JAK3-IN-18
JAK3-IN-18 is an orally active JAK3 and TEC inhibitor, with IC50s of 0.5391 nM and 12.40 nM, respectively. JAK3-IN-18 demonstrates outstanding selectivity over AK1, AK2, and TYk2, with selectivity ratios exceeding 10,000-fold. JAK3-IN-18 demonstrates excellent therapeutic efficacy in the experimental autoimmune encephalomyelitis (EAE) mouse model. JAK3-IN-18 can be used for the study of multiple sclerosis.
For research use only. We do not sell to patients.
- CAS No.: 2914873-59-7
- Formula: C18H16FN5O
- Molecular Weight:337.35
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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
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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JAK3 0.5391 nM (IC50) |
JAK1 8575 nM (IC50) |
JAK2 7431 nM (IC50) |
JAK3-IN-18 (Compound 8a) (1-100000 nM, 80 min) inhibits p-stat5 with an IC50 value of 177.8 nM in the IL-15-stimulated human whole blood (HWB) assay[1]. JAK3-IN-18 (1 μM, 135 min) inhibits only 11 kinases with more than 60% inhibition apart from JAK3 and TEC against 310 kinases[1]. JAK3-IN-18 (10 μM, 0-60 min) exhibits acceptable GSH stability with favorable drug-like properties[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | Vss | CL | Cmax | AUC0-t | F |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.v. | 0.11 h | 2.8 L/kg | 543.6 mL/min/kg | 115.4 ng/mL | 30.9 ng·h/mL | / |
| Mice[1] | 2 mg/kg | p.o. | 0.45 h | / | / | 11.64 ng/mL | 6.92 ng·h/mL | 11.2 % |
| Mice[1] | 30 mg/kg | p.o. | 0.84 h | / | / | 3299 ng/mL | 1870 ng·h/mL | / |
| Rat[1] | 1 mg/kg | i.v. | 0.29 h | 1.45 L/kg | 116.8 mL/min/kg | 430.1 ng/mL | 142.7 ng·h/mL | / |
| Rat[1] | 2 mg/kg | p.o. | 0.97 h | / | / | 233.2 ng/mL | 218.6 ng·h/mL | 76.6 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Experimental autoimmune encephalomyelitis (EAE) mice (6-8 weeks)[1]
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Dosage:10, 100 mg/kg
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Administration:p.o. twice daily for 24 days
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Result:Decreased the clinical scores.
Showed no body weight loss.
Chemical Information
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CAS No. 2914873-59-7
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Molecular Weight 337.35
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Formula C18H16FN5O
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SMILES
O=C(C=C)N1CC2=C([C@@H](NC3=C4C=CNC4=NC=N3)C1)C=CC(F)=C2
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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)
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