Ipatasertib (GDC-0068)

別名:RG7440

Ipatasertib (GDC-0068, RG7440) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM in cell-free assays, 620-fold selectivity over PKA. Phase 2.

Ipatasertib (GDC-0068)化学構造

CAS No. 1001264-89-6

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 56700 国内在庫あり
JPY 40500 国内在庫あり
JPY 118500 国内在庫あり
JPY 250500 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
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文献中Selleckの製品使用例(123)

製品安全説明書

現在のバッチを見る: 純度: 99.87%
99.87

Ipatasertib (GDC-0068)関連製品

シグナル伝達経路

Akt阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
PC-3 Growth Inhibition Assay 1/5/10 μM 24/48/72 h dose-dependently increases the G0–G1 phase population  23287563
IGROV-1 Function Assay 0.0038-2.5 μM 1 h induces a dose-dependent increase in Akt phosphorylation at both Thr308 (T308) and Ser473 23287563
BT474M1 Function Assay 0.0038-2.5 μM 1 h induces a dose-dependent increase in Akt phosphorylation at both Thr308 (T308) and Ser473 23287563
PC-3 Function Assay 0.0038-2.5 μM 1 h induces a dose-dependent increase in Akt phosphorylation at both Thr308 (T308) and Ser473 23287563
MDA-MB-468  Growth Inhibition Assay 1 μM 5 d enhances the antiproliferative response 24667376
HCC70  Growth Inhibition Assay 1 μM 5 d enhances the antiproliferative response 24667376
MDA-MB-468  Function Assay 1 μM 24 h increases the abundance of HER3 24667376
HCC70  Function Assay 1 μM 24 h increases the abundance of HER3 and induces the phosphorylation (activation) of both EGFR and HER3 24667376
MCF7-neo/HER2 Growth Inhibition Assay 1/5/10 μM 24/48/72 h dose-dependently increases the G0–G1 phase population  23287563
BT474M1 Growth Inhibition Assay 1/5/10 μM 24/48/72 h dose-dependently increases the G0–G1 phase population  23287563
PC-3 Apoptosis Assay 1/5/10 μM 15/48/72 h causes a dose- and time-dependent increase in apoptotic and necrotic populations 23287563
MCF7-neo/HER2 Apoptosis Assay 1/5/10 μM 15/48/72 h causes a dose- and time-dependent increase in apoptotic and necrotic populations 23287563
BT474M1 Apoptosis Assay 1/5/10 μM 15/48/72 h causes a dose- and time-dependent increase in apoptotic and necrotic populations 23287563
PC3 Function assay 50 mg/kg 9 hrs Plasma concentration in nu/nu mouse xenografted with human PC3 cells at 50 mg/kg, po at 9 hrs by LC/MS/MS analysis, Cp = 0.5 μM. 22934575
PC3 Function assay 50 mg/kg 1 hr Plasma concentration in nu/nu mouse xenografted with human PC3 cells at 50 mg/kg, po at 1 hr by LC/MS/MS analysis, Cp = 7.4 μM. 22934575
PC3 Function assay 100 mg/kg 8 hrs Inhibition of Akt in nu/nu mouse xenografted with human PC3 cells assessed as decrease in tumor p-S6RP level at 100 mg/kg, po at 8 hrs by ELISA relative to total S6RP 22934575
LNCAP Cytotoxicity assay 72 hrs Cytotoxicity against human LNCAP cells assessed as reduction of resazurin to resorufin after 72 hrs, IC50 = 0.095 μM. 22934575
LNCAP Function assay 1.5 hrs Inhibition of Akt1 in human LNCAP cells assessed as phosphorylation of PRAS40 at Thr246 after 1.5 hrs, IC50 = 0.157 μM. 22934575
BT474M1 Cytotoxicity assay 96 hrs Cytotoxicity against human BT474M1 cells assessed as decrease in cell viability after 96 hrs by CellTitre-Glo assay, IC50 = 1 μM. 22934575
PC3 Cytotoxicity assay 96 hrs Cytotoxicity against human PC3 cells assessed as decrease in cell viability after 96 hrs by CellTitre-Glo assay, IC50 = 1 μM. 22934575
MCF7 Cytotoxicity assay 96 hrs Cytotoxicity against human MCF7 cells overexpressing Her2 assessed as decrease in cell viability after 96 hrs by CellTitre-Glo assay, IC50 = 1 μM. 22934575
MCF7 Function assay Inhibition of Akt1-mediated PRAS40 phosphorylation in human MCF7 cells overexpressing Her2 22934575
BT474M1 Function assay Inhibition of Akt1-mediated PRAS40 phosphorylation in human BT474M1 cells 22934575
PC3 Function assay Inhibition of Akt1-mediated PRAS40 phosphorylation in human PC3 cells 22934575
LNCAP Function assay Inhibition of Akt1-mediated PRAS40 phosphorylation in human LNCAP cells 22934575
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
SJ-GBM2 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 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
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生物活性

製品説明 Ipatasertib (GDC-0068, RG7440) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM in cell-free assays, 620-fold selectivity over PKA. Phase 2.
Targets
Akt1 [1]
(Cell-free assay)
Akt3 [1]
(Cell-free assay)
Akt2 [1]
(Cell-free assay)
5 nM 8 nM 18 nM
In Vitro
In vitro

Testing against a broad panel of 230 kinases, GDC-0068 only inhibits 3 kinases by >70% at 1 μM concentration (PRKG1α, PRKG1β, and p70S6K, with IC50 of 98 nM, 69 nM, and 860 nM, respectively). GDC-0068 displays >100-fold selectivity for Akt over PKA with IC50 of 3.1 μM. In LNCaP, PC3 and BT474M1 cells, GDC-0068 treatment inhibits the phosphorylation of the Akt substrate, PRAS40 with IC50 of 157 nM, 197 nM, and 208 nM, respectively. Furthermore, GDC-0068 selectively inhibits cell cycle progression and viability of cancer cell lines driven by Akt signaling, including those with defects in the tumor suppressor PTEN, oncogenic mutations in PIK3CA, and amplification of HER2, with strongest effects in HER2+ and Luminal subtypes. [1-4]

実験結果図 Methods Biomarkers 結果図 PMID
Western blot PUMA p-AKT / AKT / p-FoxO3a / FoxO3a / p-p65 / p65 Noxa / Bid / Bad / Bim / Bcl-2 / Bcl-xl / Mcl-1 cleaved-caspase3 p-PRAS40(T246) / PRAS40 / p-ERK / ERK / pFOXO1 / pFOXO3a / pGSK3b(S9) / pAS160(S318) / pBAD(S136) / pS6 / p4E-BP1 30185800
In Vivo
In Vivo

Oral administration of GDC-0068 in PC3 prostate tumor xenografts model induces down-regulation of p-PRAS40. In BT474-Tr xenografts, GDC-0068 treatment reduces pS6 and peIF4G levels, re-localizes FOXO3a to nucleus, and induces feedback upregulation of HER3 and pERK. Administration of GDC-0068 exhibits potent antitumor efficacy in multiple xenograft tumor models, including the PTEN-deficient prostate cancer models LNCaP and PC3, the PIK3CA H1047R mutant breast cancer model KPL-4, and MCF7-neo/HER2 tumor model. [1-4]

動物実験 動物モデル Female nude mice bearing LNCaP, PC3, KPL-4, or MCF7 tumor xenografts
投与量 ~100 mg/kg/day
投与経路 Orally
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01090960 Completed
Solid Cancers
Genentech Inc.
March 2010 Phase 1

化学情報

分子量 458 化学式

C24H32ClN5O2

CAS No. 1001264-89-6 SDF Download Ipatasertib (GDC-0068) SDFをダウンロードする
Smiles CC1CC(C2=C1C(=NC=N2)N3CCN(CC3)C(=O)C(CNC(C)C)C4=CC=C(C=C4)Cl)O
保管

In vitro
Batch:

DMSO : 91 mg/mL ( (198.68 mM); 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 : 91 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。

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Handling Instructions

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