LAS191954
LAS191954 is a potent, selective and orally active PI3Kδ inhibitor for inflammatory diseases treatment, with an IC50 of 2.6 nM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 1403947-26-1
- Formel: C20H15N9O
- Molecular Weight:397.39
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
PI3Kδ 2.6 nM (IC50) |
Cellular Effect
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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
|
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
|
[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
|
[PMID: 28105286] |
Chemical Information
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CAS. Nr. 1403947-26-1
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Molecular Weight 397.39
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Formel 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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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)