| 中文名称: | AV-412 free base | ||||
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| 英文名称: | AV-412 free base | ||||
| 别名: | MP-412 free base MP-412 free base | ||||
| CAS No: | 451492-95-8 | 分子式: | C27H28ClFN6O | 分子量: | 507 |
| CAS No: | 451492-95-8 | ||||
| 分子式: | C27H28ClFN6O | ||||
| 分子量: | 507 | ||||
基本信息
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产品编号：A12263 |
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产品名称：AAV-412 free base |
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CAS: |
451492-95-8 |
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 |
507.00 |
-20℃ |
一个月 |
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化学名： |
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Solubility (25°C) |
体外 |
DMSO |
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Ethanol |
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Water |
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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 |
1.9724mL |
9.8619mL |
19.7239mL |
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5mM |
0.3945mL |
1.9724mL |
3.9448mL |
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10mM |
0.1972mL |
0.9862mL |
1.9724mL |
生物活性
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产品描述 |
一种EGFR抑制剂，抑制EGFR，EGFRL858R，EGFRT790M，EGFRL858R/T790M和ErbB2的IC50值分别为0.75，0.5，0.79，2.3，19nM。 |
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靶点/IC50 |
EGFR 0.75nM (IC50) |
ErbB2 19nM (IC50) |
EGFRL858R 0.51nM (IC50) |
EGFRL858R/T790M 2.3nM (IC50) |
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EGFRT790M 0.79nM (IC50) |
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体外研究 |
AV-412 inhibits autophosphorylation of EGFR and ErbB2 with IC50 of 43 and 282nM, respectively. AV-412 also inhibits epidermal growth factor (EGF)-dependent cell proliferation with an IC50 of 100nM. AV-412 abrogates EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR. |
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体内研究 |
In animal studies using cancer xenograft models, AV-412 (30mg/kg) demonstrates complete inhibition of tumor growth of the A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively. AV-412 suppresses autophosphorylation of EGFR and ErbB2 at the dose corresponding to its antitumor efficacy. When various dosing schedules are applied, AV-412 shows significant effects with daily and every-other-day schedules, but not with a once-weekly schedule, suggesting that frequent dosing is preferable for this compound. Furthermore, AV-412 shows a significant antitumor effect on the ErbB2- overexpressing breast cancer KPL-4 cell line, which is resistant to gefitinib. |
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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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Recombinant intracellular kinase domains of EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M, and purified EGFR from A431 cell membranes are used. Kinase reactions are carried out in 8mM MOPS (pH 7.0), 0.2mM ethylenediaminetetraacetic acid (EDTA), 10mM MnCl2, 10mM Mg acetate, 0.1mg/mL poly(Glu, Tyr) 4:1, [γ 33P-ATP], and 5–10mU of enzyme, except that 250µM of the GGMEDIYFEFMGGKKK peptide substrate is used for EGFRT790M. Phosphorylation is initiated by the addition of ATP and is allowed to proceed for 40 min at room temperature. The reaction is stopped by the addition of 3% phosphoric acid, then aliquots of the reaction mixture are spotted onto a filtermat. After rinsing to remove peptides bound non-specifically, the filter is scintillation counted. |
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细胞实验: |
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To test the effects of AV-412 on growth factor-dependent cell proliferation, A431 and A7r5 cells are cultured for 24h at 37°C in the presence of 1 ng/mL epidermal growth factor and 50 ng/mL platelet-derived growth factor, respectively. The 3Hthymidine incorporation during this period is measured. |
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动物实验: |
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Mice: For studies examining the dosing schedule in relation to efficacy against TE-8 tumors, AV-412 is administered either once daily, every other day, or once per week for 2 weeks. Mice are killed 1 day after the final treatment, and the tumors are dissected and weighed. For evaluation of tumor phosphorylation, tumor-bearing mice are given a single administration of AV-412 and tumors are dissected 4h later. |
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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 )
