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LY294002 PI3K 억제제

Name: LY294002
Brand: Selleck Chemicals
SKU: S1105
Rating: 5 (1657 reviews)

제품 번호S1105

LY294002 (SF 1101, NSC 697286)는 각각 0.5 μM/0.57 μM/0.97 μM의 IC50으로 PI3Kα/δ/β를 억제하는 것으로 알려진 최초의 합성 분자이며, 워트마닌보다 용액에서 더 안정하고 자가포식체 형성을 차단합니다. 이는 Class I PI3K 및 기타 PI3K 관련 키나아제뿐만 아니라 PI3K 계열과 관련이 없어 보이는 새로운 표적에도 결합합니다. 이 화합물은 또한 98 nM의 IC50으로 CK2를 억제합니다. 이는 비특이적인 DNA-PKcs 억제제이며 autophagy 및 apoptosis를 활성화합니다.

화학 구조

분자량: 307.34

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품질 관리

배치: 순도: 99.99%

99.99

관련 타겟	Akt mTOR GSK-3 ATM/ATR DNA-PK AMPK PDPK1 PTEN PP2A PDK
기타 PI3K 억제제	GDC-0077 (Inavolisib) SAR405 Quercetin (Sophoretin) XL147 analogue Tersolisib (STX-478) Buparlisib (BKM120) 740 Y-P (PDGFR 740Y-P) GO-203 TFA Eganelisib (IPI-549) Paxalisib (GDC-0084)

세포 배양, 처리 및 작업 농도

세포주	분석 유형	농도	배양 시간	활성 설명	PMID
Sf9 cells	Function assay			Inhibition of His-tagged bovine PI3K expressed in Sf9 cells, IC50=10 μM.	10998351
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
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
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 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 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
mouse mast cells	Function assay	20 μM		Inhibition of SCF-induced PKB/Akt phosphorylation in mouse mast cells at 20 μM	16789742
THP1 cells	Function assay			Inhibition of MCP1-induced chemotaxis of THP1 cells, IC50=37 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 PKB/Akt phosphorylation in THP1 cells, IC50=1.65 μM.	16789742
THP1 cells	Function assay			Inhibition of SCF1-induced PKB/Akt phosphorylation in THP1 cells, IC50=1.01 μM.	16789742
human A375 cells	Proliferation assay		46 h	Antiproliferative activity against human A375 cells after 46 hrs, IC50=8.4 μM.	17049248
HeLa cells	Function assay			Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot, IC5=3 μM.	17135248
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 A375 cells	Proliferation assay			Inhibition of serum-induced proliferation of human A375 cells, IC50=8.4 μM.	17601739
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 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
Sf9 cells	Function assay			Inhibition of CK2 expressed in Sf9 cells, IC50=6.9 μM.	18321716
rat RBL2H3 cells	Function assay			Inhibition of A23187-induced degranulation in rat RBL2H3 cells	18328716
human U87MG cells	Function assay			Inhibition of GSK3-beta in human U87MG cells by ELISA, IC50=8.1 μM.	18345609
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
human U251HRE cells	Function assay			Inhibition of hypoxia-induced HIF1 activation in human U251HRE cells by cell based reporter gene assay	18501601
human 184B5 cells	Cytotoxic assay			Cytotoxicity against human 184B5 cells by SRB assay, GI50=39.37 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 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
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 20 uM chloroquine by SRB assay， IC50=4.76 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-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 MCF7 cells	Cytotoxic assay			Cytotoxicity against human MCF7 cells by SRB assay, GI=3.16 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 in presence of 20 μM chloroquine by SRB assay, GI50=2.63 μM.	18691894
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 PI3Kgamma expressed in Sf9 cells by fluorescent polarization assay	21121631
Sf9 cells	Fluorescent polarization assay			Inhibition of human PI3Kalpha expressed in Sf9 cells by fluorescent polarization assay, IC50=0.55 μM.	21121631
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 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		24/48 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 HCT116 cells	Cytotoxic assay		72 h	Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=56.01 μM.	21945250
human KB cells	Cytotoxic assay		72 h	Cytotoxicity against human KB cells after 72 hrs by MTT assay, IC50=44.76 μM.	21945250
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
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
human HCT116 cells	Function assay	10 μM		Inhibition of Akt expression in human HCT116 cells 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 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	10 min	Inhibition of PI3Kalpha H1047R mutant 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 in human HCT116 cells using [32P]ATP at 10 uM after 10 mins	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	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
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
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
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
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 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 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 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
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
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
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
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
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
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
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
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
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성

분자량	307.34	화학식	C₁₉H₁₇NO₃	보관 (수령일로부터)	3년-20°C분말
CAS 번호	154447-36-6	SDF 다운로드		원액 보관	1년-80°C용매에 보관 1개월-20°C용매에 보관
동의어	SF 1101, NSC 697286			Smiles	C1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC=C4

용해도

In vitro
배치:

DMSO : 80 mg/mL (260.29 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 15 mg/mL

Water : Insoluble

DMSO : 61 mg/mL (198.47 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 61 mg/mL

Water : Insoluble

DMSO : 61 mg/mL (198.47 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 10 mg/mL

Water : Insoluble

DMSO : 61 mg/mL (198.47 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 61 mg/mL

Water : Insoluble

DMSO : 31 mg/mL (100.86 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 31 mg/mL

Water : Insoluble

몰농도 계산기

질량	농도	부피	분자량
=	×	×

희석 계산기 분자량 계산기

In vivo 배치:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	3.400mg/ml (11.06mM)	Taking the 1 mL working solution as an example, add 50 μL of 68 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%absolute ethyl alcohol 1 95%Corn oil Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	1.000mg/ml (3.25mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear absolute ethyl alcohol stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 20%PEG300 2 5%Tween80 3 70%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	3.500mg/ml (11.39mM)	Taking the 1 mL working solution as an example, add 50 μL of 70 mg/ml clarified DMSO stock solution to 200 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 700 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Selleck 연구소에서 검증되었습니다. 이 제형에 대한 조정이 필요한 경우 맞춤 테스트를 위해 당사 영업팀에 문의하십시오.	3.000mg/ml (9.76mM)	Taking the 1 mL working solution as an example, add 50 μL of 60 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

투여량: mg/kg 동물 평균 체중: g 동물당 투여량:μL 동물 수:

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH₂O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘

Targets/IC₅₀/Ki	CK2 (Cell-free assay) 98 nM p110α (Cell-free assay) 0.5 μM p110δ (Cell-free assay) 0.57 μM p110β (Cell-free assay) 0.97 μM DNA-PK (Cell-free) 1.4 μM
시험관 내(In vitro)	LY294002는 PI3K에만 독점적으로 선택적인 것이 아니며, 사실 다른 지질 키나아제와 추가적인 관련 없어 보이는 단백질에도 작용할 수 있습니다. 이 화합물은 mTOR 및 DNA-PK뿐만 아니라 CK2 (casein kinase 2) 및 Pim-1과 같은 다른 단백질 키나아제도 억제하는 것으로 나타났습니다. 이는 Akt/PKB를 비활성화하여 결과적으로 세포 증식을 억제하고 세포자멸사를 유도합니다. 이 화학 물질은 인산화된 Akt (Ser473)의 발현 감소와 함께 이러한 결장암 세포주에서 현저한 성장 억제 및 세포자멸사 유도 효과를 보입니다. 이는 종양 세포에서 현저한 핵 응축 및 감소된 세포질 부피를 유도합니다. 따라서 이 화합물은 시험관 내에서 난소암 세포 증식을 현저히 억제합니다. 이는 세포 성장 시 특정 G1기 정지를 유도하여 흑색종 세포 증식의 거의 완전한 억제와 MG-63 (골육종 세포주) 증식의 부분적인 억제를 초래합니다. 이 화학 물질의 세포 주기 진행에 대한 효과는 PI3K 활성화 경로와 암세포 주기 조절 사이의 가능한 연관성에 대한 통찰력을 제공할 수 있습니다.
키나아제 분석	키나아제 분석
키나아제 분석	LY294002에 의한 PI3K 억제는 1 μM ATP를 사용하여 정제된 재조합 효소로 방사능 분석법으로 결정됩니다. 키나아제 반응은 실온(24°C)에서 1시간 동안 수행되며 PBS를 첨가하여 종료됩니다. IC50 값은 이어서 시그모이드 용량-반응 곡선 적합(가변 기울기)을 사용하여 결정됩니다. CK2 및 GSK3β (glycogen synthase kinase 3β) 억제는 키나아제 선택성 스크리닝에 의해 확립됩니다. 이 화합물은 Upstate 키나아제 패널에 대해 10 μM ATP에서 테스트됩니다.
생체 내(In vivo)	LY294002는 또한 종양 성장 억제 및 세포자멸사 유도를 초래하며, 특히 LoVo 종양에서 그러하고, 따라서 마우스 복막암종 모델에서 현저한 효능을 보입니다. 이 화합물은 난소암의 성장 및 복수 형성을 유의하게 억제합니다.
참조	[1] https://pubmed.ncbi.nlm.nih.gov/17362206/ [2] https://pubmed.ncbi.nlm.nih.gov/12060641/ [3] https://pubmed.ncbi.nlm.nih.gov/10741711/ [4] https://pubmed.ncbi.nlm.nih.gov/17302559/ [5] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1868829/ [6] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3560216/

적용 분야

방법	바이오마커	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

임상시험 정보

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호	모집	조건	스폰서/협력자	시작일	단계
NCT02337309	Terminated	Neuroblastoma	New Approaches to Neuroblastoma Therapy Consortium\|SignalRX Pharmaceuticals Inc.\|University of Southern California	July 9 2015	Phase 1

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자주 묻는 질문

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

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

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

답변:
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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