JAK1-IN-17
JAK1-IN-17 (Compound 31) is a highly selective inhibitor of JAK1 with a Ki of 1.9 nM. JAK1-IN-17 exhibits a low whole blood shift, which allows maintaining good whole blood potency. JAK1-IN-17 is also a nitrile-containing analogue with consistent, yet weak reversible inhibition of CYP3A4 using a midazolam probe (IC50 = 7.9 μM). JAK1-IN-17 can be studied in cancer research.
For research use only. We do not sell to patients.
- CAS No.: 1315490-71-1
- Formula: C17H19N5O
- Molecular Weight:309.37
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>100 μM
Compound: 31
|
Inhibition of human ERG channel expressed in HEK293 cells by patch clamp assay
Inhibition of human ERG channel expressed in HEK293 cells by patch clamp assay
|
[PMID: 23659214] |
| TF-1 | EC50 |
120 nM
Compound: 31
|
Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins
Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins
|
[PMID: 23659214] |
| TF-1 | EC50 |
130 nM
Compound: 31
|
Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins in presence of whole blood
Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins in presence of whole blood
|
[PMID: 23659214] |
Chemical Information
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CAS No. 1315490-71-1
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Molecular Weight 309.37
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Formula C17H19N5O
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SMILES
N#C[C@H]1CC[C@H](N2C([C@H](O)C)=NC3=CN=C(NC=C4)C4=C32)CC1
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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)