Ipatasertib (GDC-0068)

別名: RG7440

目錄號(hào)：S2808 Purity: 99.87%

Ipatasertib (GDC-0068, RG7440)是一種高選擇性的pan-Akt抑制劑，靶向作用于Akt1/2/3，在無細(xì)胞試驗(yàn)中IC50為5 nM/18 nM/8 nM，比作用于PKA選擇性高620倍。Phase 2。

Ipatasertib (GDC-0068) Chemical Structure

CAS: 1001264-89-6

規(guī)格	價(jià)格	庫存
10mM (1mL in DMSO)	1392.3	現(xiàn)貨
5mg	1203.93	現(xiàn)貨
25mg	3595.41	現(xiàn)貨
50mg	5708.43	現(xiàn)貨
100mg	9148.23	現(xiàn)貨
更大包裝有超大折扣
400-668-6834 info@selleck.cn

產(chǎn)品質(zhì)控

批次：純度： 99.87%

99.87

常與Ipatasertib (GDC-0068)一起在實(shí)驗(yàn)中被使用的化合物

Paclitaxel

Ipatasertiba與Paclitaxel聯(lián)用具有更強(qiáng)的降低HEC-1A和ECC-1細(xì)胞中Bcl-xL表達(dá)的能力。

Palbociclib

Ipatasertib和Palbociclib組合使用在患者來源的腫瘤異種移植模型TMA-027中顯示出顯著延遲的腫瘤生長(zhǎng)。

Kase AM, et al. Journal of Clinical Oncology 40, no. 6_suppl (February 20, 2022) 176-176.

Carboplatin

Ipatasertib和Carboplatin聯(lián)合使用可顯著抑制ARK-1和SPEC-2細(xì)胞中的細(xì)胞增殖并降低Bcl-XL和MCL-1的表達(dá)。

Burkett WC, et al. Ann Med. 2023 Dec;55(1):603-614.

Erdafitinib

Ipatasertib和Erdafitinib聯(lián)合治療可協(xié)同抑制細(xì)胞增殖并誘導(dǎo)膀胱癌(BC)細(xì)胞死亡。

Hu C, et al. Biochem Biophys Res Commun. 2022 May 14;604:165-171.

Bevacizumab (anti-VEGF)

Ipatasertib和Bevacizumab聯(lián)合使用可減少子宮內(nèi)膜樣子宮內(nèi)膜癌(EC)轉(zhuǎn)基因小鼠模型中的腫瘤生長(zhǎng)。

Newton M, et al. Gynecologic Oncology 166 (2022): S31.

Ipatasertib (GDC-0068)相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	Akt1 Akt2 Akt3	點(diǎn)擊展開
相關(guān)產(chǎn)品	MK-2206 2HCl Perifosine SC79 Capivasertib (AZD5363) GSK690693 Triciribine (API-2) CCT128930 Afuresertib (GSK2110183) A-674563 HCl AT7867 Oridonin Akti-1/2 PHT-427 TIC10 (ONC201) Miransertib (ARQ 092) HCl AT13148 Uprosertib (GSK2141795) Miransertib (ARQ-092) SC66 Deguelin ML-9 HCl	點(diǎn)擊展開
相關(guān)化合物庫	激酶抑制劑庫 PI3K/Akt 抑制劑庫凋亡分子化合物庫細(xì)胞周期化合物庫 NF-κB信號(hào)通路庫	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息
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
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點(diǎn)

Akt1 ^[1] (Cell-free assay)	Akt3 ^[1] (Cell-free assay)	Akt2 ^[1] (Cell-free assay)
5 nM	8 nM	18 nM

體外研究(In Vitro)
體外研究活性	對(duì)一大組230種激酶測(cè)試，GDC-0068只抑制3種激酶，濃度為 1 μM 時(shí)抑制70%以上,(抑制PRKG1α,PRKG1β,和p70S6K時(shí), IC50分別為98 nM, 69 nM, 和 860 nM)。GDC-0068 作用于Akt比作用于PKA 選擇性高100倍以上，抑制Akt時(shí) IC50為3.1 μM。GDC-0068處理LNCaP, PC3 和 BT474M1 細(xì)胞,抑制Akt底物PRAS40磷酸化,IC50分別為157 nM, 197 nM, 和208 nM。而且, GDC-0068選擇性抑制細(xì)胞周期進(jìn)展和Akt信號(hào)驅(qū)動(dòng)的癌細(xì)胞活力, 包括腫瘤抑制基因PTEN缺陷,PIK3CA致癌基因突變, 和HER2擴(kuò)增,在HER2⁺和Luminal 亞型中作用效果最強(qiáng)。^[1-4]
實(shí)驗(yàn)圖片	檢測(cè)方法	檢測(cè)指標(biāo)	實(shí)驗(yàn)圖片	PMID
實(shí)驗(yàn)圖片	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

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	GDC-0068口服處理給藥PC3前列腺移植瘤模型，誘導(dǎo)p-PRAS40下調(diào)。GDC-0068 處理BT474-Tr移植瘤,降低 pS6 和 peIF4G 水平,重新定位FOXO3a到細(xì)胞核,且誘導(dǎo) HER3 和pERK的反饋上調(diào)。GDC-0068 處理多種移植瘤模型，具有有效抗癌活性，包括PTEN-缺陷的前列腺癌模型LNCaP 和 PC3, PIK3CA H1047R 突變的乳腺癌模型 KPL-4, 和 MCF7-neo/HER2腫瘤模型。^[1-4]
動(dòng)物實(shí)驗(yàn)	Animal Models	攜帶LNCaP, PC3, KPL-4, 或MCF7移植瘤的雌性裸鼠
	Dosages	~100 mg/kg/day
	Administration	口服處理

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT01090960	Completed	Solid Cancers	Genentech Inc.	March 2010	Phase 1

參考文獻(xiàn)
[1] Lin K. Cancer Res, 2011, 71(8 Supplement), abstract DDT02-01. [2] James F. Blake. 2011. [3] Tabernero J, et al. Ann Oncol, 2011, 22(suppl 3), abstract IL33. [4] Heidi M. Savage, et al. Cancer Res, 2012, 72(8 Supplement), 966. [5] Roel Funke, et al. American Society of Clinical Oncology (ASCO) Annual Meeting, 1-5, 2012. [6] Lin J, et al. Clin Cancer Res.?2013 Apr 1;19(7):1760-72. + 展開

參考文獻(xiàn)

[1] Lin K. Cancer Res, 2011, 71(8 Supplement), abstract DDT02-01.
[2] James F. Blake. 2011.
[3] Tabernero J, et al. Ann Oncol, 2011, 22(suppl 3), abstract IL33.

[4] Heidi M. Savage, et al. Cancer Res, 2012, 72(8 Supplement), 966.
[5] Roel Funke, et al. American Society of Clinical Oncology (ASCO) Annual Meeting, 1-5, 2012.
[6] Lin J, et al. Clin Cancer Res.?2013 Apr 1;19(7):1760-72.

+ 展開

化學(xué)信息&溶解度

分子量	458	分子式	C₂₄H₃₂ClN₅O₂
CAS號(hào)	1001264-89-6	SDF	Download Ipatasertib (GDC-0068) SDF
Smiles	CC1CC(C2=C1C(=NC=N2)N3CCN(CC3)C(=O)C(CNC(C)C)C4=CC=C(C=C4)Cl)O
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 91 mg/mL ( (198.68 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 91 mg/mL (198.68 mM)

Water : Insoluble

DMSO : 92 mg/mL ( (200.87 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 92 mg/mL (200.87 mM)

Water : 10 mg/mL (21.83 mM)

DMSO : 92 mg/mL ( (200.87 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 92 mg/mL (200.87 mM)

Water : Insoluble

DMSO : 92 mg/mL ( (200.87 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 92 mg/mL (200.87 mM)

Water : Insoluble

DMSO : 92 mg/mL ( (200.87 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 92 mg/mL (200.87 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

技術(shù)支持

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* 必填項(xiàng)

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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Ipatasertib (GDC-0068)

產(chǎn)品質(zhì)控

常與Ipatasertib (GDC-0068)一起在實(shí)驗(yàn)中被使用的化合物

Ipatasertib (GDC-0068)相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

生物活性

化學(xué)信息&溶解度

實(shí)驗(yàn)計(jì)算

技術(shù)支持