umbralisib (TGR-1202)

製品コードS8194 バッチS819403

印刷

化学情報

Synonyms

Rp-5264

Storage
(From the date of receipt)

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

化学式

C₃₁H₂₄F₃N₅O₃

分子量

571.55

CAS No.

1532533-67-7

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

100 mg/mL (174.96 mM)

Ethanol (warmed with 50ºC water bath)

6 mg/mL (10.49 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.
Clear solution	2%DMSO 1 30%PEG300 2 2%Tween80 3 66%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。	3.000mg/ml (5.25mM)	Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clarified DMSO stock solution to 300 μL of PEG300, mix evenly to clarify it; add 20 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 660 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	次世代PI3Kδ阻害剤であるumbralisib (TGR-1202, Rp-5264) は、酵素および細胞ベースのアッセイにおいて、それぞれ22.2 nMおよび24.3 nMのIC50およびEC50値でPI3Kδ活性を阻害します。
in vitro	The compound displays a high degree of selectivity over the alpha (>1000 fold), beta (>30-50 fold), and gamma (>15-50 fold) isoforms. Additionally, the compound causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM. Treatment of PBMC with RP5264 results initially in a G2/M arrest followed by subsequent increase in the number of Sub G0 cells. Viability assays demonstrate that the compound causes a significant inhibition in growth as well as Akt phosphorylation of immortalized and primary leukemic cells.
in vivo	The compound exhibits good oral absorption with favourable pharmacokinetic properties in rodents. It also has an excellent safety profile.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Multiple Myeloma resistant (MM-1R) or sensitive (MM-1S) cells
	濃度	--
	反応時間	96 h
	実験の流れ	Multiple Myeloma resistant (MM-1R) or sensitive (MM-1S) cells are incubated with desired concentrations of RP5264. Growth is assessed after 96 h by a MTT assay.
動物実験	動物モデル	Female Balb/c mice
	投薬量	12.5, 25, 50 mg/kg
	投与方法	oral administration

参考

http://www.tgtxinc.com/AACR2012Poster3741.pdf

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
Targeting IRAK4 with Emavusertib in Lymphoma Models with Secondary Resistance to PI3K and BTK Inhibitors [ J Clin Med, 2023, 12(2)399]	PubMed: 36675328
Využití vybraných inhibitorů k překonání anthracyklinové rezistence v terapii nádorových onemocnění (in vitro studie). [ Charles University, 2023, ]	PubMed: None
Functional Testing to Characterize and Stratify PI3K Inhibitor Responses in Chronic Lymphocytic Leukemia [ Clin Cancer Res, 2022, 28-20:4444-4455]	PubMed: 35998013
Resistance to PI3κδ inhibitors in marginal zone lymphoma can be reverted by targeting the IL-6/PDGFRA axis [ Haematologica, 2022, 10.3324/haematol.2021.279957]	PubMed: 35484662
The delta isoform of PI3K predominates in chronic myelomonocytic leukemia and can be targeted effectively with umbralisib and ruxolitinib [ Exp Hematol, 2021, S0301-472X(21)00089-8]	PubMed: 33617893
Ex vivo blockade of PI3K gamma or delta signaling enhances the antitumor potency of adoptively transferred CD8+ T cells. [ Eur J Immunol, 2020, 8]	PubMed: 32383488

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。