Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK2256098 (GTPL7939) 是一种选择性FAK 激酶抑制剂,抑制胰腺癌细胞的生长和存活。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 322 | 现货 | ||
2 mg | ¥ 463 | 现货 | ||
5 mg | ¥ 728 | 现货 | ||
10 mg | ¥ 1,130 | 现货 | ||
25 mg | ¥ 2,260 | 现货 | ||
50 mg | ¥ 3,480 | 现货 | ||
100 mg | ¥ 4,900 | 现货 | ||
500 mg | ¥ 9,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 786 | 现货 |
产品描述 | GSK2256098 (GTPL7939) is a small molecule FAK kinase inhibitor. |
靶点活性 | FAK:0.4 nM(Ki) |
体外活性 | GSK2256098 has been developed to inhibit FAK activity through targeting the phosphorylation site of FAK, tyrosine (Y) 397. After a 30-min incubation, GSK2256098 inhibits FAK activity or Y397 phosphorylation in cancer cell lines, OVCAR8 (ovary), U87 mg (brain), and A549 (lung), at IC50 values of 15, 8.5 and 12 nM, respectively. In addition, the data suggests that cellular inhibition of FAK by GSK2256098 can occur as early as 30 min in cultured cells and lasts up to 12 hours in mouse tumor xenografts. GSK2256098 inhibition of FAK kinase activity can decrease Akt and ERK activity. PI3K/Akt and ERK signaling contributes to cell survival, implying a pharmacological value of GSK2256098 in attenuation of abnormal survival pathways in specific types of PDAC cells. GSK2256098 can promote apoptosis in L3.6P1 cells through caspase-9/PARP-related pathways. It attenuates abnormal growth and aberrant motility of PDAC cells in a FAK specific manner[1]. GSK2256098 also inhibits growth, migration, and invasion and induces apoptosis in a subset of GBM cell lines[2]. |
体内活性 | Pharmacokinetic (PK) studies in mice and rats with an intact blood brain barrier indicate that the penetration of GSK2256098 into the CNS is poor. However, it achieves concentrations in tumor of patients with GBM(glioblastoma) exceeding those associated with preClinicalal activity[2]. GSK2256098 has an acceptable safety profile, has evidence of target engagement at doses at or below the MTD (maximum tolerated dose), and has Clinicalal activity in patients with mesothelioma, particularly those with merlin loss[3]. In the Ishikawa orthoptopic murine model, treatment with GSK2256098 results in lower tumor weights and fewer metastases than mice inoculated with Hec1A cells. Tumors treated with GSK2256098 have lower microvessel density (CD31), less cellular proliferation (Ki67), and higher apoptosis (TUNEL) rates in the Ishikawa model when compared to the Hec1a model. GSK2256098 may be therapeutically beneficial to patients with PTEN-mutant uterine cancer, and PTEN represents a potential predictive biomarker[4]. |
细胞实验 | PDAC cells are cultured on a 6-well plate. When cell confluence reachs about 70% in regular medium, the cells are incubated in the medium containing 0.1-10 μM GSK2256098 for 48 or 72 hr. At the end of treatments, cells are re-seeded and kept for 9 d Then, the cells are stained using Clonogenic Reagent, and the blue colonies are counted. (Only for Reference) |
别名 | GSK 2256098, GSK-2256098, GTPL7939 |
分子量 | 414.89 |
分子式 | C20H23ClN6O2 |
CAS No. | 1224887-10-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 76 mg/mL (183.2 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: 76 mg/mL (183.2 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.4103 mL | 12.0514 mL | 24.1028 mL | 60.2569 mL |
5 mM | 0.4821 mL | 2.4103 mL | 4.8206 mL | 12.0514 mL | |
10 mM | 0.241 mL | 1.2051 mL | 2.4103 mL | 6.0257 mL | |
20 mM | 0.1205 mL | 0.6026 mL | 1.2051 mL | 3.0128 mL | |
50 mM | 0.0482 mL | 0.241 mL | 0.4821 mL | 1.2051 mL | |
100 mM | 0.0241 mL | 0.1205 mL | 0.241 mL | 0.6026 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
GSK2256098 1224887-10-8 Angiogenesis Apoptosis Cytoskeletal Signaling Tyrosine Kinase/Adaptors FAK Focal adhesion kinase PTK2 protein tyrosine kinase 2 GTPL 7939 GSK 2256098 Inhibitor GSK-2256098 GTPL-7939 GTPL7939 inhibit PTK2 inhibitor