AM-0687
AM-0687 is a selective inhibitor for PI3Kδ with an IC50 of 2.9 nM. AM-0687 decreases the levels of IgG and IgM specific antibodies, inhibits the anti-IgM/CD40L-induced proliferation of human B cell (IC50=0.8 nM) and the phosphorylation of AKT (IC50=0.7 nM), and exhibits anti-inflammatory efficacy.
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- CAS No.: 1259522-94-5
- Formule: C23H19FN8O
- Masse moléculaire:442.45
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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PI3Kδ 2.9 nM (IC50) |
PI3Kβ 2840 nM (IC50) |
PI3Kγ 3530 nM (IC50) |
PI3Kα 17600 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B cell | IC50 |
0.8 nM
Compound: 6a; AM-0687
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Inhibition of cell proliferation of human B cells pre-incubated for 30 mins before anti-IgM/CD40L stimulation and measured after 72 hrs by [3H]thymidine incorporation assay
Inhibition of cell proliferation of human B cells pre-incubated for 30 mins before anti-IgM/CD40L stimulation and measured after 72 hrs by [3H]thymidine incorporation assay
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[PMID: 27411843] |
| Sf9 | IC50 |
17600 nM
Compound: 6a; AM-0687
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Inhibition of polyHis tagged full length recombinant PI3Kalpha (unknown origin) expressed in Sf9 cells co-expressing p85 incubated for 20 mins by alpha screen assay
Inhibition of polyHis tagged full length recombinant PI3Kalpha (unknown origin) expressed in Sf9 cells co-expressing p85 incubated for 20 mins by alpha screen assay
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[PMID: 27411843] |
| Sf9 | IC50 |
2.9 nM
Compound: 6a; AM-0687
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Inhibition of polyHis tagged full length recombinant PI3Kdelta (unknown origin) expressed in Sf9 cells co-expressing p85 incubated for 20 mins by alpha screen assay
Inhibition of polyHis tagged full length recombinant PI3Kdelta (unknown origin) expressed in Sf9 cells co-expressing p85 incubated for 20 mins by alpha screen assay
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[PMID: 27411843] |
| Sf9 | IC50 |
2840 nM
Compound: 6a; AM-0687
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Inhibition of polyHis tagged full length recombinant PI3Kbeta (unknown origin) expressed in Sf9 cells co-expressing p85 incubated for 20 mins by alpha screen assay
Inhibition of polyHis tagged full length recombinant PI3Kbeta (unknown origin) expressed in Sf9 cells co-expressing p85 incubated for 20 mins by alpha screen assay
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[PMID: 27411843] |
Chemical Information
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CAS No. 1259522-94-5
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Masse moléculaire 442.45
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Formule C23H19FN8O
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SMILES
O=C(C1=C(C2=NC=CC=C2)C([C@@H](NC3=NC=NC(N)=C3C#N)C)=NC4=CC=C(F)C=C14)NC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Gonzalez-Lopez de Turiso F, et al. Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-1430). J Med Chem. 2016 Aug 11;59(15):7252-67. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AM-0687 Related Classifications
HY-120471 Related Classifications
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