AM-1430
AM-1430 is an efficient, highly selective and orally active small molecule inhibitor of PI3Kδ with an IC50 of 4.6 nM. AM-1430 exhibits IC50s for PI3Kα, PI3Kβ and PI3Kγ of 14.18, 2.2 and 3.22 μM, respectively. AM-1430 inhibits B cell proliferation and exhibits excellent in vivo activity in pAKT inhibition models and the hemoglobin (KLH) immune response model. AM-1430 can be used for the study of inflammation and autoimmune diseases.
For research use only. We do not sell to patients.
- CAS No.: 1975263-74-1
- Formula: C23H19FN8O
- Molecular Weight:442.45
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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 4.6 nM (IC50) |
PI3Kα 14.18 μM (IC50) |
PI3Kβ 2.2 μM (IC50) |
PI3Kγ 3.22 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B cell | IC50 |
0.2 nM
Compound: 7; AM-1430
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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 |
14180 nM
Compound: 7; AM-1430
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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 |
2200 nM
Compound: 7; AM-1430
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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] |
| Sf9 | IC50 |
4.6 nM
Compound: 7; AM-1430
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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] |
Chemical Information
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CAS No. 1975263-74-1
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Molecular Weight 442.45
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Formula C23H19FN8O
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SMILES
CNC(C1=C(C([C@@H](NC2=NC=NC(N)=C2C#N)C)=NC3=CC=CC(F)=C13)C4=NC=CC=C4)=O
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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
[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-1430 Related Classifications
HY-115814 Related Classifications
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