LY294002

別名:SF 1101, NSC 697286

LY294002 (SF 1101, NSC 697286) は人工的に合成した分子としては初めての PI3Kα/δ/β 阻害剤であり、IC50 はそれぞれ 0.5 μM/ 0.57 μM/ 0.97 μM です。溶液中でウォルトマンニン (wortmannin) よりも安定しています。クラス I PI3K および PI3K 関連キナーゼだけでなく、一見 PI3K ファミリーには無関係にある新規のターゲットにも結合します。LY294002 は CK2 阻害剤でもあり、IC50 は 98 nM です。また LY294002 はオートファゴソーム (autophagosome) の形成をブロックする一方で、DNA-PKcs を非特異的に阻害することによりオートファジー (autophagy) を活性化し、アポトーシス (apoptosis) を誘導します。

LY294002化学構造

CAS No. 154447-36-6

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 28600 国内在庫あり
JPY 22000 国内在庫あり
JPY 40500 国内在庫あり
JPY 115500 国内在庫あり
JPY 220500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
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LY294002関連製品

シグナル伝達経路

PI3K阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
human HCT116 cells Function assay 10 μM 10 min Inhibition of PI3Kalpha in human HCT116 cells using [32P]ATP at 10 uM after 10 mins 22212721
human HCT116 cells Function assay 10 μM 10 min Inhibition of PI3Kalpha H1047R mutant in human HCT116 cells using [32P]ATP at 10 uM after 10 mins 22212721
HUVEC Function assay 10-25 μM 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 Function assay 10-25 μM 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
human A2780 cells Apoptosis assay 2 μM 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 SW480 cells Function assay 20 μM 24 h Decrease in survivin expression in human SW480 cells at 20 uM after 24 hrs by immunoblot analysis 17472962
human BJ cells Function assay 25 μM 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 Function assay 25 μM 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 PC3 cells Proliferation assay 25 μM 120 h Antiproliferative activity against human PC3 cells at 25 uM after 120 hrs by MTT assay relative to DMSO 16680159
human H1299 cells Function assay 0.1-30 μM 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 H1299 cells Function assay 0.1-30 μM 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 Function assay 0.1-30 μM 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 Function assay 0.1-30 μM 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 LNCAP cells Function assay 0.1-30 μM 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 LNCAP cells Function assay 0.1-30 μM 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 PC3 cells Function assay 50 μM 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 MGC803 cells Function assay 25 μM 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
mouse RAW264.7 cells Function assay 25 μM 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
MCF7 cells Function assay 10 uM 1 hr Inhibition of IGF1R phosphorylation at Tyr1161 residue in human MCF7 cells at 10 uM after 1 hr by Hoechst 33258 staining based immunohistochemical analysis 28557430
SKOV3 cells Function assay 20 uM 24 hrs Inhibition of BDNF-induced invasion in human SKOV3 cells at 20 uM after 24 hrs in by matrigel invasion assay 29122484
SKOV3 cells Antimigratory assay 20 uM 24 hrs Antimigratory activity against human SKOV3 cells assessed as inhibition of BDNF-induced cell migration at 20 uM after 24 hrs by scratch wound healing assay 29122484
J774 cells Function assay 10 uM 4 hrs Inhibition of PI3K/Akt in mouse J774 cells assessed as reduction in LPS-induced Akt phosphorylation at Ser473 at 10 uM after 4 hrs by Western blot analysis 29726680
human HCT116 cells Function assay 10 μM Inhibition of PI3Kalpha in human HCT116 cells assessed as inhibition of Akt Ser473 phosphorylation at 10 uM by immunoblot analysis 22212721
human HCT116 cells Function assay 10 μM 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 Function assay 10 μM Inhibition of Akt expression in human HCT116 cells at 10 uM by immunoblot analysis 22212721
human H460 cells Function assay 30 μM Inhibition of PI3K in human H460 cells assessed as Akt phosphorylation at Ser 473 up to 30 uM 18501601
mouse mast cells Function assay 20 μM Inhibition of SCF-induced PKB/Akt phosphorylation in mouse mast cells at 20 μM 16789742
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 KB cells Cytotoxic assay 72 h Cytotoxicity against human KB cells after 72 hrs by MTT assay, IC50=44.76 μM. 21945250
human HCT116 cells Cytotoxic assay 72 h Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=56.01 μM. 21945250
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 5 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 1 fold IC50 after 24 hrs by flow cytometry 21216151
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 A375 cells Proliferation assay 46 h Antiproliferative activity against human A375 cells after 46 hrs, IC50=8.4 μM. 17049248
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 H1047R mutant after 48 hrs by MTT assay, IC50=5.3 μM 22212721
human A549 cells Cytotoxic assay 72 h Cytotoxicity against human A549 cells after 72 hrs by MTT assay 22480851
human PC3 cells Cytotoxic assay 72 h Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50=61.35 μM. 22480851
human HL60 cells Cytotoxic assay 72 h Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=9.94 μM. 22480851
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
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
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 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 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 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 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 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
HL60 cells Antiproliferative assay 3 days Antiproliferative activity against human HL60 cells measured after 3 days by MTS assay, IC50 = 14 μM. 26945110
U937 cells Antiproliferative assay 3 days Antiproliferative activity against human U937 cells measured after 3 days by MTS assay, IC50 = 14 μM. 26945110
Jurkat cells Antiproliferative assay 3 days Antiproliferative activity against human Jurkat cells measured after 3 days by MTS assay, IC50 = 22 μM. 26945110
K562 cells Antiproliferative assay 3 days Antiproliferative activity against human K562 cells measured after 3 days by MTS assay, IC50 = 38 μM. 26945110
U266 cells Antiproliferative assay 3 days Antiproliferative activity against human U266 cells measured after 3 days by MTS assay, IC50 = 46 μM. 26945110
MDA-MB-231 cells Antimigratory assay 24 hrs Antimigratory activity against EGF induced chemotaxis in human MDA-MB-231 cells preincubated for 24 hrs followed by EGF addition for 3.5 hrs by light microscopy, IC50 = 0.38 μM. 27598237
MDA-MB-231 cells Antiinvasive assay 3.5 hrs Antiinvasive activity in human MDA-MB-231 cells assessed as inhibition of EGF-induced cell invasion after 3.5 hrs, IC50 = 0.38 μM. 28009521
HEK293T cells Function assay 1 hr Inhibition of immobilized N-LY294002 bead binding to PI3Kbeta (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis, IC50 = 0.42 μM. 28280261
HEK293T cells Function assay 1 hr Inhibition of immobilized N-LY294002 bead binding to PI3Kdelta (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis, IC50 = 1.53 μM. 28280261
HEK293T cells Function assay 1 hr Inhibition of immobilized N-LY294002 bead binding to PI3Kalpha (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis, IC50 = 2.37 μM. 28280261
J774 cells Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced MCP1 expression after 24 hrs by ELISA, IC50 = 3.7 μM. 29726680
J774 cells Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced IL6 expression after 24 hrs by ELISA, IC50 = 5.1 μM. 29726680
J774 cells Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50 = 8.9 μM. 29726680
Sf9 cells Fluorescent polarization assay Inhibition of human PI3Kalpha expressed in Sf9 cells by fluorescent polarization assay, IC50=0.55 μM. 21121631
Sf9 cells fluorescent polarization assay Inhibition of human PI3Kgamma expressed in Sf9 cells by fluorescent polarization assay 21121631
Sf21 cells Function assay Inhibition of mouse recombinant PI3Kalpha expressed in baculovirus-infected Sf21 cells, IC50=0.5 μM. 19748269
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
MDA-MB-231 cells Cytotoxic assay Cytotoxicity against human MDA-MB-231 cells by SRB assay, GI50=6.71 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 184B5 cells Cytotoxic assay Cytotoxicity against human 184B5 cells by SRB assay, GI50=39.37 μM. 18691894
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
rat RBL2H3 cells Function assay Inhibition of A23187-induced degranulation in rat RBL2H3 cells 18328716
Sf9 cells Function assay Inhibition of CK2 expressed in Sf9 cells, IC50=6.9 μM. 18321716
human A375 cells Proliferation assay Inhibition of serum-induced proliferation of human A375 cells, IC50=8.4 μM. 17601739
HeLa cells Function assay Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot, IC5=3 μM. 17135248
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
mouse Raw264 macrophage Function assay Inhibition of C5a-mediated PKB/Akt phosphorylation in mouse Raw264 macrophage, IC50=10 μM. 16789742
THP1 cells Function assay Inhibition of MCP1-induced chemotaxis of THP1 cells, IC50=37 μM. 16789742
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 Binding affinity assay Binding affinity for PI3-kinase isolated from HeLa cells, Ki=6 μM 15658870
HeLa cells Function assay Inhibition of mTOR protein isolated from HeLa cells, IC50=2.5 μM. 15658870
Sf9 cells Function assay Inhibition of His-tagged bovine PI3K expressed in Sf9 cells, IC50=10 μM. 10998351
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
Sf9 cells Function assay Inhibition of His-tagged human CK2 expressed in Sf9 cells, IC50 = 6.9 μM. 10998351
HeLa cells Function assay In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells., IC50 = 1.4 μM. 12941339
HeLa cells Function assay Inhibition of DNA dependent protein kinase isolated from HeLa cells, IC50 = 1.5 μM. 15658870
Sf21 cells Function assay Inhibition of human recombinant PI3Kbeta expressed in baculovirus-infected Sf21 cells, IC50 = 0.9 μM. 19748269
Sf21 cells Function assay Inhibition of bovine recombinant PI3Kgamma expressed in baculovirus-infected Sf21 cells, IC50 = 7 μM. 19748269
HeLa cells Function assay Activity at PI3K in human HeLa cells by ELISA, EC50 = 1.5 μM. 20092323
Sf21 cells Function assay Inhibition of PI3Kdelta expressed in cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging, IC50 = 0.57 μM. 22520630
Sf21 cells Function assay Inhibition of human wild type PI3Kbeta expressed in Sf21 cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging, IC50 = 0.97 μM. 22520630
MDA-MB-231 cells Function assay Inhibition of EGF-induced invasion of human MDA-MB-231 cells by MTT assay, IC50 = 0.38 μM. 28302401
NB1643 cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
SJ-GBM2 cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
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生物活性

製品説明 LY294002 (SF 1101, NSC 697286) は人工的に合成した分子としては初めての PI3Kα/δ/β 阻害剤であり、IC50 はそれぞれ 0.5 μM/ 0.57 μM/ 0.97 μM です。溶液中でウォルトマンニン (wortmannin) よりも安定しています。クラス I PI3K および PI3K 関連キナーゼだけでなく、一見 PI3K ファミリーには無関係にある新規のターゲットにも結合します。LY294002 は CK2 阻害剤でもあり、IC50 は 98 nM です。また LY294002 はオートファゴソーム (autophagosome) の形成をブロックする一方で、DNA-PKcs を非特異的に阻害することによりオートファジー (autophagy) を活性化し、アポトーシス (apoptosis) を誘導します。
Targets
CK2 [5]
(Cell-free assay)
p110α [1]
(Cell-free assay)
p110δ [1]
(Cell-free assay)
p110β [1]
(Cell-free assay)
DNA-PK [6]
(Cell-free)
98 nM 0.5 μM 0.57 μM 0.97 μM 1.4 μM
In Vitro
In vitro

LY294002 is not exclusively selective for the PI3Ks, and could in fact act on other lipid kinases and additional apparently unrelated proteins. LY294002 is shown to inhibit not only mTOR and DNA-PK, but also other protein kinases, such as CK2 (casein kinase 2) and Pim-1[5]. LY294002 inactivates Akt/PKB, consequently inhibiting cell proliferation and inducing apoptosis. LY294002 demonstrates a remarkable growth-inhibitory and apoptosis-inducing effect in these colon cancer cell lines, with decreased expression of phosphorylated Akt (Ser473). [2]LY294002 induces marked nuclear pyknosis and diminished cytoplasmic volume in the tumor cells. Thus, LY294002 markedly inhibits ovarian cancer cell proliferation in vitro. LY294002 induces specific G1 arrest in cell growth, leading to almost complete inhibition of melanoma cell proliferation and partial inhibition of MG-63 (osteosarcoma cell line) proliferation. The effect of LY294002 on cell cycle progression may provide insights into a possible link between the PI3K activation pathway and cancer cell cycle regulation. [3]

Kinase Assay kinase assays
PI3K inhibition by LY294002 is determined in a radiometric assay using purified, recombinant enzymes with 1 μM ATP. The kinase reaction is carried out for 1 hour at room temperature (24oC) and is terminated by addition of PBS. IC50 values are subsequently determined using a sigmoidal dose–response curve fit (variable slope). CK2 and GSK3β (glycogen synthase kinase 3β) inhibition is established by kinase selectivity screening. LY294002 is tested against the Upstate panel of kinases in 10 μM ATP.
細胞実験 細胞株 Colon cancer cell lines DLD-1, LoVo, HCT15, and Colo205
濃度 0–50 μM
反応時間 0–48 hours
実験の流れ

1.0×105 cells (100 μL volume/well) are inoculated into 96-well microtiter plates. LY294002 is added to triplicate wells and cultured at 37oC for 0–48 hours. After treatment, 10 μL of Premix WST-1 are added to each microculture well, and the plates are incubated for 60 minutes at 37oC, after which absorbance at 450 nm is measured with a microplate reader.

実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-p70S6K (T389) / p-GSK3β(S9) / pERK / Vinculin Bcl-xl / Bax / caspase3 / cleaved caspase-3 beta-catenin / p-GSK3β / Cyclin D1 E-cadherin / p-Akt / Akt pPKB-S473 23251002
Growth inhibition assay Cell viability 25344912
Immunofluorescence COX-2 / p-NFκB E-cadherin / beta-catenin α-SMA / CD31 FOXO3a 29731993
ELISA IL-10 / IL-1β / TNFα / IL-6 22208359
In Vivo
In Vivo

LY294002 also results in suppression of tumor growth and induction of apoptosis, especially in the LoVo tumors, and therefore shows remarkable effectiveness in the mouse peritonitis carcinomatosa model. [2] LY294002 significantly inhibits growth and ascites formation of ovarian carcinoma. [3]

動物実験 動物モデル Two groups of athymic nude mice (5–7 weeks) are inoculated i.p. with OVCAR-3 cells
投与量 0–100 mg/kg
投与経路 Administered via i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02337309 Terminated
Neuroblastoma
New Approaches to Neuroblastoma Therapy Consortium|SignalRX Pharmaceuticals Inc.|University of Southern California
July 9 2015 Phase 1

化学情報

分子量 307.34 化学式

C19H17NO3

CAS No. 154447-36-6 SDF Download LY294002 SDFをダウンロードする
Smiles C1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC=C4
保管

In vitro
Batch:

DMSO : 61 mg/mL ( (198.47 mM); Warmed with 50℃ water bath; 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 15 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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よくある質問(FAQ)

質問1:
I want to buy a inhibitor that can inactivates Akt/PI3K. I notice the protocol of LY294002 (catalog no. s1105) says it will inactivates Akt/PKB. Is LY294002 available for Akt/PI3K inhibition?

回答
LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively. It can inhibit PI3K/AKT. PKB is the alternative name of AKT.

質問2:
What is the suggested formulation of this compound for mouse injection(i.p.)?

回答
It can be dissolved in 4% DMSO/30% PEG 300/5% Tween 80/ddH2O at 5 mg/ml clearly, and the concentration of DMSO is safe for in vivo experiments.

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