BIBR 1532 化学構造
分子量: 331.36

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Quality Control & MSDS

製品説明

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    Telomerase製品生物活性の比較
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製品の説明

生物活性

製品説明 BIBR1532は、100nMのIC50による強力で選択的なテロメラーゼ阻害剤です。
ターゲット Telomerase
IC50 100 nM [1]
In vitro試験 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/MlnR 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]
In vivo試験
臨床試験
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

Conventional Telomerase 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'-AATCCGTCGAGCAGAGTT). For the recombinant enzyme, 1–7 μL of affinity-purified telomerase (containing less than 0.025 μm hTERT) are assayed in a final volume of 40 μL containing 50 mM Tris acetate (pH 8.5), 50 mM KCl, 1 mM MgCl2, 1 mM spermidine, 5 mM 2-mercaptoethanol, 1 mM dATP, 1 mM dTTP, 2.5 μM dGTP, 15 μCi of [α-32P]dGTP (3000 Ci/mmol) and 2.5 μm (TTAGGG)3. The reaction is initiated by incubation at 37  °C for 2 hours and stopped by addition of 50 μL of RNase mix (0.1 mg/mL RNaseA-100 u/mL RNaseT1 in 10 mM Tris-Cl (pH 8.3) and 20 mm EDTA) and incubation for 20 min at 37 °C. Samples are deproteinated by adding 50 μL of 0.3 mg/m proteinase K in 10 mM Tris-Cl (pH 8.3) and 0.5% w/v SDS, for a 30-minute incubation at 37  °C. DNA is recovered by phenol extraction and ethanol precipitation, and the extension products are analyzed on an 8% (endogenous telomerase) or 12% (recombinant telomerase) polyacrylamide-urea gel. Dried gels are exposed to a Kodak phosphorimager screen, and the results are analyzed.

細胞アッセイ: [2]

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download BIBR 1532 SDF
分子量 331.36
化学式

C21H17NO3

CAS No. 321674-73-1
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 66 mg/mL (199.17 mM)
エタノール 3 mg/mL (9.05 mM)
<1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
* <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.
化学名 (E)-2-(3-(naphthalen-2-yl)but-2-enamido)benzoic acid

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Source J Mol Neurosci, 2013, 51(1), 187-98. BIBR 1532 purchased from Selleck
Method MTT assay
Cell Lines SK-N-BE2 cells
Concentrations 1 uM
Incubation Time 24 h
Results Combination therapy with BIBR 1532 and APG is effective in reducing cell viability in SK-N-BE2 cells.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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