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[1].
Product Specifications
CAS Number
1975263-74-1
UNSPSC
12352005
Target
PI3K
Related Pathways
PI3K/Akt/mTOR
Field of Research
Inflammation/Immunology
Smiles
CNC(C1=C(C([C@@H](NC2=NC=NC(N)=C2C#N)C)=NC3=CC=CC(F)=C13)C4=NC=CC=C4)=O
Molecular Formula
C23H19FN8O
Molecular Weight
442.45
References & Citations
[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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
PI3Kα; PI3Kβ; PI3Kγ; PI3Kδ
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