LAS191954
LAS191954 is a potent, selective and orally active PI3Kδ inhibitor for inflammatory diseases treatment, with an IC50 of 2.6 nM.
For research use only. We do not sell to patients.
- CAS No.: 1403947-26-1
- Formula: C20H15N9O
- Molecular Weight:397.39
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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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PI3Kδ 2.6 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HUVEC | IC50 |
295 nM
Compound: 26; LAS191954
|
Inhibition of PI3Kbeta in HUVEC assessed as reduction in sphingosine-1-phosphate stimulated akt phosphorylation at Ser473 residue preincubated for 15 mins followed by sphingosine-1-phosphate stimulation for 5 mins by HTRF assay
Inhibition of PI3Kbeta in HUVEC assessed as reduction in sphingosine-1-phosphate stimulated akt phosphorylation at Ser473 residue preincubated for 15 mins followed by sphingosine-1-phosphate stimulation for 5 mins by HTRF assay
|
[PMID: 28105286] |
| Sf21 | IC50 |
2.6 nM
Compound: 26; LAS191954
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Inhibition of full length recombinant human N-terminal His6-tagged PI3K p110delta/human p85alpha expressed in baculovirus infected sf21 cells using PIP2 as substrate preincubated for 30 mins followed by substrate addition by HTRF assay
Inhibition of full length recombinant human N-terminal His6-tagged PI3K p110delta/human p85alpha expressed in baculovirus infected sf21 cells using PIP2 as substrate preincubated for 30 mins followed by substrate addition by HTRF assay
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[PMID: 28105286] |
| THP-1 | IC50 |
7.8 nM
Compound: 26; LAS191954
|
Inhibition of PI3Kdelta in human THP1 cells assessed as reduction in MCSF-stimulated akt phosphorylation at Thr308 preincubated for 30 mins followed by MCSF stimulation for 3 mins by ELISA
Inhibition of PI3Kdelta in human THP1 cells assessed as reduction in MCSF-stimulated akt phosphorylation at Thr308 preincubated for 30 mins followed by MCSF stimulation for 3 mins by ELISA
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[PMID: 28105286] |
Chemical Information
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CAS No. 1403947-26-1
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Molecular Weight 397.39
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Formula C20H15N9O
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SMILES
O=C1N(C2=CC=CC=C2)C([C@@H](NC3=C(C#N)C(N)=NC=N3)C)=NN4C1=C(C#N)C=C4
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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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