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BPR1J-097 Sale

目录号 : GC19080

An FLT3 inhibitor

BPR1J-097 Chemical Structure

Cas No.:1327167-19-0

规格 价格 库存 购买数量
2mg
¥483.00
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5mg
¥756.00
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10mg
¥1,229.00
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50mg
¥3,759.00
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100mg
¥5,733.00
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Sample solution is provided at 25 µL, 10mM.

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Quality Control & SDS

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实验参考方法

Kinase experiment:

The FLT3 Kinase-Glo kinase assays are carried out in 96-well plates at 30°C for 4 h in a final volume of 50 μL, including 25 mM Tris pH 7.4, 10 mM MgCl2, 4 mM MnCl2, 1 mM DTT, 0.02% Triton X-100, 0.01% BSA, 1 μM ATP, 20 μM peptide (GGMEDIYFEFMGGKKK), 75 ng recombinant FLT3 proteins, and test compound (BPR1J-097) at the indicated concentration. After incubation, 50 μL Kinase-Glo Plus Reagent is added and incubated at 25°C for 20 min. A 70 μL aliquot of each reaction mixture is transferred to a black microtiter plate and the luminescence is measured on a multilabel counter. Each IC50 value is determined by three different experiments[1].

Cell experiment:

Proliferation assays are performed by seeding 10 000 cells per well in a 96-well culture plate. After 16 h, cells are then treated with vehicle or BPR1J-097 Hydrochloride at various concentrations in medium for 72 h. Cell viability is quantitated using the MTS method. The results are determined by measuring absorbance at 490 nm using a plate reader. The GC50 value is defined as the amount of compound that causes 50% reduction in cell viability in comparison with DMSO-treated (vehicle) control and is calculated using Prism version 4 software[1].

Animal experiment:

Male nude mice of 8 weeks of age are used. Nude mice (n=5 to 7 per group) are inoculated subcutaneously with MOLM-13 (1×106 per flank) or MV4-11 cells (5×106 per flank). When the tumour size reaches 100 to 200 mm3, animals are grouped and treated with BPR1J-097 Hydrochloride at various doses in a 2-week treatment period as indicated. Animals are treated with BPR1J-097 Hydrochloride (10 and 25 mg/kg, i.v.) or vehicle as control at once daily for 5 days per week for 2 weeks. Tumour volumes are measured and calculated with the formula length×width2/2 after initiation of treatments. Tumour size and animal body weight are measured twice a week after tumour cell inoculation. At the end of the study, animals are killed by carbon dioxide inhalation followed by cervical dislocation[1].

References:

[1]. Lin WH, et al. BPR1J-097, a novel FLT3 kinase inhibitor, exerts potent inhibitory activity against AML. Br J Cancer. 2012 Jan 31;106(3):475-81.

产品描述

BPR1J-097 is a novel potent FLT3 inhibitor with an IC50 of 11 nM.

References:
[1]. Lin WH, et al. BPR1J-097, a novel FLT3 kinase inhibitor, exerts potent inhibitory activity against AML. Br J Cancer. 2012 Jan 31;106(3):475-81.

Chemical Properties

Cas No. 1327167-19-0 SDF
Canonical SMILES O=C(NC1=NNC(C2=CC=CC(NS(=O)(C3=CC=CC=C3)=O)=C2)=C1)C4=CC=C(N5CCN(C)CC5)C=C4
分子式 C27H28N6O3S 分子量 516.61
溶解度 DMSO : 6 mg/mL (10.85 mM) 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.9357 mL 9.6785 mL 19.357 mL
5 mM 0.3871 mL 1.9357 mL 3.8714 mL
10 mM 0.1936 mL 0.9678 mL 1.9357 mL
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