BIBR 1532

BIBR 1532 is a potent, selective, non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay. No inhibition of DNA and RNA polymerases, including HIV reverse transcriptase are observed at concentrations vastly exceeding the IC50 for telomerase. BIBR 1532 induces apoptosis in cancer cells.

CAS No. 321674-73-1

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
10mg	JPY 22000	国内在庫あり
50mg	JPY 70500	国内在庫あり
1g	JPY 598500	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] よく尋ねられる質問

文献中Selleckの製品使用例（29）

カスタマーフィードバック2个实验数据

製品安全説明書

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99.99

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シグナル伝達経路

Telomeraseシグナル伝達経路

Telomerase阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Incubation Time	活性情報	PMID
human MDA-MB-231 cells	Function assay	24 h	Inhibition of telomerase in human MDA-MB-231 cells after 24 hrs by TRAP-PCR-ELISA, IC50=0.17 μM	25965778
human HeLa cells	Function assay	2 h	Inhibition of telomerase in human HeLa cells after 2 hrs by [alpha-32P]dGTP incorporation assay, IC50=93 nM	22413845
human MGC803 cells	Function assay	24 h	Inhibition of telomerase in human MGC803 cells after 24 hrs by TRAP-PCR-ELISA, IC50=0.28 μM	25554922
HeLa	Function assay	15 mins	Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction by telomeric repeat amplification protocol, IC50=3.6μM	22413845
HeLa	Function assay	15 mins	Inhibition of telomerase in human HeLa cells using 5'-AAT CCG TCG AGC AGA GTT-3' as substrate incubated for 15 mins prior to extension reaction followed by compound washout by spin-telomeric repeat amplification protocol, IC50=4.6μM	22413845
HeLa	Function assay	30 mins	Inhibition of human telomerase isolated from human HeLa cells nuclear extracts expressed in insect cells assessed as [33P]dCMP incorporation after 30 mins by liquid scintillation counting analysis, IC50=0.093μM	24053596
HEK293	Function assay		Inhibition of human telomerase activity isolated from HEK293 cells assessed as reduction in dNTP incorporation using 5'-biotinylated AATCCGTCGAGCAGAGTT primer by flash plate assay, IC50=3.6μM	27657809
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生物活性

製品説明

BIBR 1532 is a potent, selective, non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay. No inhibition of DNA and RNA polymerases, including HIV reverse transcriptase are observed at concentrations vastly exceeding the IC50 for telomerase. BIBR 1532 induces apoptosis in cancer cells.

Targets

Telomerase ^[1]
(Cell-free assay)

100 nM

In Vitro
In vitro	BIBR 1532 exhibits an non-competitive inhibitory effect on telomerase activity. ^[1] In JVM13 leukemia cell line, BIBR 1532 shows an antiproliferative effect in a dose-dependent range with IC50 of 52 μM, and similar results are also observed in other leukemia cell lines including Nalm-1, HL-60, and Jurkat. In addition, BIBR 1532 results in a direct antiproliferative effect on acute myeloid leukemia (AML) with IC50 of 56 μM without affecting the proliferative capacity of normal hematopoietic progenitor cells. ^[2] BIBR 1532 (2.5 μM) reduces colony-forming ability, and induces telomere length shortening as well as chemotherapeutic sensitization by inhibiting telomerase activity in MCF-7/WT and melphalan-resistant MCF-7/Mln^R cell lines. ^[3] In T-cell prolymphocytic leukemia (T-PLL), BIBR 1532 shows selective cytotoxic effects in a dose-dependent manner and BIBR 1532-treated cells also demonstrates nuclear condensation and formation of apoptotic bodies morphologically compatible with apoptosis. ^[4] A recent study shows that combination treatment of BIBR 1532 and chemotherapeutic agents carboplatin results in a potential synergy for eliminateing ovarian cancer spheroid-forming cells in ES2, SKOV3, and TOV112D cell lines. ^[5]
Kinase Assay	Conventional Telomerase Assay
Kinase Assay	For the direct telomerase assay with the endogenous telomerase, 10 μL of telomerase-enriched extract is mixed with different concentrations of BIBR1532 in a final volume of 20 μL. After 15-minute preincubation on ice, 20 μL of the reaction mixture is added, and the reaction is initiated by transferring the tubes to 37 °C. The final concentrations in the reaction mixture are 25 mM Tris-Cl (pH 8.3), 1 mM MgCl₂, 1 mM EGTA, 1 mM dATP, 1 mM dTTP, 6.3 μM cold dGTP, 15 μCi [α-³²P]dGTP (3000 Ci/mmol; NEN), 1.25 mM spermidine, 10 units of RNasin, 5 mM 2-mercaptoethanol, and 2.5 μM TS-primer (5
細胞実験	細胞株	JVM13
	濃度	0 to 80 μM
	反応時間	24 -72 hours
	実験の流れ	Cells are plated as triplicates in complete RPMI 1640 medium with various concentrations of BIBR1532. After 24 to 72 hours, water-soluble tetrazolium (WST-1) is added, which is transformed into formazan by mitochondrial reductase systems. The increase in the number of viable cells results in an increase of activity of mitochondrial dehydrogenases, leading to an increase of formazan dye formed, which is quantified by ELISA reader after 2, 3, and 4 hours of incubation.

参考
[1] Pascolo E, et al. J Biol Chem. 2002, 277(18), 15566-15572. [2] El-Daly H, et al. Blood. 2005, 105(4), 1742-1749. [3] Ward RJ, et al. Mol Pharmacol. 2005, 68(3), 779-786. [4] R?th A, et al. Leukemia. 2007, 21(12), 2456-2462. [5] Meng E, et al. Gynecol Oncol. 2012, 124(3), 598-605. + 展開

参考

+ 展開

化学情報

分子量	331.36	化学式	C₂₁H₁₇NO₃
CAS No.	321674-73-1	SDF	Download BIBR 1532 SDFをダウンロードする
Smiles	CC(=CC(=O)NC1=CC=CC=C1C(=O)O)C2=CC3=CC=CC=C3C=C2
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 66 mg/mL ( (199.17 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 : 16 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
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):