| 中文名称: | LFM-A13 | ||||
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| 英文名称: | LFM-A13 | ||||
| 别名: | α-Cyano-β-hydroxy-β-methyl-N-(2,5-dibromophenyl)propenamide | ||||
| CAS No: | 244240-24-2 | 分子式: | C11H8Br2N2O2 | 分子量: | 360 |
| CAS No: | 244240-24-2 | ||||
| 分子式: | C11H8Br2N2O2 | ||||
| 分子量: | 360 | ||||
基本信息
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产品编号：L10044 |
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产品名称：LFM-A13 |
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CAS: |
244240-24-2 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
六个月
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分子量 |
360.00 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
72mg/mL warmed with 50ºC water bath (200.0mM) |
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Ethanol |
Insoluble |
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Water |
Insoluble |
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体内（现配现用） |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
2.7778mL |
13.8889mL |
27.7778mL |
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5mM |
0.5556mL |
2.7778mL |
5.5556mL |
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10mM |
0.2778mL |
1.3889mL |
2.7778mL |
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50mM |
0.0556mL |
0.2778mL |
0.5556mL |
生物活性
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产品描述 |
一种有效的、选择性的BTK（布鲁顿氏酪氨酸激酶）抑制剂，IC50：2.5μM。 |
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靶点/IC50 |
Plx1 10μM (IC50) |
PLK3 61μM (IC50) |
BRK 267μM (IC50) |
BMX 281μM (IC50) |
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BMX 281μM (IC50) |
Hepatocyte growth factor receptor kinase (Met) 215μM (IC50) |
BTK 2.5μM (IC50) |
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体外研究 |
LFM-A13 significantly inhibits BTK activity with an IC50 of 6.2 ± 0.3μg/mL (= 17.2 ± 0.8μM). The calculated Kis of LFM-A13 for BTK, JAK1, JAK3, IRK, EGFR and HCK are 1.4, 110, 148, 31.6, 166 and 214μM. LFM-A13 (200μM) markedly increases the chemosensitivity of ALL-1 cells to ceramide-induced apoptosi. LFM-A13 (100μM) suppresses Epo-induced phosphorylation of EpoR, Jak2, Btk, Stat5 and Erk1/2 in R10 cells. LFM-A13 (100μM) inhibits auto-phosphorylation of Jak2, Tec and Btk rather than Lyn kinase auto-phosphorylation in COS cells. LFM-A13 potently inhibits Plx1 with IC50 of 10μM; also inhibits BRK, BMX, FYN and with IC50s of 267,281,240 and 215μM. |
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体内研究 |
LFM-A13 (25,50 and 100mg/kg) shows no apparent toxicity to rats. LFM-A13 (50mg/kg, three times a week, i.p.) attenuates DMBA-induced mammary tumorigenesis in mice. LFM-A13 alone or in combination with paclitaxel shows marked effect on the DMBA-induced breast tumor incidence, mean tumor numbers, average tumor weight, and size in BALB/c mice. LFM-A13 (50mg/kg, three times a week, i.p.) significantly decreases PLK1, cyclin D1, CDK-4, P53 and Bcl-2 expression, but increases the expression of p21,IκB,Bax and caspase 3 expression in mice. LFM-A13 (200mg/kg) does not cause hematologic toxicity in rats. LFM-A13 (10 or 50mg/kg, i.p.) exhibits anti-tumor effects dose dependently in the MMTV/Neu transgenic mouse model of breast cancer. |
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推荐实验方法(仅供参考)
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激酶实验： |
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Purified His6-Plx1 (250ng) is added to a 20μL reaction mixture containing 1× kinase buffer (10mM Tris-HCl, pH 7.5,10mM MgCl2, and 1mM TT), 25μM cold ATP, and 1μCi [γ-32P]ATP in the presence of different concentrations of LFM-A13 ranging from 5μg/mL (13.9μM) to 100μg/mL (278μM). The reaction mixtures are incubated at room temperature for 15-30 min and autophosphorylation is stopped by addition of 2× SDS-PAGE reducing sample buffer. A parallel experiment is performed in the presence of cold ATP. The kinase reactions are then subjected to immunoblotting using the commercially available antiPlk antibodies. The immunoblots confirmed that the same amount of Plx1 protein is present in each reaction. In addition,we also examined the effects of LFM-A13 on substrate phosphorylation by Plx1. In brief, 250ng of purified Plx1 is first incubated at room temperature for one hour with different concentrations of LFM-A13. After one hour of incubation, the tubes containing the reaction mixtures are put on ice and the substrate, GST-Cdc25 peptide (254-316) (200ng), kinase buffer, and [γ-32P]ATP are added and the kinase reaction allowed to proceed for 15 min at room temperature.Immunoblotting with anti-Cdc25 antibodies is used to confirm that equal amounts of the substrate peptide are present in each reaction mixture. Anti-Plk antibodies, the polyclonal antibodies to gluthathione-S-transferase (GST) and ECL kit are used in the assay. The mode of human PLK3 inhibition by LFM-A13 is examined in titration experiments using increasing concentrations of [γ-32P]ATP and purified N-terminal His6-tagged recombinant human PLK3, residues 19-301, expressed by baculovirus in Sf21 insect cells. In brief, in a final reaction volume of 25μL, PLK3 (h) (5-10mU) is incubated with 8 mM MOPS,pH 7.0,0.2mM EDTA, 2mg/mL casein, 10mM Mg acetate, and [γ-32P-ATP] (specific activity approx. 500 cpm/pmol,concentration as required). The reaction is initiated by the addition of the MgATP mix. After incubation for 40min at room temperature, the reaction is stopped by the addition of 5μL of a 3% phosphoric acid solution. Ten microliters of the reaction is then spotted onto a P30 filtermat and washed three times for 5min in 75mM phosphoric acid and once in methanol prior to drying and scintillation counting. The Ki of PLK3 by LFM-A13 is calculated from the reciprocal plots of the intensity of phosphorylation of the substrate (1/v) versus the concentration of the inhibitor (i) (viz., LFM-A13). From this Dixon plot, the Ki represents the dissociation constants of the EI complex, which is determined by the point of linear intersection. |
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动物实验: |
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Mice Neu transgenic mice carrying one or more tumors are randomLy placed in the study. For the evaluation of tumor kinetics,tumor-bearing mice are randomLy assigned to either vehicle control or treatment groups. Tumor growth is determined by the measurement of tumors with a caliper in three dimensions three days a week and expressed as tumor volume in cubic millimeters (mm3). Tumor volumes are calculated using the formula for the volume of a prolate spheroid, V = 4/3 × 3. 14 ×length/2 × width/2 × depth/2. Due to the large heterogeneity in transgenic tumor volumes on day 0, tumor growth for each mouse is normalized to the starting volume for that particular tumor. Therefore, each mouse also serves as its own control and the tumor growth curves are generated to show the rate of change in tumor volumes. LFM-A13 (10 or 50mg/kg) is administered by twice daily intraperitoneal injections on 5 consecutive days per week. Paclitaxel is administered intraperitoneally on days 1,3,5,8,10 and 12 at a dose level of 6.7mg/kg.Gemcitabine is administered on days 1, 8, and 15 at a dose level of 33.7mg/kg. |
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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
