|2-吗啉-8-苯基-4H-苯并吡喃-4-酮|CsnPharm

CAS No.: 154447-36-6

LY294002/2-吗啉代-8-苯基色酮 Catalog No. CSN11346

Synonyms: SF 1101;NSC 697286

LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays. It is an early-stage autophagy inhibitor and also inhibits CK2.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 PI3Kα

IC50:0.5μM PI3Kβ

IC50:0.97μM PI3Kδ

IC50:0.57μM
描述PI3Ks (Phosphatidylinositol-4,5-bisphosphate 3-kinase) participate in a diverse array of process, including the regulation of cellular survival, differentiation and stem cell-like properties, growth, proliferation, metabolism, migration, and angiogenesis^[2]. LY294002 is the first synthetic molecule to inhibit p110α, p110β and p110δ, which is the 110 kDa catalytic subunit of class IA PI3Ks, with IC50 value of 0.5 μM, 0.57 μM, 0.97 μM (determined using the PI3K lipid kinase assays on recombinant protein), respectively^[1]. LY294002 can induce apoptosis of human nasopharyngeal carcinoma in vitro and in vivo^[3], induce a senescence-like growth arrest in human diploid fibroblasts^[4], decrease invasion and migration of human ovarian carcinoma cells^[5]. Also it can be used as an autophagy inhibitor^[6].
作用机制LY294002 acts at the ATP-binding site of the PI3Ks enzyme.^[7]
细胞研究

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
HEK293 cells	-	Function assay	1.5 h	Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting	22537153
HeLa (human carcinoma) cells.	-	Function assay	-	In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells, IC50=1.4 μM.	15658870
HeLa cells	-	Function assay	-	Inhibition of mTOR protein isolated from HeLa cells, IC50=2.5 μM.	15658870

更多
动物研究
剂量
Mice: 0 - 100 mg/kg^[1] Rats: min = 50 mg/kg^[2], max = 100 mg/kg^[3]

给药途径
i.p.
临床研究

动物研究
剂量	Mice: 0 - 100 mg/kg^[1] Rats: min = 50 mg/kg^[2], max = 100 mg/kg^[3]
给药途径	i.p.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02337309	Neuroblastoma	Phase 1	Terminated(Low patient accrual... more >>) Collapse <<	-	United States, California ... more >> Children's Hospital Los Angeles Los Angeles, California, United States, 90027-0700 UCSF Helen Diller Family Comprehensive Cancer Center San Francisco, California, United States, 94143 United States, Colorado Children Hospital of Colorado Aurora, Colorado, United States, 80045 United States, Georgia AFLAC Cancer Center and Blood Disorders Service of Children's Healthcare of Atlanta - Egleston Campus Atlanta, Georgia, United States, 30322 United States, Illinois University of Chicago Comer Children's Hospital Chicago, Illinois, United States, 60637 United States, Massachusetts Childrens Hospital Boston, Dana-Farber Cancer Institute. Boston, Massachusetts, United States, 02115 United States, Michigan C.S Mott Children's Hospital Ann Arbor, Michigan, United States, 48109 United States, North Carolina University of North Carolina Chapel Hill, North Carolina, United States, 27599 United States, Ohio Cincinnati Children's Hospital Medical Center Cincinnati, Ohio, United States, 45229-3039 United States, Texas Cook Children's Healthcare System Fort Worth, Texas, United States, 76104 United States, Washington Children's Hospital and Regional Medical Center - Seattle Seattle, Washington, United States, 98105 Collapse <<

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.2537 mL
- 16.2686 mL
- 32.5373 mL
- 5 mM
- 0.6507 mL
- 3.2537 mL
- 6.5075 mL
- 10 mM
- 0.3254 mL
- 1.6269 mL
- 3.2537 mL

技术信息

CAS号

154447-36-6

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H17NO3

运输

蓝冰

分子量

307.34

别名

SF 1101;NSC 697286

溶解度

DMSO	51.67 mg/mL (168.1 mM)
Water	insoluble

动物实验配方

5% DMSO+ 40%PEG 300+5% Tween 80+50%water

3 mg/mL

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Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources

HEK293 cells	-	Function assay	1.5 h	Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting	22537153
HeLa (human carcinoma) cells.	-	Function assay	-	In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells, IC50=1.4 μM.	15658870
HeLa cells	-	Function assay	-	Inhibition of mTOR protein isolated from HeLa cells, IC50=2.5 μM.	15658870
HeLa cells	-	Function assay	-	Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot, IC5=3 μM.	17135248
HeLa cells	-	Binding affinity assay	-	Binding affinity for PI3-kinase isolated from HeLa cells, Ki=6 μM	15658870
human 184B5 cells	-	Cytotoxic assay	-	Cytotoxicity against human 184B5 cells by SRB assay, GI50=39.37 μM.	18691894
human A2780 cells	2 μM	Apoptosis assay	12 h	Induction of apoptosis in cisplatin-resistant human A2780 cells assessed as decrease in phosphorylated Akt level at 2 uM after 12 hrs by immunoblot analysis.	17684018
human A375 cells	-	Proliferation assay	46 h	Antiproliferative activity against human A375 cells after 46 hrs, IC50=8.4 μM.	17049248
human A375 cells	-	Proliferation assay	-	Inhibition of serum-induced proliferation of human A375 cells, IC50=8.4 μM.	17601739
human A549 cells	-	Proliferation assay	72 h	Antiproliferative activity against human A549 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=82.32 μM.	25693787
human A549 cells	-	Cytotoxic assay	72 h	Cytotoxicity against human A549 cells after 72 hrs by MTT assay	22480851
human BJ cells	25 μM	Function assay	2 h	Inhibition of PI3K signaling in PDGF-stimulated serum starved human BJ cells transfected with plasmid EGFP/PH domain of Akt assessed as suppression of PH-EGFP redistribution to plasma membrane at 25 uM treated 2 hrs before PDGF challenge by confocal microscopy	16767085
human BJ cells	25 μM	Function assay	2 h	Activation of Akt phosphorylation at Thr308 in PDGF-stimulated serum starved human BJ cells at 25 uM treated 2 hrs before PDGF challenge by immunoblotting	16767085
human BT474 cell	-	Proliferation assay	72 h	Inhibition of human BT474 cell proliferation after 72 hrs by spectrophotometric analysis， IC50=20.7 μM.	23410005
human H1299 cells	0.1-30 μM	Function assay	24 h	Down regulation of cIAP2 expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis	22622069
human H1299 cells	0.1-30 μM	Function assay	24 h	Down regulation of cIAP2 expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis in presence of 100 ug/ml TRAIL and PI3K inhibitor LY294002	22622069
human H1299 cells	0.1-30 μM	Function assay	24 h	Induction of DR5 expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis	22622069
human H1299 cells	0.1-30 μM	Function assay	24 h	Induction of JNK-mediated CHOP expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis	22622069
human H4 cells	-	Function assay	2 h	Decrease in FYVE-RFP+ vesicle intensity per cell in human H4 cells after 2 hrs relative to control	18024584
human H460 cells	30 μM	Function assay	-	Inhibition of PI3K in human H460 cells assessed as Akt phosphorylation at Ser 473 up to 30 uM	18501601
human HCT116 cells	-	Growth inhibition assay	48 h	Growth inhibition of human HCT116 cells overexpressing PI3Kalpha H1047R mutant after 48 hrs by MTT assay, IC50=5.3 μM	22212721
human HCT116 cells	-	Growth inhibition assay	48 h	Growth inhibition of human HCT116 cells after 48 hrs by MTT assay, IC50=5.8 μM.	22212721
human HCT116 cells	-	Growth inhibition assay	48 h	Growth inhibition of human HCT116 cells overexpressing PI3Kalpha after 48 hrs by MTT assay, IC50=6.7 μM.	22212721
human HCT116 cells	10 μM	Function assay	10 min	Inhibition of PI3Kalpha in human HCT116 cells using [32P]ATP at 10 uM after 10 mins	22212721
human HCT116 cells	10 μM	Function assay	10 min	Inhibition of PI3Kalpha H1047R mutant in human HCT116 cells using [32P]ATP at 10 uM after 10 mins	22212721
human HCT116 cells	10 μM	Function assay	-	Inhibition of PI3Kalpha in human HCT116 cells assessed as inhibition of Akt Ser473 phosphorylation at 10 uM by immunoblot analysis	22212721
human HCT116 cells	10 μM	Function assay	-	Inhibition of PI3Kalpha H1047R mutant in human HCT116 cells assessed as inhibition of Akt Ser473 phosphorylation at 10 uM by immunoblot analysis	22212721
human HCT116 cells	10 μM	Function assay	-	Inhibition of Akt expression in human HCT116 cells at 10 uM by immunoblot analysis	22212721
human HCT116 cells	-	Proliferation assay	72 h	Antiproliferative activity against human HCT116 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=51.82 μM.	25693787
human HCT116 cells	-	Cytotoxic assay	72 h	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=56.01 μM.	21945250
human HL60 cells	-	Cytotoxic assay	72 h	Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=9.94 μM.	22480851
human HL60 cells	-	Proliferation assay	72 h	Antiproliferative activity against human HL60 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=18.43 μM.	25693787
human HuH7 cells	-	Proliferation assay	72 h	Antiproliferative activity against human HuH7 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=67.18 μM.	25693787
human IGROV1 cells	-	Function assay	24/48 h	Inhibition of PI3K/Akt in human IGROV1 cells assessed as decrease in phosphorylated AKT level at 1 to 5 times IC50 after 24 to 48 hrs by Western blot analysis	21216151
human IGROV1 cells	-	Function assay	24/48 h	Inhibition of PI3K/Akt in human IGROV1 cells assessed as decrease in cyclin D1 level at 1 to 5 times IC50 after 24 to 48 hrs by Western blot analysis	21216151
human IGROV1 cells	-	Function assay	24 h	Cell cycle arrest in human IGROV1 cells assessed as accumulation at G1 phase at 1 fold IC50 after 24 hrs by flow cytometry	21216151
human IGROV1 cells	-	Function assay	24 h	Cell cycle arrest in human IGROV1 cells assessed as accumulation at G1 phase at 5 fold IC50 after 24 hrs by flow cytometry	21216151
human KB cells	-	Cytotoxic assay	72 h	Cytotoxicity against human KB cells after 72 hrs by MTT assay, IC50=44.76 μM.	21945250
human LNCAP cells	0.1-30 μM	Function assay	30 min	Inhibition of Akt phosphorylation in human LNCAP cells at 0.1 to 30 uM after 30 mins by Western blot analysis	22832316
human LNCAP cells	0.1-30 μM	Function assay	24 h	Downregulation of survivin expression in human LNCAP cells at 0.1 to 30 uM after 24 hrs by Western blot analysis	22832316
human MCF7 cells	-	Cytotoxic assay	-	Cytotoxicity against human MCF7 cells in presence of 20 μM chloroquine by SRB assay, GI50=2.63 μM.	18691894
human MCF7 cells	-	Cytotoxic assay	-	Cytotoxicity against human MCF7 cells in presence of 10 uM chloroquine by SRB assay, GI50=3.08 μM.	18691894
human MCF7 cells	-	Cytotoxic assay	-	Cytotoxicity against human MCF7 cells by SRB assay, GI=3.16 μM.	18691894
human MDA-MB-231 cells	-	Cytotoxic assay	-	Cytotoxicity against human MDA-MB-231 cells in presence of 20 μM chloroquine by SRB assay, GI=3.32 μM.	18691894
human MDA-MB-231 cells	-	Cytotoxic assay	-	Cytotoxicity against human MDA-MB-231 cells in presence of 10 uM chloroquine by SRB assay, GI50=4.35 μM.	18691894
human MDA-MB-468 cells	-	Cytotoxic assay	-	Cytotoxicity against human MDA-MB-468 cells in presence of 20 uM chloroquine by SRB assay， IC50=4.76 μM.	18691894
human MDA-MB-468 cells	-	Cytotoxic assay	-	Cytotoxicity against human MDA-MB-468 cells in presence of 10 uM chloroquine by SRB assay, GI50=8.2 μM.	18691894
human MDA-MB-468 cells	-	Cytotoxic assay	-	Cytotoxicity against human MDA-MB-468 cells by SRB assay, IC50=10.4 μM.	18691894
human MGC803 cells	25 μM	Function assay	48 h	Cell cycle arrest in human MGC803 cells assessed as accumulation at G2/M phase at 25 uM after 48 hrs using propidium iodide staining after 48 hrs by flow cytometer relative to control	24119869
human PC3 cell	-	Proliferation assay	72 h	Inhibition of human PC3 cell proliferation after 72 hrs by spectrophotometric analysis, IC50=12.1 μM.	23410005
human PC3 cells	-	Function assay	30 min	Inhibition of PI3K in human PC3 cells assessed as decrease in AKT phosphorylation at serine 473 after 30 mins by ELISA, IC50=1.3μM.	23410005
human PC3 cells	50 μM	Function assay	8 h	Induction of p21 protein expression in human PC3 cells at 50 uM incubated for 8 hrs by Western blotting relative to untreated control	22998472
human PC3 cells	-	Cytotoxic assay	72 h	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50=61.35 μM.	22480851
human PC3 cells	25 μM	Proliferation assay	120 h	Antiproliferative activity against human PC3 cells at 25 uM after 120 hrs by MTT assay relative to DMSO	16680159
human SW480 cells	20 μM	Function assay	24 h	Decrease in survivin expression in human SW480 cells at 20 uM after 24 hrs by immunoblot analysis	17472962
human U251HRE cells	-	Function assay	-	Inhibition of hypoxia-induced HIF1 activation in human U251HRE cells by cell based reporter gene assay	18501601
human U87MG cells	-	Function assay	-	Inhibition of GSK3-beta in human U87MG cells by ELISA, IC50=8.1 μM.	18345609
HUVEC	10-25 μM	Function assay	16 h	Inhibition of TNFalpha-stimulated ICAM-1 mRNA expression in HUVEC at 10 to 25 uM pretreated for 16 hrs before TNFalpha challenge measured after 6 hrs by RT-PCR analysis	22026410
HUVEC	10-25 μM	Function assay	30 min	Inhibition of TNFalpha-stimulated human ICAM-1 promoter activity expressed in HUVEC assessed as beta-galactosidase activity at 10 to 25 uM pretreated for 30 mins before TNFalpha challenge measured after 5 hrs by luciferase reporter gene assay	22026410
MDA-MB-231 cells	-	Cell invasion assay	24 h	Inhibition of epithelial growth factor-induced cell migration of human MDA-MB-231 cells pre-incubated for 24 hrs by cell invasion assay, IC50=0.38 μM.	22804108
MDA-MB-231 cells	-	Cytotoxic assay	-	Cytotoxicity against human MDA-MB-231 cells by SRB assay, GI50=6.71 μM.	18691894
mouse mast cells	20 μM	Function assay	-	Inhibition of SCF-induced PKB/Akt phosphorylation in mouse mast cells at 20 μM	16789742
mouse Raw264 macrophage	-	Function assay	-	Inhibition of C5a-mediated PKB/Akt phosphorylation in mouse Raw264 macrophage, IC50=10 μM.	16789742
mouse RAW264.7 cells	25 μM	Function assay	20 h	Inhibition of PI3K/AKT in mouse RAW264.7 cells assessed as inhibition of LPS-induced iNOS protein expression at 25 μM after 20 hrs by Western blot analysis	24299616
rat RBL2H3 cells	-	Function assay	-	Inhibition of A23187-induced degranulation in rat RBL2H3 cells	18328716
Sf21 cells	-	Function assay	-	Inhibition of mouse wild type PI3Kalpha expressed in Sf21 cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging, IC50=0.5 μM	22520630
Sf21 cells	-	Function assay	-	Inhibition of mouse recombinant PI3Kalpha expressed in baculovirus-infected Sf21 cells, IC50=0.5 μM.	19748269
Sf9 cells	-	Fluorescent polarization assay	-	Inhibition of human PI3Kalpha expressed in Sf9 cells by fluorescent polarization assay, IC50=0.55 μM.	21121631
Sf9 cells	-	Function assay	-	Inhibition of CK2 expressed in Sf9 cells, IC50=6.9 μM.	18321716
Sf9 cells	-	Function assay	-	Inhibition of His-tagged bovine PI3K expressed in Sf9 cells, IC50=10 μM.	10998351
Sf9 cells	-	fluorescent polarization assay	-	Inhibition of human PI3Kgamma expressed in Sf9 cells by fluorescent polarization assay	21121631
THP1 cells	-	Function assay	-	Inhibition of SCF1-induced PKB/Akt phosphorylation in THP1 cells, IC50=1.01 μM.	16789742
THP1 cells	-	Function assay	-	Inhibition of MCP1-induced PKB/Akt phosphorylation in THP1 cells, IC50=1.65 μM.	16789742
THP1 cells	-	Function assay	-	Inhibition of MCP1-induced chemotaxis of THP1 cells, IC50=37 μM.	16789742

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02337309

Neuroblastoma

Phase 1

Terminated(Low patient accrual... more >>) Collapse <<

United States, California ... more >> Children's Hospital Los Angeles Los Angeles, California, United States, 90027-0700 UCSF Helen Diller Family Comprehensive Cancer Center San Francisco, California, United States, 94143 United States, Colorado Children Hospital of Colorado Aurora, Colorado, United States, 80045 United States, Georgia AFLAC Cancer Center and Blood Disorders Service of Children's Healthcare of Atlanta - Egleston Campus Atlanta, Georgia, United States, 30322 United States, Illinois University of Chicago Comer Children's Hospital Chicago, Illinois, United States, 60637 United States, Massachusetts Childrens Hospital Boston, Dana-Farber Cancer Institute. Boston, Massachusetts, United States, 02115 United States, Michigan C.S Mott Children's Hospital Ann Arbor, Michigan, United States, 48109 United States, North Carolina University of North Carolina Chapel Hill, North Carolina, United States, 27599 United States, Ohio Cincinnati Children's Hospital Medical Center Cincinnati, Ohio, United States, 45229-3039 United States, Texas Cook Children's Healthcare System Fort Worth, Texas, United States, 76104 United States, Washington Children's Hospital and Regional Medical Center - Seattle Seattle, Washington, United States, 98105 Collapse <<

靶点	Description	IC50
PI3Kα		IC50:0.5μM
PI3Kβ		IC50:0.97μM
PI3Kδ		IC50:0.57μM

LY294002/2-吗啉代-8-苯基色酮 Catalog No. CSN11346

靶点选择性

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