ホームページ Apoptosis p53 activator - E3 Ligase inhibitor RITA For research use only.

RITA

別名：NSC 652287

RITA induces both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks, and also inhibits MDM2-p53 interaction by targeting p53.

RITA化学構造

CAS No. 213261-59-7

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 37000 国内在庫あり
JPY 25500 国内在庫あり
JPY 40500 国内在庫あり
JPY 145500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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製品安全説明書

現在のバッチを見る： S278101 DMSO] 58 mg/mL] false] Ethanol] 8 mg/mL] false] Water] Insoluble] false 純度： 99.93%
99.93

RITA関連製品

シグナル伝達経路

p53 Signaling Pathways

p53シグナル伝達経路

p53阻害剤の選択性比較

生物活性

製品説明 RITA induces both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks, and also inhibits MDM2-p53 interaction by targeting p53.
特性 Inducer of DNA cross-links, not a DNA intercalator.
Targets
Mdm2 [1] p53 [3]
In Vitro
In vitro RITA shows a highly selective pattern of differential cytotoxic activity in the tumor cell lines, due to cellular accumulation to the cytosolic (S100) fraction. RITA also inhibits the growth of other renal cell lines including ACHN and UO-31 with IC50 of 13 μM and 37 μM, respectively. [1] RITA (10 nM) causes cell cycle arrest with accumulation of cells at the G2-M phase and induces DNA fragmentation and apoptosis at 100 nM, both with evaluated p53 protein levels. RITA (30 nM) also induces both DNA-protein and DNA-DNA cross-links in A498 cells. Meanwhile RITA has no effects on top1-mediated relaxation of supercoiled SV40 DNA. [2] RITA significantly suppresses the growth of HCT116 cells (97%) but only slightly inhibits the growth of HCT116 TP53-/- cells (13%). RITA is much more efficient at growth suppression in wild-type p53-expressing tumor cell lines than in cell lines lacking p53 and those expressing mutant p53. RITA binds full-length p53 but not glutathione S-transferase (GST) protein or HDM-2 (a key regulator of p53 is strongly supported by the rescue of embryonic lethality of MDM2). RITA blocks p53−HDM-2 interaction and p53 ubiquitination. RITA substantially decreases the amount of HDM-2 that is co-precipitated with p53, although both proteins are upregulated. RITA prevents interactions between the purified GST-p53 and 6XHis-tagged His-HDM-2 proteins. [3] RITA is shown to induce apoptosis by promoting p53Ser46 phosphorylation. [4] RITA induces activation of p53 in conjunction with up-regulation of phosphorylated ASK-1, MKK-4 and c-Jun. RITA induces the activation of JNK signaling. [5] But On the contrary, another results by nuclear magnetic resonance (NMR) show that RITA does not block the formation of the complex between p53 (residues 1-312) and the N-terminal p53-binding domain of MDM2 (residues 1-118), which is highly probable that the binding of RITA requires native conformation of p53. [6]
細胞実験 細胞株 HCT116 cells and HCT116 TP53-/- cells
濃度 0.1 nM - 1 mM, 10 mM stocked in DMSO
反応時間 48 hours
実験の流れ Examination to assess susceptibility of cells to RITA (0.1 nM - 1 mM) is done using the XTT assay. Cells are inoculated into 96-well flat-bottom plates at a density of 1500 cells per well and incubated for 24 hours at 37 °C in a humidified 5% CO2 5% air atmosphere. Serial concentrations of RITA in DMSO are added to the wells, and sensitivity is determined 48 hours after the addition of RIT
In Vivo
In Vivo RITA is well tolerated in mice after intraperitoneal administration, with no observable weight loss at doses up to 10 mg/kg during 1 month. After five injections of 0.1 mg/kg of RITA, the growth of the HCT116 tumors is suppressed by 40%, without apparent effects on the HCT116 TP53-/- tumors. At a dose of 1 or 10 mg/kg, RITA shows strong antitumor activity. Five 1 mg/kg injections of RITA results in a more than twofold decrease in the growth rate of p53-positive xenografts without any effect on p53-null xenografts. HCT116 tumors are 90% smaller in mice treated with 10 mg/kg of RITA than in control untreated mice. RITA inhibits the tumor growth in a wild-type p53−dependent manner. [3]
動物実験 動物モデル SCID mice carrying HCT116 and HCT116 TP53-/- xenografts
投与量 0.1 mg/kg, 1 mg/kg or 10 mg/kg
投与経路 Administered via i.v. or i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05260203 Completed
Multiple Myeloma|Solitary Plasmacytoma|Amyloidosis|Chronic Myeloid Leukemia|Chronic Lymphocytic Leukemia|T Cell Non-Hodgkin Lymphoma|Lymphocytic Lymphoma|Hodgkin Lymphoma|B-cell Non Hodgkin Lymphoma|Acute Myeloid Leukemia|Myelodysplasia|Chronic Myeloproliferative Disorder|Treatment Adherence|Treatment Adherence and Compliance
Advice Pharma Group srl
 June 4 2022 Not Applicable
NCT05153551 Completed
Autism Spectrum Disorder
University of Michigan|Blue Cross Blue Shield of Michigan Foundation
 January 27 2022 Not Applicable
NCT03806127 Completed
Irritable Bowel Syndrome
Urovant Sciences GmbH
 December 31 2018 Phase 2
NCT00779025 Completed
Coitus
Johnson & Johnson Consumer and Personal Products Worldwide
 January 2008 Not Applicable

化学情報

分子量 292.37 化学式

C14H12O3S2
CAS No. 213261-59-7 SDF Download RITA SDFをダウンロードする
Smiles C1=C(SC(=C1)C2=CC=C(O2)C3=CC=C(S3)CO)CO
保管

In vitro
Batch:

DMSO : 58 mg/mL ( (198.37 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 8 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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