Ipatasertib (GDC-0068)

製品コードS2808 バッチS280806

印刷

化学情報

Synonyms

RG7440

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₄H₃₂ClN₅O₂

分子量

458

CAS No.

1001264-89-6

Solubility (25°C)*

体外

DMSO

92 mg/mL (200.87 mM)

Ethanol

92 mg/mL (200.87 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

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.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

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.
in vitro	Ipatasertib (GDC-0068) was tested against a broad panel of 230 kinases, and it 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). This compound displays >100-fold selectivity for Akt over PKA with IC50 of 3.1 μM. In LNCaP, PC3 and BT474M1 cells, it inhibits the phosphorylation of the Akt substrate, PRAS40 with IC50 of 157 nM, 197 nM, and 208 nM, respectively. Furthermore, it 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]
in vivo	Oral administration of Ipatasertib (GDC-0068) in PC3 prostate tumor xenografts model induces down-regulation of p-PRAS40. In BT474-Tr xenografts, this compound treatment reduces pS6 and peIF4G levels, re-localizes FOXO3a to nucleus, and induces feedback upregulation of HER3 and pERK. It 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]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	PC3 cells
	濃度
	反応時間	1 h
	実験の流れ	Cells were treated with various concentrations of this compound.
動物実験	動物モデル	Female nude mice bearing LNCaP, PC3, KPL-4, or MCF7 tumor xenografts
	投薬量	~100 mg/kg/day
	投与方法	Orally

参考

http://cancerres.aacrjournals.org/cgi/content/meeting_abstract/71/8_MeetingAbstracts/DDT02-01?sid=e2
http://www.arraybiopharma.com/_documents/Publication/PubAttachment478.pdf
http://www.arraybiopharma.com/_documents/Publication/PubAttachment437.pdf

http://cancerres.aacrjournals.org/cgi/content/short/72/8_MeetingAbstracts/966?rss=1
http://www.arraybiopharma.com/_documents/Publication/PubAttachment524.pdf
https://pubmed.ncbi.nlm.nih.gov/23287563/

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カスタマーフィードバック

: Data from [Data independently produced by , , Cell, 2015, 160(1-2): 161-76 ]

: Data from [Data independently produced by , , Clin Cancer Res, 2018, 78(7):1657-1671]

: Data from [Data independently produced by , , Neoplasia, 2017, 19(4):310-320]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

KBTBD11 loss promotes AKT hyperactivation and therapeutic vulnerability in prostate cancer [ Oncogene, 2025, 44(44):4324-4337]	PubMed: 40983636
JAK2 Inhibition Augments the Anti-Proliferation Effects by AKT and MEK Inhibition in Triple-Negative Breast Cancer Cells [ Int J Mol Sci, 2025, 26(13)6139]	PubMed: 40649917
UBE2S inhibits colorectal cancer proliferation by regulating the PI3K/AKT and MAPK/ERK pathways via TRAF6 [ Sci Rep, 2025, 15(1):35610]	PubMed: 41083491
Development of Acquired Resistance in Alpelisib-treated Gastric Cancer Cells With PIK3CA Mutations and Overcoming Strategies [ Anticancer Res, 2025, 45(5):1877-1896]	PubMed: 40295072
The glycosyltransferase ALG3 is an AKT substrate that regulates protein N-glycosylation [ bioRxiv, 2025, 2025.04.01.646556]	PubMed: 40236010
AKT and EZH2 inhibitors kill TNBCs by hijacking mechanisms of involution [ Nature, 2024, 10.1038/s41586-024-08031-6]	PubMed: 39385030
Arachidonic acid released by PIK3CA mutant tumor cells triggers malignant transformation of colonic epithelium by inducing chromatin remodeling [ Cell Rep Med, 2024, S2666-3791(24)00179-4]	PubMed: 38614093
Combined inhibition of CDK4/6 and AKT is highly effective against the luminal androgen receptor (LAR) subtype of triple negative breast cancer [ Cancer Lett, 2024, 604:217219]	PubMed: 39244005
Assessments of prostate cancer cell functions highlight differences between a pan-PI3K/mTOR inhibitor, gedatolisib, and single-node inhibitors of the PI3K/AKT/mTOR pathway [ Mol Oncol, 2024, 10.1002/1878-0261.13703]	PubMed: 39092562
Increased mTOR activity and RICTOR copy number in small cell lung carcinoma progression [ Eur J Cell Biol, 2024, 103(4):151468]	PubMed: 39571513

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。