LY294002
别名: SF 1101, NSC 697286
LY294002 (SF 1101, NSC 697286) 是首个合成的已知抑制PI3Kα/δ/β的小分子，在无细胞测定中IC50分别为 0.5 μM/0.57 μM/0.97 μM；在溶液中比在Wortmannin中稳定，也能够阻断自噬体的形成。它不仅能够结合class I PI3Ks和其他PI3K相关的激酶，还能够结合一些与PI3K家族无关的新型靶点。LY294002 可以抑制CK2，对应的IC50值为98 nM。LY294002 是一种非特异的 DNA-PKcs 抑制剂，并可激活自噬和凋亡。
LY294002 Chemical Structure
CAS: 154447-36-6
产品质控
批次：
纯度：
99.99%
99.99
LY294002相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | LY294002 (SF 1101, NSC 697286) 是首个合成的已知抑制PI3Kα/δ/β的小分子，在无细胞测定中IC50分别为 0.5 μM/0.57 μM/0.97 μM；在溶液中比在Wortmannin中稳定，也能够阻断自噬体的形成。它不仅能够结合class I PI3Ks和其他PI3K相关的激酶，还能够结合一些与PI3K家族无关的新型靶点。LY294002 可以抑制CK2，对应的IC50值为98 nM。LY294002 是一种非特异的 DNA-PKcs 抑制剂，并可激活自噬和凋亡。 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | LY294002是选择性的, 可渗透细胞的特定PI3K抑制剂，可作用于酶的ATP结合位点，且抑制自体吞噬的螯合作用。 | ||||||||||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | LY294002是一种非特异性抑制剂，除了class I PI3Ks，它同样还能抑制其他类型PI3Ks、mTOR、DNA-PK以及其他蛋白激酶，如CK2和Pim-1[5]。LY294002使Akt/PKB失活,因此抑制细胞增殖和诱导细胞凋亡。 LY294002作用于结肠癌细胞系，使磷酸化Akt (Ser473)的表达下降， 明显抑制生长和诱导凋亡。[2] LY294002作用于肿瘤细胞，诱导明显的核固缩和减少细胞质体积。因此，在体外，LY294002明显抑制卵巢癌细胞增殖。LY294002诱导细胞停在G1期，导致几乎全部的黑色素瘤细胞增殖被抑制，部分MG-63 (骨肉瘤细胞系)增殖被抑制。LY294002作用于细胞周期的效果可用于研究PI3K激活通路和癌细胞周期之间关系。[3] |
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| 激酶实验 | 激酶实验 | |||
| 使用重组酶和1 μM ATP，通过辐射实验测定LY294002对PI3K的抑制效果。室温下(24oC)进行激酶反应1小时，然后加入PBS终止反应。通过剂量反应曲线测定IC50值。通过激酶选择性筛选来抑制CK2和GSK3β。加入10 μM ATP，测定LY294002作用于一组激酶的效果。 | ||||
| 细胞实验 | 细胞系 | 结肠癌细胞系： DLD-1, LoVo, HCT15, 和Colo205 | ||
| 浓度 | 0-50 μM | |||
| 孵育时间 | 0-48小时 | |||
| 方法 | 1×105个细胞(每孔100 μL)接种在96孔板上。设三个复孔，加入LY294002，在37oC下培养0-48小时。处理后, 10 μL Premix WST-1 加到每孔中,然后在37oC下温育60分钟,然后用微型计数板在450nm处测定吸光值。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | E-cadherin / p-Akt / Akt beta-catenin / p-GSK3β / Cyclin D1 Bcl-xl / Bax / caspase3 / cleaved caspase-3 p-p70S6K (T389) / p-GSK3β(S9) / pERK / Vinculin pPKB-S473 |
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29731993 | |
| Growth inhibition assay | Cell viability |
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25344912 | |
| Immunofluorescence | α-SMA / CD31 E-cadherin / beta-catenin COX-2 / p-NFκB FOXO3a |
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27671604 | |
| ELISA | IL-10 / IL-1β / TNFα / IL-6 |
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22208359 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 体内，LY294002也抑制肿瘤生长和诱导凋亡，尤其作用于LoVo肿瘤, 因此作用于鼠癌性腹膜炎模型具有明显药效。[2] LY294002明显抑制卵巢癌生长和腹水形成。[3] |
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|---|---|---|
| 动物实验 | Animal Models | 腹腔注射OVCAR-3细胞的无胸腺裸鼠(5-7周大) |
| Dosages | 0-100 mg/kg | |
| Administration | 每天腹腔注射，持续3周 | |
| 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 |
化学信息&溶解度
| 分子量 | 307.34 | 分子式 | C19H17NO3 |
| CAS号 | 154447-36-6 | SDF | Download LY294002 SDF |
| Smiles | C1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC=C4 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 61 mg/mL ( (198.47 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 15 mg/mL (48.8 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
技术支持
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常见问题及建议解决方法
问题 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.
问题 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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