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Merck

SML1381

Sigma-Aldrich

PIK-294

≥98% (HPLC)

别名:

2-((4-Amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)methyl)-5-methyl-3-o-tolylquinazolin-4(3H)-one, 2-[[4-Amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl]methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone, PIK294

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About This Item

经验公式(希尔记法):
C28H23N7O2
分子量:
489.53
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

品質等級

化驗

≥98% (HPLC)

形狀

powder

顏色

white to beige

溶解度

H2O: 10 mg/mL, clear
DMSO: 5 mg/mL, clear (warmed)

儲存溫度

−20°C

SMILES 字串

NC1=C2C(N(CC(N3C4=C(C)C=CC=C4)=NC5=C(C(C)=CC=C5)C3=O)N=C2C6=CC(O)=CC=C6)=NC=N1

InChI

1S/C28H23N7O2/c1-16-7-3-4-12-21(16)35-22(32-20-11-5-8-17(2)23(20)28(35)37)14-34-27-24(26(29)30-15-31-27)25(33-34)18-9-6-10-19(36)13-18/h3-13,15,36H,14H2,1-2H3,(H2,29,30,31)

InChI 密鑰

WFSLJOPRIJSOJR-UHFFFAOYSA-N

應用

PIK-294 has been used as PI3K inhibitor in drug combination studies and their synergy quantification using the Chou-Talalay method.

生化/生理作用

PIK-294 is a highly selective inihibitor of the phosphoinositide 3-kinase (PI3K) p110δ with an IC50 value of 10 nM compared to IC50 values of 10 μM, 490 nM and 160 nM for PI3Kα/β/γ, respectively. PIK-294 has been used to help distinguish the unique roles of the various PI3-K isoforms. For example, in a study of CXCL8-induced neutrophil migration, PIK-294 inhibited both chemokinetic and chemotactic CXCL8-induced migration whereas PI3Kγ inhibitor AS-605240 markedly reduced CXCL8 induced chemokinetic migration but had no effect on CXCL8 induced chemotactic migration.

象形圖

Skull and crossbones

訊號詞

Danger

危險聲明

危險分類

Acute Tox. 3 Oral

儲存類別代碼

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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Raoni Pais Siqueira et al.
Toxicology in vitro : an international journal published in association with BIBRA, 65, 104777-104777 (2020-01-22)
The serine/arginine protein kinases respond to the EGFR-PI3K-AKT signaling module in the context of pre-mRNA alternative splicing regulation. These enzymes (notably SRPK1 and SRPK2) have been found dysregulated in a variety of cancers, which suggests them as promising drug targets

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