JAK3-IN-1
Modify Date: 2024-01-14 18:01:05
JAK3-IN-1 structure
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Common Name | JAK3-IN-1 | ||
|---|---|---|---|---|
| CAS Number | 1805787-93-2 | Molecular Weight | 508.015 | |
| Density | 1.3±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C26H30ClN7O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of JAK3-IN-1JAK3-IN-1 is a potent JAK3 inhibitor with IC50 of 4.8 nM, also inhibits JAK1 (IC50 = 896 nM) and JAK2 (IC50 = 1050 nM).IC50 value: 4.8 nM [1]Target: JAK3in vitro: JAK3-IN-1 provides a set of useful tools to pharmacologically interrogate JAK3-dependent biology. JAK3-IN-1 completely inhibits IL-4 induced p-STAT6 at a concentration of 500 nM and only partially inhibits IFNβ-induced p-STAT1 at a concentration of 5.0 μM. In a similar way, JAK3-IN-1 exhibits consistent potency and selectivity for JAK3 in leukemia cancer cell lines: TALL-1 and OCL-AML5. [1]in vivo: JAK3-IN-1 demonstrates reasonable pharmacokinetic properties, with moderate T1/2 of 1.4 h, area under the curve (AUC) value of 795 ng·h/mL following a 10 mg/kg oral dose and good oralbioavailability of 66%. [1] |
| Name | JAK3-IN-1 |
|---|---|
| Synonym | More Synonyms |
| Description | JAK3-IN-1 is a potent JAK3 inhibitor with IC50 of 4.8 nM, also inhibits JAK1 (IC50 = 896 nM) and JAK2 (IC50 = 1050 nM).IC50 value: 4.8 nM [1]Target: JAK3in vitro: JAK3-IN-1 provides a set of useful tools to pharmacologically interrogate JAK3-dependent biology. JAK3-IN-1 completely inhibits IL-4 induced p-STAT6 at a concentration of 500 nM and only partially inhibits IFNβ-induced p-STAT1 at a concentration of 5.0 μM. In a similar way, JAK3-IN-1 exhibits consistent potency and selectivity for JAK3 in leukemia cancer cell lines: TALL-1 and OCL-AML5. [1]in vivo: JAK3-IN-1 demonstrates reasonable pharmacokinetic properties, with moderate T1/2 of 1.4 h, area under the curve (AUC) value of 795 ng·h/mL following a 10 mg/kg oral dose and good oralbioavailability of 66%. [1] |
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| Related Catalog | |
| Target |
JAK3:4.8 nM (IC50) JAK1:896 nM (IC50) JAK2:1050 nM (IC50) TTK:49 nM (IC50) BTK:794 nM (IC50) ITK:1070 nM (IC50) |
| References |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Molecular Formula | C26H30ClN7O2 |
| Molecular Weight | 508.015 |
| Exact Mass | 507.214966 |
| LogP | 2.18 |
| Index of Refraction | 1.672 |
| Storage condition | 2-8℃ |
| N-(3-{[(5-Chloro-2-{[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino}-4-pyrimidinyl)amino]methyl}phenyl)acrylamide |
| N-(3-{[(5-Chloro-2-{[2-Methoxy-4-(4-Methylpiperazin-1-Yl)phenyl]amino}pyrimidin-4-Yl)amino]methyl}phenyl)prop-2-Enamide |
| 2-Propenamide, N-[3-[[[5-chloro-2-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]methyl]phenyl]- |