1975263-74-1
Chemical Structure
AM-1430
- CAS No.: 1975263-74-1
- Formula:C23H19FN8O
- Molecular Weight:442.45
IUPAC Name: (S)-2-(1-((6-amino-5-cyanopyrimidin-4-yl)amino)ethyl)-5-fluoro-N-methyl-3-(pyridin-2-yl)quinoline-4-carboxamide
InChIKey: CCLUQQJLBVGECO-LBPRGKRZSA-N
SMILES: CNC(C1=C(C([C@@H](NC2=NC=NC(N)=C2C#N)C)=NC3=CC=CC(F)=C13)C4=NC=CC=C4)=O
Biological Activity: 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[1].
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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. | |||||||||||||||||||||
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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]
