LAS191954
LAS191954 is a potent, selective and orally active PI3Kδ inhibitor for inflammatory diseases treatment, with an IC50 of 2.6 nM.
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- CAS No.: 1403947-26-1
- 화학식: C20H15N9O
- 분자량:397.39
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
PI3Kδ 2.6 nM (IC50) |
|
Cell Line
|
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 No. 1403947-26-1
-
분자량 397.39
-
화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)