 h by Western blot.
|
24359159 |
In Vitro
JAK2-IN-24 (Compound 19a) inhibits the proliferation of BaF3 TEL-Jak2 cells (GI50 0.012 μM) as well as the V617F cell lines SET-2 (0.014 μM) and UKE-1 (0.055 μM)[1].
JAK2-IN-24 (0.001-3 μM; 1-24 h (UKE-1 and SET-2)) inhibits pSTAT5 in JAK2-dependent and V617F cell lines[1].
JAK2-IN-24 is a potent biochemical Jak2 inhibitor (IC50 <0.003 μM) with selectivity over Jak3 (IC50 0.22 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BaF3 TEL-JAK2, BaF3 TEL-TYK2, UKE-1, and SET-2 cells
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Concentration:0.001, 0.003, 0.010, 0.030, 0.100, 0.300, 1, and 3 μM
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Incubation Time:1 h and 24 h (UKE-1 and SET-2)
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Result:Inhibited pSTAT5 in BaF3 TEL-JAK2, BaF3 TEL-TYK2 with IC50 0.012, 0.24 μM.
Inhibited pSTAT5 in UKE-1 with IC50 0.002 μM at 1 h and 0.005 μM at 24 h.
Inhibited pSTAT5 in SET-2 with IC50 0.030 μM at 1 h and 0.054 μM at 24 h.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID (female)[1]
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Dosage:3 or 10 mg/kg
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Administration:p.o.; BID; 14 days
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Result:We observed a significant dose-dependent tumor growth inhibition with 19a-treated animals.
At the end of the dosing phase, maximum tumor growth inhibition was 77% with 10 mg/kg twice daily and 50% with 3 mg/kg twice daily.
No significant body weight loss was observed; maximum weight loss/gain on day 31 was 3.1% for 10 mg/kg and 7.2% for 3 mg/kg.
Chemical Information
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CAS No. 1220516-48-2
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Molecular Weight 353.36
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Formula C16H16FN9
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SMILES
CN1C=C(NC2=C3C(NC=C3)=NC(N[C@H](C4=NC=C(F)C=N4)C)=N2)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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JAK2-IN-24 Related Classifications
HY-12615 Related Classifications
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