Duvelisib (IPI-145)

製品コードS7028 バッチS702804

印刷

化学情報

Synonyms

INK1197

Storage
(From the date of receipt)

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

化学式

C₂₂H₁₇ClN₆O

分子量

416.86

CAS No.

1201438-56-3

Solubility (25°C)*

体外

DMSO

83 mg/mL (199.1 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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	10.000mg/ml (23.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 200 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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	Duvelisib (IPI-145, INK1197) is a novel and selective PI3K δ/γ inhibitor with K_i and IC50 of 23 pM/243 pM and 1 nM/50 nM in cell-free assays, highly selective for PI3K δ/γ than other protein kinases. Phase 3.
in vitro	Duvelisib (IPI-145) suppresses murine/human B-cell proliferation with EC50 of 0.5 nM/0.5 nM and also inhibits human T-cell proliferation with EC50 of 9.5 nM. ^[1]
in vivo	Duvelisib (IPI-145) (10 mg/kg, p.o.) shows well pharmacokinetics with C_max and AUC of 390 ng/mL and 137 ng•h/mL in mouse and rat. It (10 mg/kg) is active in murine DTH model with ~50% ear swelling. This compound (10 mg/kg) demonstrates dose-dependent effect in rat collagen induced arthritis (CIA) model. It prevents inflammation and protects joint bone and cartilage in the rat CIA model. IPI-145 (10 mg/kg,QD) demonstrates activity in rat adjuvant induced polyarthritis model. ^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	AML cell lines
	濃度	10 μM
	反応時間	72 h
	実験の流れ	AML cell lines were treated with 10 μM of this compound and cultured for 72 hours.
動物実験	動物モデル	Brown Norway rats
	投薬量	(0.1, 0.3, 1, or 10 mg/kg
	投与方法	p.o.

参考

http://infi.com/pdfs/palombella_nyas_2012.pdf
https://pubmed.ncbi.nlm.nih.gov/27174919/
https://pubmed.ncbi.nlm.nih.gov/24211136/

カスタマーフィードバック

: , , Dr. Antonino Maria Spartà from University of Bolog

: Data from [Data independently produced by , , Leukemia, 2018, 32(9):1958-1969]

: Data from [Data independently produced by , , Blood Cancer J, 2017, 7(3):e539]

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
Complementary approaches define the metabolic features that accompany Richter syndrome transformation [ Cell Mol Life Sci, 2025, 82(1):152]	PubMed: 40204982
Granuloma Dual RNA-Seq Reveals Composite Transcriptional Programs Driven by Neutrophils and Necrosis within Tuberculous Granulomas [ bioRxiv, 2025, 2025.04.26.650783]	PubMed: 40391323
Genomic and transcriptomic profiling of peripheral T cell lymphoma reveals distinct molecular and microenvironment subtypes [ Cell Rep Med, 2024, 5(2):101416]	PubMed: 38350451
Longitudinal phosphoproteomics reveals the PI3K-PAK1 axis as a potential target for recurrent colorectal liver metastases [ Cell Rep, 2024, 43(12):115061]	PubMed: 39689713
A molecular circuit linking the BCR to the NAD biosynthetic enzyme NAMPT is an actionable target in Richter syndrome [ Blood Adv, 2024, 8(8):1920-1933]	PubMed: 38359376
Patient-derived rhabdomyosarcoma cells recapitulate the genetic and transcriptomic landscapes of primary tumors [ iScience, 2024, 27(10):110862]	PubMed: 39319271
Dual inhibition of phosphoinositide 3-kinases delta and gamma reduces chronic B cell activation and autoantibody production in a mouse model of lupus [ Front Immunol, 2023, 14:1115244]	PubMed: 37234154
Dual inhibition of phosphoinositide 3-kinases delta and gamma reduces chronic B cell activation and autoantibody production in a mouse model of lupus [ Front Immunol, 2023, 14:1115244]	PubMed: 37234154
Selective Inhibition of PI3K Isoforms in Brain Tumors Suppresses Tumor Growth by Increasing Radiosensitivity [ Yonsei Med J, 2023, 64(2):139-147]	PubMed: 36719022

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。