AS1940477 | p38α/β inhibitor | Probechem Biochemicals

Chemical Structure : AS1940477

AS1940477 (AS 1940477, AS-1940477)

Catalog No.: PC-61001Not For Human Use, Lab Use Only.

AS1940477 is a potent, selective, orally active p38α/p38β inhibitor with IC50 of 11.2/36.5 nM respectively, with no effect on p38γ and δ isoforms (IC50>1 uM).

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Biological Activity

AS1940477 is a potent, selective, orally active p38α/p38β inhibitor with IC50 of 11.2/36.5 nM respectively, with no effect on p38γ and δ isoforms (IC50>1 uM).
AS1940477 displays no activity against a panel of 100 protein kinases, including JNK2, EGFR, Akt and Pim.
AS1940477 inhibits LPS- or PHA-induced production of proinflammatory cytokines, including TNFα, IL-1β, and IL-6 at low concentrations (LPS/TNFα, IC50=0.45 nM; PHA/TNFα, IC50=0.40 nM) in human PBMCs, also inhibits TNFα- and IL-1 β-induced production of IL-6, PGE(2), and MMP-3 in human synovial stromal cells.
AS1940477 potently inhibits TNF production in whole blood (IC50=12 nM) and effectively inhibits TNFα production induced by LPS in rats with long-acting anti-inflammatory effect.

Physicochemical Properties

M.Wt	431.471
Formula	C24H22FN5O2
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	6-[(6R)-2-(4-fluorophenyl)-6-(hydroxymethyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidin-3-yl]-2-(2-methylphenyl)pyridazin-3(2H)-one

References

1. Asano T, et al. J Med Chem. 2012 Sep 13;55(17):7772-85.

2. Terajima M, et al. Eur J Pharmacol. 2013 Jan 5;698(1-3):455-62.

AS1940477 (AS 1940477, AS-1940477)

Biological Activity

Physicochemical Properties

References

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