Lirametostat (CPI-1205)

製品コードS8353 バッチS835301

印刷

化学情報

Synonyms

CPI 1205, CPI1205

Storage
(From the date of receipt)

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

化学式

C₂₇H₃₃F₃N₄O₃

分子量

518.57

CAS No.

1621862-70-1

Solubility (25°C)*

体外

DMSO

100 mg/mL (192.83 mM)

Ethanol

100 mg/mL (192.83 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	Lirametostat (CPI-1205) is an orally available selective inhibitor of the histone lysine methyltransferase EZH2, with potential antineoplastic activity.
in vitro	Treatment with Lirametostat (CPI-1205), an EZH2 inhibitor, causes apoptosis in multiple myeloma and plasmacytoma cell models^[2].
in vivo	Lirametostat (CPI-1205) shows excellent oral bioavailability and was well-tolerated for repeat dosing as demonstrated by the absence of significant body weight loss. It shows relatively high clearance in both rats and dogs (3.19 L/h/kg and 1.41 L/h/kg, respectively) but demonstrates good oral bioavailability in both species(44.6% F in rats and 46.2% F in dogs). This compound was well-tolerated in the 28-day GLP toxicology studies, and any findings were reversible over the recovery period^[1].

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Cell-free assays
	濃度	0.002 μM
	反応時間
	実験の流れ
動物実験	動物モデル	CB-17 SCID mice
	投薬量	160 mg/kg orally twice daily
	投与方法	p.o

参考

https://pubmed.ncbi.nlm.nih.gov/27739677/
http://www.bloodjournal.org/content/128/22/5672?sso-checked=true

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：

Select EZH2 inhibitors enhance viral mimicry effects of DNMT inhibition through a mechanism involving NFAT:AP-1 signaling [ Sci Adv, 2024, 10(13):eadk4423]	PubMed: 38536911
ARID1A-deficient bladder cancer is dependent on PI3K signaling and sensitive to EZH2 and PI3K inhibitors [ JCI Insight, 2022, e155899]	PubMed: 35852858
Intrinsic immunogenicity of small cell lung carcinoma revealed by its cellular plasticity [ Cancer Discov, 2021, candisc.0913.2020]	PubMed: 33707236
Multi-omics analysis identifies therapeutic vulnerabilities in triple-negative breast cancer subtypes [ Nat Commun, 2021, 12(1):6276]	PubMed: 34725325
Druggable epigenetic suppression of interferon-induced chemokine expression linked to MYCN amplification in neuroblastoma [ J Immunother Cancer, 2021, 9(5)e001335]	PubMed: 34016720
EZH2 presents a therapeutic target for neuroendocrine tumors of the small intestine [ Sci Rep, 2021, 11(1):22733]	PubMed: 34815475
Multiple pharmacological inhibitors targeting the epigenetic suppressor enhancer of Zeste homolog 2 (EZH2) accelerate osteoblast differentiation [ Bone, 2021, S8756-3282(21)00155-1]	PubMed: 33940225
Precision Targeting with EZH2 and HDAC Inhibitors in Epigenetically Dysregulated Lymphomas [ Clin Cancer Res, 2019, 10.1158/1078-0432]	PubMed: 30979734
Precision Targeting with EZH2 and HDAC Inhibitors in Epigenetically Dysregulated Lymphomas [ Clin Cancer Res, 2019, 25(17):5271-5283]	PubMed: 30979734
Precision Targeting with EZH2 and HDAC Inhibitors in Epigenetically Dysregulated Lymphomas [ American Association for Cancer Research, 2019, 10.1158/1078-0432.CCR-18-3989]	PubMed: None

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。