LY294002

别名: SF 1101, NSC 697286

目录号：S1105 Purity: 99.99%

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

规格	价格	库存
10mM (1mL in DMSO)	RMB 1570.11	现货
10mg	RMB 1188.16	现货
25mg	RMB 2196.01	现货
200mg	RMB 6298.74	现货
1g	RMB 12039.3	现货
更大包装有超大折扣
400-668-6834 info@selleck.cn

客户使用Selleck的LY294002发表文献1552篇

产品质控

批次：纯度： 99.99%

99.99

LY294002相关产品

相关靶点	p110α p110β p110δ p110γ C2β Vps34	点击展开
相关化合物库	激酶抑制剂库 PI3K/Akt 抑制剂库凋亡分子化合物库细胞周期化合物库 NF-κB信号通路库	点击展开

PI3K抑制剂选择性比较

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

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

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

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]
激酶实验	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(24^oC)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37^oC下培养0-48小时。处理后, 10 μL Premix WST-1 加到每孔中,然后在37^oC下温育60分钟,然后用微型计数板在450nm处测定吸光值。
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		29731993
	Growth inhibition assay	Cell viability		25344912
	Immunofluorescence	α-SMA / CD31 E-cadherin / beta-catenin COX-2 / p-NFκB FOXO3a		27671604
	ELISA	IL-10 / IL-1β / TNFα / IL-6		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]
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
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT02337309	Terminated	Neuroblastoma	New Approaches to Neuroblastoma Therapy Consortium\|SignalRX Pharmaceuticals Inc.\|University of Southern California	July 9 2015	Phase 1

参考文献
[1] Chaussade C, et al. Biochem J, 2007, 404(3), 449-58. [2] Semba S, et al. Clin Cancer Res, 2002, 8(6), 1957-63. [3] Hu L, et al. Clin Cancer Res, 2000, 6(3), 880-6. [4] Gharbi SI, et al. Biochem J, 2007, 404(1), 15-21. [5] Severine I. Gharbi, et al. Biochem J. 2007, 404(3):449-58. [6] David Davidson, et al. Front Pharmacol. 2013, 4: 5. + 展开

参考文献

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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)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

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

Water : Insoluble

摩尔浓度计算器

体内溶解度批次：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
体内溶解度批次：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	澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	3.4mg/ml (11.06mM)	以 1 mL 工作液为例,取50μL68mg/ml的澄清DMSO储备液加到400μLPEG300中,混合均匀使其澄清;向上述体系中加入50μLTween80,混合均匀使其澄清;然后继续加入500μLddH2O定容至1mL。工作液请现配现用!	动物体内配方计算器
澄清溶液	5%absolute ethyl alcohol 1 95%Corn oil	1mg/ml (3.25mM)	以 1 mL 工作液为例，取50μL20mg/ml的澄清 absolute ethyl alcohol 储备液加到950μL玉米油中，混合均匀。工作液请现配现用！
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	3mg/ml (9.76mM)	以 1 mL 工作液为例，取50μL60mg/ml的澄清DMSO储备液加到 400μL PEG300中，混合均匀使其澄清；向上述体系中加入50μLTween80，混合均匀使其澄清；然后继续加入500μL ddH2O定容至 1 mL。工作液请现配现用！

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

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）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

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。

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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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