- AS-252424
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- $33.00
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2026-08-20
- CAS:900515-16-4
- Purity: 99.26%
- Supply Ability: 10g
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| | 5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione Basic information |
| | 5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione Chemical Properties |
| Melting point | >235oC (dec.) | | density | 1.559±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: >20mg/mL | | pka | 7.20±0.20(Predicted) | | form | solid | | color | yellow |
| | 5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione Usage And Synthesis |
| Uses | AS-252424 is a novel, potent, and selective phosphoinositide 3-kinase gamma (PI3Kγ) inhibitor. It is also an inhibitor of Casein kinase and PI3K p110α. | | Biological Activity | as-252424 is a potent, selective and novel small-molecule pi3kγ inhibitor (ic50= 30 nm)pi3k (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. it plays a key role in pi3k/akt/mtor pathway.in thp-1 (human monocytic cell line), as-252424 inhibited the phosphorylation of pkb/akt due to mcp1 binding to the gpcr receptor ccr2 at lowest ic50 values of 0.4 μm. in primary monocytes and monocytic wild-type cell line thp-1, as-252424 inhibited mcp-1-mediated chemotaxis in a concentration-dependent manner (ic50 value= 52 μm and 53 μm, respectively). [1] in capan 1 and hpaf (pancreatic cancer cell lines), as52424 specifically inhibited the cell proliferation. [2]in a mouse model of thioglycollate-induced peritonitis, oral administration of as-252424 at 10 mg/kg led to moderate reduction of neutrophil recruitment (35% ±14%). [1] | | Biochem/physiol Actions | AS-252424 is a potent and selective phosphoinositide 3-kinase PI3Kγ inhibitor with IC50 = 30 nM in a mouse model. | | in vivo | Oral administration of AS-252424 in a mouse model of acute peritonitis leads to a significant reduction of leukocyte recruitment. To evaluate the efficacy of AS-252424 to block leukocyte migration in vivo, it is tested in a mouse model of thioglycollate-induced peritonitis. Oral administration of AS-252424 at 10 mg/kg results in moderate reduction of neutrophil recruitment (35%±14%), almost matching the result observed in PI3Kγ-deficient mice. Given the short oral half-life of AS-252424 (t1/2=1 h) and relative high clearance (2.25 L/kg per h), investigations at later time points (24-48 h) to assess macrophage and monoycyte recruitment are not undertaken. The modest pharmacokinetic properties do not appear to be caused by rapid oxidative metabolism (microsomal metabolism after 1 h: 16% (rat), 10% (human))[1]. | | IC 50 | PI3Kγ: 30 nM (IC50); PI3Kα: 935 nM (IC50); PI3Kδ: 20 μM (IC50); PI3Kβ: 20 μM (IC50) | | references | 1. pomel v, klicic j, covini d et al. furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma. j med chem. 2006 jun 29;49(13):3857-71.2. edling ce, selvaggi f, buus r et al. key role of phosphoinositide 3-kinase class ib in pancreatic cancer. clin cancer res. 2010 oct 15;16(20):4928-37. |
| | 5-[[5-(4-Fluoro-2-hydroxyphenyl)-2-furanyl]methylene]-2,4-thiazolidinedione Preparation Products And Raw materials |
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