Idasanutlin (RG7388)

製品コードS7205 バッチS720504

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

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

化学式

C₃₁H₂₉Cl₂F₂N₃O₄

分子量

616.48

CAS No.

1229705-06-9

Solubility (25°C)*

体外

DMSO

100 mg/mL (162.21 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。	1.250mg/ml (2.03mM)	Taking the 1 mL working solution as an example, add 50 μL 25 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL 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	Idasanutlin (RG7388) is a potent and selective p53-MDM2 inhibitor with IC50 of 6 nM showing improved in vitro binding as well as cellular potency/selectivity.
in vitro	Idasanutlin (RG7388) inhibits cell proliferation with IC50 of 30 nM, and it induces dose-dependent p53 stabilization, cell cycle arrest, as well as cell apoptosis in cancer cells expressing wild-type p53. ^[1]
in vivo	In a mouse SJSA human osteosarcoma xenograft model, Idasanutlin (RG7388) (25 mg/kg p.o.) causes tumor growth inhibition and regression. ^[1] In a SJSA xenograft model, this compound results in induction of apoptosis and antiproliferation. ^[2]

プロトコル(参考用のみ)

キナーゼアッセイ	Biochemical Binding Affinity – HTRF Assay
キナーゼアッセイ	The p53-MDM2 HTRF assay is performed in buffer containing 50 mM Tris-HCl, pH 7.4, 100 mM NaCl, 1 mM DTT, 0.02 or 0.2 mg/ml BSA. Idasanutlin (RG7388) is stored in aliquots as a 10 mM stock solution in DMSO at 4°C in 96-deep-well plates. It is thawed and mixed immediately prior to testing. This compound is incubated with GST-MDM2 and a biotinylated p53 peptide for one hour at 37°C. Phycolink goat anti-GST (Type 1) allophycocyanin and Eu-8044-streptavidin are then added and followed by one hour incubation at room temperature. Plates are read using the Envision fluorescence reader. IC50 values are determined from inter-plate duplicate or triplicate sets of data. Data are analyzed by XLfit4 (Microsoft) using a 4 Parameter Logistic Model (Sigmoidal Dose-Response Model) and the equation Y= (A+ ((B-A)/ (1+ ((C/x)^D)))), where A and B are enzyme activity in the absence or presence of infinite inhibitor compound, respectively, C is the IC50 and D is the Hill coefficient.
細胞アッセイ	細胞株	wt-p53 cancer cell lines (SJSA1, RKO, HCT116)
	濃度	~10 μM
	反応時間	24 hours
	実験の流れ	Idasanutlin (RG7388) is evaluated for cell proliferation by the tetrazolium dye assay. The concentration at which 50% inhibition (IC50) or 90% inhibition (IC90) of cell proliferation is determined from the linear regression of a plot of the logarithm of the concentration versus percent inhibition.
動物実験	動物モデル	Mice bearing SJSA human osteosarcoma xenografts
	投薬量	~50 mg/kg daily
	投与方法	p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/23808545/
https://pubmed.ncbi.nlm.nih.gov/24812409/

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：

p53 enhances DNA repair and suppresses cytoplasmic chromatin fragments and inflammation in senescent cells [ Nat Commun, 2025, 16(1):2229]	PubMed: 40044657
The Prolonged Half-Life of the p53 Missense Variant R248Q Promotes Accumulation and Heterotetramer Formation with Wildtype p53 to Exert the Dominant-Negative Effect [ Cancer Res, 2025, 10.1158/0008-5472.CAN-24-1136]	PubMed: 40163352
Downregulation of rRNA synthesis by BCL-2 induces chemoresistance in diffuse large B cell lymphoma [ iScience, 2025, 28(5):112333]	PubMed: 40276769
Adipocyte p53 coordinates the response to intermittent fasting by regulating adipose tissue immune cell landscape [ Nat Commun, 2024, 15(1):1391]	PubMed: 38360943
Synthetic lethality of combined ULK1 defection and p53 restoration induce pyroptosis by directly upregulating GSDME transcription and cleavage activation through ROS/NLRP3 signaling [ J Exp Clin Cancer Res, 2024, 43(1):248]	PubMed: 39215364
Small molecule NMD and MDM2 inhibitors synergistically trigger apoptosis in HeLa cells [ Mol Cells, 2024, 47(7):100079]	PubMed: 38871298
miR-16-5p enhances sensitivity to RG7388 through targeting PPM1D expression (WIP1) in Childhood Acute Lymphoblastic Leukemia [ Cancer Drug Resist, 2023, 6(2):242-256]	PubMed: 37457129
miR-16-5p enhances sensitivity to RG7388 through targeting PPM1D expression (WIP1) in Childhood Acute Lymphoblastic Leukemia [ Cancer Drug Resist, 2023, 6(2):242-256]	PubMed: 37457129
Genome-wide CRISPR/Cas9 screening for therapeutic targets in NSCLC carrying wild-type TP53 and receptor tyrosine kinase genes [ Clin Transl Med, 2022, 12(6):e882]	PubMed: 35692096
Epstein Barr virus-positive B-cell lymphoma is highly vulnerable to MDM2 inhibitors in vivo [ Blood Adv, 2022, 6(3):891-901]	PubMed: 34861697

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。