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  3. BPR1J-097 Hydrochloride

BPR1J-097 Hydrochloride 

目录号: HY-13537A 纯度: 99.20%
COA 产品使用指南

BPR1J-097 Hydrochloride 是一个新型且强效的 FLT3 抑制剂,其 IC50 值为 11 nM。

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BPR1J-097 Hydrochloride Chemical Structure

BPR1J-097 Hydrochloride Chemical Structure

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ¥852
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2 mg ¥500
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5 mg ¥700
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10 mg ¥1200
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50 mg ¥4500
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100 mg ¥6500
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500 mg   询价  

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Customer Review

Other Forms of BPR1J-097 Hydrochloride:

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

IC50 & Target

IC50: 11 nM (FLT3)[1]

体外研究
(In Vitro)

BPR1J-097 Hydrochloride is a novel and potent FLT3 inhibitor with an IC50 of 11nM. Phosphorylation of all FLT3-WT, FLT3-IDT, and FLT3-D835Y are inhibited by BPR1J-097 Hydrochloride at a concentration as low as 10 nM. BPR1J-097 Hydrochloride suppresses the phosphorylation of FLT3 and STAT5 in a dose-dependent manner. The IC50 values of BPR1J-097 Hydrochloride on MOLM-13 and MV4-11 cells are 21±7 and 46±14 nM, respectively. The emergence of active caspase-3 is observed in MOLM-13 cells treated with BPR1J-097 Hydrochloride at 10 nM. The effect of BPR1J-097 Hydrochloride seems to be weaker in MV4-11 cells as caspase-3 is not evident until 100 nM of BPR1J-097 Hydrochloride is applied to treat cells[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

After i.v. administration of mice with BPR1J-097 Hydrochloride at two cycles of 10 or 25 mg/kg, a clear dose-dependent anti-tumour effect is observed. Tumours in mice treated with BPR1J-097 Hydrochloride (25 mg/kg per day) stop growing. BPR1J-097 Hydrochloride (25 mg/kg) shows a significant tumour shrinkage effect on the subcutaneously growing MOLM-13 tumours in a size of >2000 mm3. BPR1J-097 Hydrochloride (10 and 25 mg/kg) also produces a dose-dependent growth reduction and shrinkage of another model using MV4-11 cells. It is noted that a prolonged disappearance of MV4-11 tumours is observed in mice treated with BPR1J-097 Hydrochloride at 25 mg/kg. There is little (3%) or no body weight loss of BPR1J-097 Hydrochloride-treated nude mice during the observation periods in these in vivo studies[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

553.08

Formula

C27H29ClN6O3S

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 6 mg/mL (10.85 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : 2 mg/mL (3.62 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8081 mL 9.0403 mL 18.0806 mL
5 mM 0.3616 mL 1.8081 mL 3.6161 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

BPR1J-097 Hydrochloride 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 1.8081 mL 9.0403 mL 18.0806 mL 45.2014 mL
DMSO 5 mM 0.3616 mL 1.8081 mL 3.6161 mL 9.0403 mL
10 mM 0.1808 mL 0.9040 mL 1.8081 mL 4.5201 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
BPR1J-097 Hydrochloride
目录号:
HY-13537A
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