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TAK-285

TAK-285

产品编号 T6039   CAS 871026-44-7
别名: TAK285, TAK 285

TAK-285 是一种新型 HER2 和 EGFR(HER1) 双重抑制剂,IC50 分别为 17 和 23 nM。它可穿过血脑屏障,有抗肿瘤活性,对 HER1/2 的选择性是 HER4 的 10 倍以上。

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TAK-285 Chemical Structure
TAK-285, CAS 871026-44-7
规格 价格/CNY 货期 数量
1 mg ¥ 688 现货
5 mg ¥ 1,680 现货
10 mg ¥ 2,530 现货
25 mg ¥ 3,920 现货
50 mg ¥ 5,580 现货
100 mg ¥ 7,830 现货
1 mL * 10 mM (in DMSO) ¥ 1,960 现货
产品目录号及名称: TAK-285 (T6039)
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纯度: 99.17%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 TAK-285 is a novel dual HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, >10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. Phase 1.
靶点活性 EGFR/HER1:23 nM, HER2:17 nM
体外活性 Among the 34 kinases tested, TAK-285 only significantly inhibits HER4 with IC50 of 260 nM, slightly inhibits MEK1, MEK5, c-Met, Aurora B, Lck, CSK, and Lyn B with IC50 of 1.1 μM, 5.7 μM, 4.2 μM, 1.7 μM, 2.4 μM, 4.7 μM, and 5.2 μM, respectively, and displays no activity against other kinases with IC50 of >10 μM. TAK-285 shows significant growth inhibitory activity against BT-474 cells (HER2-overexpressing human breast cancer cell line) with GI50 of 17 nM. [1] Compared with SYR127063 a potent inhibitor of HER2, TAK-285 displays similar in vitro potency against HER2 and EGFR. Compared with the full cytoplasmic domains of the wild-type proteins, the mutations and shortened boundaries used for structure determination of HER2-KD and EGFR-KD do not significantly change the inhibitory activity (IC50) of TAK-285. TAK-285 binds to the inactive conformation of EGFR, and shows a similar binding mode with lapatinib in the active site. [2]
体内活性 The oral bioavailability of TAK-285 is 97.7% in rats and 72.2% in mice at a dose of 50 mg/kg. Oral administration of TAK-285 at 100 mg/kg twice daily for 14 days displays significant antitumor efficacy in the HER2-overexpressing BT-474 tumor xenograft mouse model with tumor/control (T/C) ratio of 29%, without affecting body weight. Similar to the BT-474 model, TAK-285 exhibits dose-dependent tumor growth inhibition of 4-1ST (HER2-overexpressing human gastric cancer tumor) xenografts in mice, with T/C of 44% and 11% at doses of 50 mg/kg and 100 mg/kg, twice daily, respectively, without significant body weight loss in mice. Furthermore, TAK-285 treatment induces dose-dependent growth inhibition of 4-1ST tumors in rats with T/C of 38% and 14% at doses of 6.25 mg/kg and 12.5 mg/kg, and, particularly noteworthy, tumor regression with T/C of -12% and -16% at doses of 25 mg/kg and 50 mg/kg, respectively. [1] After oral administration of TAK-285, a significant amount of TAK-285 is present in the brain of rats in pharmacologically active, unbound form (approximately 20% of its free plasma level), indicating that TAK-285 has a potential in the therapy of CNS malignancies/metastases. [3]
激酶实验 HER2 and EGFR kinase assay: The cytoplasmic domain (amino acids 676-1255) of human HER2 and the cytoplasmic domain (amino acids 669-1210) of human EGFR are expressed as N-terminal peptide (DYKDDDD)-tagged protein using a baculovirus expression system. The expressed HER2 kinase and EGFR kinase are purified by anti-FLAG M2 affinity gel. The EGFR and HER2 kinase assays are performed using radiolabeled [γ-32P]ATP in 96-well plates. The kinase reactions are performed in 50 mM Tris-HCl (pH 7.5), 5 mM MnCl2, 0.01% Tween 20, and 2 mM DTT containing 0.9 uCi of [γ-32P]ATP per reaction, 50 μM ATP, 5 ug/mL poly(Glu)-Tyr (4:1), and each purified cytoplasmic domain (0.25 μg/mL EGFR or HER2) in a total volume of 50 μL. To measure the IC50 value for enzyme inhibition, Increasing concentrations of TAK-285 are incubated with the enzyme for 5 minutes prior to the reaction at room temperature. The kinase reactions are initiated by adding ATP. After 10 minutes at room temperature, the reactions are stopped by the addition of 10% (final concentration) trichloroacetic acid. The γ-32P phosphorylated proteins are filtrated in a harvest plate with a cell harvester and washed free of [γ-32P]ATP with 3% phosphoric acid. The plates are dried followed by the addition of 25 μL of MicroScint0. The radioactivity is counted by a TopCount scintillation counter. IC50 values are calculated by nonlinear regression analysis of the percent inhibitions.
细胞实验 The cells are treated continuously with various concentrations of TAK-285 for 5 days. The live cell numbers are counted with a particle analyzer.(Only for Reference)
别名 TAK285, TAK 285
分子量 547.96
分子式 C26H25ClF3N5O3
CAS No. 871026-44-7

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 102 mg/mL (186.1 mM)

Ethanol: 50 mg/mL (91.2 mM)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 1.825 mL 9.1248 mL 18.2495 mL 45.6238 mL
5 mM 0.365 mL 1.825 mL 3.6499 mL 9.1248 mL
10 mM 0.1825 mL 0.9125 mL 1.825 mL 4.5624 mL
20 mM 0.0912 mL 0.4562 mL 0.9125 mL 2.2812 mL
50 mM 0.0365 mL 0.1825 mL 0.365 mL 0.9125 mL
DMSO 100 mM 0.0182 mL 0.0912 mL 0.1825 mL 0.4562 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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参考文献

1. Ishikawa T, et al. J Med Chem, 2011, 54(23), 8030-8050. 2. Aertgeerts K, et al. J Biol Chem, 2011, 286(21), 18756-18765. 3. Erdo F, et al. Brain Res Bull, 2012, 87(4-5), 413-419.
(S)-Afatinib Epertinib hydrochloride PD-118057 Sulfatinib Terfenadine CUDC-101 SU5204 NS1643

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 酪氨酸激酶分子库 抗癌临床化合物库 抗癌活性化合物库 抗肥胖化合物库 抗肺癌化合物库 ReFRAME 相关化合物库 抗胰腺癌化合物库 抗卵巢癌化合物库 表观遗传库

剂量换算

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% ddH2O
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

TAK-285 871026-44-7 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic JAK/STAT signaling MAPK Tyrosine Kinase/Adaptors HER MEK EGFR Aurora Kinase ErbB-1 HER2 Inhibitor CNS penetration orally Epidermal growth factor receptor inhibit antitumor TAK285 HER1 TAK 285 inhibitor

 

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