ホームページ Cell Cycle BMI-1 inhibitor PTC-209 For research use only.

PTC-209

PTC-209 is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM in HEK293T cell line, and results in irreversible reduction of cancer-initiating cells (CICs).

PTC-209化学構造

CAS No. 315704-66-6

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 53800 国内在庫あり
JPY 22000 国内在庫あり
JPY 37000 国内在庫あり

代表番号: 045-509-1970|電子メール：[email protected]
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文献中Selleckの製品使用例（24）

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製品安全説明書

現在のバッチを見る： S737201 DMSO] 99 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false 純度： 99.99%
99.99

PTC-209関連製品

BMI-1阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
HCT116 Function assay 0.1 to 0.4 uM 7 days Inhibition of colony formation in human HCT116 cells at 0.1 to 0.4 uM after 7 days by crystal violet staining based assay 30429953
HCT116 Antitumor assay 10 mg/kg/day 18 days Antitumor activity against human HCT116 cells xenografted in nude mouse assessed as tumor growth inhibition at 10 mg/kg/day, ip for 18 days 30429953
HCT116 Antitumor assay 10 mg/kg/day 18 days Antitumor activity against human HCT116 cells xenografted in nude mouse assessed as reduction in Ki67 expression in tumor at 10 mg/kg/day, ip for 18 days by IHC analysis 30429953
HCT116 Function assay 10 mg/kg/day 18 days Decrease in Bmi1 expression in tumors of nude mouse xenografted with human HCT116 cells at 10 mg/kg/day, ip for 18 days by IHC analysis 30429953
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells after 72 hrs by SRB assay, IC50 = 0.00065 μM. 30429953
HCT8 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT8 cells after 72 hrs by SRB assay, IC50 = 0.59 μM. 30429953
HT-29 Antiproliferative assay 72 hrs Antiproliferative activity against human HT-29 cells after 72 hrs by SRB assay, IC50 = 0.61 μM. 30429953
HCT116 Function assay 8 hrs Inhibition of Bmi1 protein expression in human HCT116 cells after 8 hrs by Western blot analysis, IC50 = 0.7 μM. 30429953
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生物活性

製品説明 PTC-209 is a potent and selective BMI-1 inhibitor with IC50 of 0.5 μM in HEK293T cell line, and results in irreversible reduction of cancer-initiating cells (CICs).
特性 BMI-1-selective inhibitor targeting self-renewal of cancer cells.
Targets
BMI-1 [1]
(HEK293T cells)
0.5 μM
In Vitro
In vitro PTC-209 inhibits both the UTR-mediated reporter expression and endogenous BMI-1 expression in human colorectal HCT116 and human fibrosarcoma HT1080 tumor cells. PTC-209 decreases colorectal tumor cell growth in a BMI-1-dependent way. In addition, PTC-209 impairs colorectal cancer-initiating cells (CICs) through irreversible growth inhibition. [1]
Kinase Assay Untranslated region-mediated luciferase reporter expression
HEK293 cells are transfected with a GEMS reporter vector that contains the luciferase open-reading frame flanked by and under post-transcriptional control of the BMI-1 5′ and 3′ UTRs. The resulting stable cells (F8) are treated with PTC-209 or vehicle control overnight, and then luciferase reporter activity is determined using Bright-Glo assays. The assays are run in triplicate for each point, and the percentage of inhibition was calculated against vehicle control.
細胞実験 細胞株 Human lymphoma U937 and HT1080 tumor cells, primary human peripheral blood mononuclear cells and human hematopoietic stem cells.
濃度 ~10 μM
反応時間 4 days
実験の流れ To determine whether pretreatment with the inhibitor affects tumor cell growth, cells are plated with the inhibitor for 4 d in vitro and plated in limiting doses in vitro without adding further inhibitor. Trypan blue exclusion is used to count viable cells. The in vitro sphere-initiating cell frequency is calculated after inhibitor treatment by evaluating the number of wells containing spheres. For the experiments where LDAs are set up following recovery of PTC-209 treated cells, 6-well plates were seeded with 1E6 cells per well and incubated overnight. Cells are subsequently treated for 4 d in triplicate with either DMSO vehicle or PTC-209 (0.01, 0.1, 1 and 10 μM). Drug treatments are washed off and 4 mL fresh suspension medium added to all wells. To assess cell viability following the 4 d treatment window, cells are trypsinized and counted at 0, 24, 72 and 120 h after removal of the drug. Long-lasting effects of the drug treatment on sphere-forming ability are assessed by plating LDAs (50,000, 10,000, 1,000,100, 10 and 1 cell per well) using the cells obtained 120 h after the 4-d drug treatment.
In Vivo
In Vivo PTC-209 (60 mg/kg/day, s.c.) effectively inhibits BMI-1 production in tumor tissue, and halts growth of preestablished tumors in mice bearing primary human colon cancer xenograft, human colon cancer cell lines LIM1215 or HCT116 xenografts. PTC-209 also reduces the frequency of functional colorectal CICs in vivo. [1]
動物実験 動物モデル Primary human colon cancer xenograft, human colon cancer cell lines LIM1215 and HCT116 xenografts in nude mice.
投与量 ~60 mg/kg/day
投与経路 s.c.

化学情報

分子量 495.19 化学式

C17H13Br2N5OS
CAS No. 315704-66-6 SDF Download PTC-209 SDFをダウンロードする
Smiles CC1=C(N2C=CC=NC2=N1)C3=CSC(=N3)NC4=C(C=C(C=C4Br)OC)Br
保管

In vitro
Batch:

DMSO : 99 mg/mL ( (199.92 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。)

Water : Insoluble

Ethanol : 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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