Inavolisib (GDC-0077)

製品コードS8668 バッチS866808

印刷

化学情報

Synonyms

RG6114, RO-7113755

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₈H₁₉F₂N₅O₄

分子量

407.37

CAS No.

2060571-02-8

Solubility (25°C)*

体外

DMSO

81 mg/mL (198.83 mM)

Water

Insoluble

Ethanol

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	Inavolisib (GDC-0077, RG6114, RO-7113755) is a potent selective inhibitor of PI3K alpha (PI3Kα) with an IC50 of 0.038 nM. GDC-0077 is >300-fold more selective for PI3K alpha over the other class I PI3K isoforms (beta, delta, and gamma) and >2000-fold more selective over PIK family members. GDC-0077 binds to the ATP binding site of PI3K and inhibits the phosphorylation of PIP2 to PIP3.
in vitro	Inavolisib (GDC-0077) potently inhibits mutant PI3K pathway signaling and cell viability through unique HER2-dependent mutant p110a degradation.[2]
in vivo	Inavolisib (GDC-0077) treatment at the MTD in vivo results in tumor regressions in multiple PIK3CA-mutant xenograft and patient-derived xenograft models.[2]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HCC1954 cells, HDQ-P1 cells, SW48 cells, MCF7 cells, HCC202 heterozygous cells
	濃度	10 nM
	反応時間	24 h
	実験の流れ	Inavolisib (GDC-0077) was evaluated using an ATP-based cell viability assay in Colon cancer cell lines. Western blot analysis measured p110a protein levels and pAKT signaling in these cell lines treated with it for gradient concentrations over 24 hours.
動物実験	動物モデル	Female NCR nude mice inoculated with HCC1954 tumor cells, female NOD-SCID gamma mice inoculated with WHIM20 tumor cells, female NOD-SCID gamma mice inoculated with HCI-003 tumor cells
	投薬量	25 mg/kg
	投与方法	Oral gavage

参考

https://cancerres.aacrjournals.org/content/78/4_Supplement/PD4-14
https://pubmed.ncbi.nlm.nih.gov/34544753/

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：

A patient-derived T cell lymphoma biorepository uncovers pathogenetic mechanisms and host-related therapeutic vulnerabilities [ Cell Rep Med, 2025, S2666-3791(25)00102-8]	PubMed: 40147445
Functional Analysis of the PI3K/AKT/mTOR Pathway Inhibitor, Gedatolisib, Plus Fulvestrant with and Without Palbociclib in Breast Cancer Models [ Int J Mol Sci, 2025, 26(12)5844]	PubMed: 40565304
AKT and EZH2 inhibitors kill TNBCs by hijacking mechanisms of involution [ Nature, 2024, 10.1038/s41586-024-08031-6]	PubMed: 39385030
Functional Assessments of Gynecologic Cancer Models Highlight Differences Between Single-Node Inhibitors of the PI3K/AKT/mTOR Pathway and a Pan-PI3K/mTOR Inhibitor, Gedatolisib [ Cancers (Basel), 2024, 16(20)3520]	PubMed: 39456616
The Oncogenic PI3K-Induced Transcriptomic Landscape Reveals Key Functions in Splicing and Gene Expression Regulation [ Cancer Res, 2022, 82(12):2269-2280]	PubMed: 35442400
PI3K inhibitors in trastuzumab-resistant HER2-positive breast cancer cells with PI3K pathway alterations [ Am J Cancer Res, 2022, 12(7):3067-3082]	PubMed: 35968355

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。