5mg AP26113-analog （ALK-IN-1）
| 參考價(jià) | ￥ 1704 |
| 訂貨量 | ≥1 |
- 公司名稱 上海高創(chuàng)化學(xué)科技有限公司
- 品牌 Selleck
- 型號(hào) 5mg
- 產(chǎn)地 美國(guó)
- 廠商性質(zhì) 代理商
- 更新時(shí)間 2017/11/21 10:17:20
- 訪問次數(shù) 451
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| 供貨周期 | 現(xiàn)貨 | 規(guī)格 | 5mg |
|---|---|---|---|
| 貨號(hào) | S7000 | 主要用途 | 科研 |
AP26113-analog (ALK-IN-1) 現(xiàn)貨
AP26113-analog (ALK-IN-1) 是AP26113的類似物，是有效的、選擇性的ALK抑制劑，同時(shí)也是EGFR的抑制劑。
化學(xué)數(shù)據(jù)
| 分子量 | 529.01 | 穩(wěn)定性 | 3年 -20°C粉狀 |
|---|---|---|---|
| 化學(xué)式 | C26H34ClN6O2P | -- -- -- | |
| CAS號(hào) | 1197958-12-5 | 別名 | AP26113-analog, AP-26113-analog, AP 26113-analog, Brigatinib-analog |
| Solubility (25°C) * | 體外 | Ethanol | 106 mg/mL (200.37 mM) |
| DMSO | 45 mg/mL (85.06 mM) | ||
| Water | Insoluble | ||
| 體內(nèi) | NMP+polyethylene glycol 300 (10+90, v+v) | 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. | |||
| 化學(xué)名 | 2,4-Pyrimidinediamine, 5-chloro-N2-[4-[4-(dimethylamino)-1-piperidinyl]-2-methoxyphenyl]-N4-[2-(dimethylphosphinyl)phenyl]- | ||
制備儲(chǔ)備液
| 濃度溶劑體積(Ethanol)質(zhì)量 | 1 mg | 5 mg | 10 mg |
| 1 mM | 1.8903 mL | 9.4516 mL | 18.9032 mL |
| 5 mM | 0.3781 mL | 1.8903 mL | 3.7806 mL |
| 10 mM | 0.1890 mL | 0.9452 mL | 1.8903 mL |
| 50 mM | 0.0378 mL | 0.1890 mL | 0.3781 mL |
生物活性
| 產(chǎn)品描述 | AP26113-analog (ALK-IN-1) 是AP26113的類似物，是有效的、選擇性的ALK抑制劑，同時(shí)也是EGFR的抑制劑。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶點(diǎn) |
| |||||||||||
| 體外研究 | Brigatinib和AP26113-analog對(duì)三突變體EGFR具有相似的效力，IC50<100 nM。在表達(dá)各種類型EGFR突變的細(xì)胞中，AP26113-analog抑制EGFR的磷酸化以及其下游信號(hào)通路[2]。 | |||||||||||
| 體內(nèi)研究 | ||||||||||||
| 臨床實(shí)驗(yàn) | ||||||||||||
| 特征 | ||||||||||||
*的實(shí)驗(yàn)操作 (此*來自于公開的文獻(xiàn)所以Selleck并不保證其有效性)
細(xì)胞實(shí)驗(yàn)：
[2]
| 細(xì)胞系 | Ba/F3細(xì)胞 |
|---|---|
| 濃度 | 0.3 nM-10 μM |
| 處理時(shí)間 | 72 h |
| 方法 | 將Ba/F3, PC9和MGH121細(xì)胞分別以 2,000, 1,500和2,000細(xì)胞/孔的密度鋪于黑色透明底的96孔板。當(dāng)天，用0.3 nM-10 μM的TKI對(duì)Ba/F3細(xì)胞進(jìn)行處理（PC9和MGH121細(xì)胞則是在鋪板后的第二天開始處理）。72小時(shí)后，檢測(cè)細(xì)胞生存活性。 |
參考
- [1] Wei-Sheng Huang, et al. J Med Chem, 2016, 59(10):4948-4964.
- [2] Uchibori K, et al. Nat Commun. 2017, 8:14768.
客戶使用selleck產(chǎn)品的實(shí)驗(yàn)數(shù)據(jù)
, , Clin Cancer Res,2015, 21(1):166-74.
Several ALK inhibitors effectively inhibit the growth of CD74–ROS1–addicted Ba/F3 cells. A, Ba/F3 cells expressing CD74–ROS1 (clone #6) were seeded in 96-well plates and treated with the indicated concentration of crizotinib, ceritinib, AP26113, ASP3026, or alectinib for 72 hours. Cell viability was analyzed using the CellTiter-Glo Assay. B, IC50 values (nmol/L) of Ba/F3 cell lines expressing CD74–ROS1 (clone #6) against various ALK inhibitors are shown. Average IC50 values against crizotinib, ceritinib, or AP26113 were calculated from the three independent experiments. IC50 values against ASP3026 and alectinib were calculated from the single experiment. C, inhibition of phospho-ROS1 by various ALK inhibitors in Ba/F3 models. CD74–ROS1–expressing Ba/F3 cells were exposed to increasing concentrations of crizotinib, ceritinib, AP26113, ASP3026, or alectinib for 3 hours. Cell lysates were immunoblotted to detect the indicated proteins.
AP26113-analog (ALK-IN-1)在4個(gè)文獻(xiàn)中得到引用
Cabozantinib Overcomes Crizotinib Resistance in ROS1 Fusion–Positive Cancer [Katayama R, et al. Clin Cancer Res, 2015, 21(1):166-74]
PubMed: 25351743Two Novel ALK Mutations Mediate Acquired Resistance to the Next-Generation ALK Inhibitor Alectinib [Katayama R, et al. Clin Cancer Res, 2014, 20(22):5686-96]
PubMed: 25228534A New Human Lung Adenocarcinoma Cell Line Harboring the EML4-ALK Fusion Gene [Isozaki H, et al. Jpn J Clin Oncol, 2014, 44(10):963-8]
PubMed: 25170107Establishment and Characterization of a Singaporean Chinese Lung Adenocarcinoma Cell Line with Four Copies of the Epidermal Growth Factor Receptor Gene [Choong ML, et al. Biores Open Access, 2014, 3(4):176-82]
如果需要*保存，請(qǐng)于零下二十度低溫保存。
禁止用于人體及治療！
特定的存儲(chǔ)和包裝每個(gè)產(chǎn)品的信息在產(chǎn)品說明書上都有注明 。大多數(shù)Selleck產(chǎn)品，在*的條件下存儲(chǔ)可穩(wěn)定保存兩年。產(chǎn)品有時(shí)建議的儲(chǔ)存溫度不同，大多數(shù)建議儲(chǔ)存在-20°C ，抑制劑屬于化學(xué)試劑，可在常溫下運(yùn)輸儲(chǔ)存兩周左右。即使如此，我們保證產(chǎn)品的出貨量將保持產(chǎn)品質(zhì)量的條件下，一般都會(huì)放入冰袋。望閣下收到產(chǎn)品后，請(qǐng)按照產(chǎn)品數(shù)據(jù)表建議適當(dāng)存儲(chǔ)。
AP26113-analog (ALK-IN-1)
AP26113-analog (ALK-IN-1)
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