基本信息

分子量
284.01

基本信息

产品性质

安全信息

产品说明

一般描述

A cell-permeable tetraamine compound that is identified from a computer-aided molecular docking screening based on Fak Y397 interaction and is shown to inhibit FAK (Cat. No. 324876) autophosphorylation as well as its kinase activity toward paxillin phosphorylation both in cell-free kinase assays (IC₅₀<1 µM) and in BT474 breast cancer cultures, while exhibiting little activity against Pyk2 (Cat. No. 662067) autophosphorylation or the kinase activity of c-Raf, c-Src, EGFR, VEGFR-3, IGF-1, Met, PDGFR-α, Pyk2, and PI 3-K (p110δ/p85α). Reported to inhibit BT474 proliferation both in cultures in vitro (IC₅₀ ~10 µM) and in mice in vivo (~25% of no treatment controls on day 23; 30 mg/kg via 5 i.p/wk).
A cell-permeable tetraamine compound that is identified from a computer-aided molecular docking screening based on Fak Y397 interaction and is shown to inhibit FAK autophosphorylation as well as its kinase activity toward paxillin phosphorylation both in cell-free kinase assays (IC₅₀<1 M) and in BT474 breast cancer cultures, while exhibiting little activity against Pyk2 autophosphorylation or the kinase activity of c-Raf, c-Src, EGFR, VEGFR-3, IGF-1, Met, PDGFR-α, Pyk2, and PI 3-K (p110δ/p85α). Reported to inhibit BT474 proliferation both in cultures in vitro (IC₅₀ ~10 M) and in mice in vivo (~25% of no treatment controls on day 23; 30 mg/kg via 5 i.p/wk).

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Golubovskaya, V.M., et al. 2008. J. Med. Chem.51, 7405.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

产品性质

安全信息

产品说明

应用

FAK 抑制剂 14 已用于肿瘤转移试验。它还用于研究其对骨形态发生蛋白 7(BMP-7)诱导的细胞迁移和粘附的影响。

包装

10, 50 mg in glass bottle

生化/生理作用

1，2，4，5-苯四胺四盐酸盐(FAK 抑制剂14；Y15)是一种细胞可透过性选择性粘着斑激酶(FAK)抑制剂。粘着斑激酶(FAK)在调节整联蛋白信号传导途径中是必需的，该信号通路主要负责调节细胞存活、细胞增殖和细胞运动。FAK 酪氨酸 397(Y397)磷酸化形成与Src 家族激酶/ PI3 激酶的 SH2 结构域具有高亲和力的结合位点。FAK 在许多人类肿瘤中过表达。1，2，4，5-苯四胺四盐酸盐(FAK 抑制剂14，Y15)阻断 Y397-FAK 的磷酸化，导致神经母细胞瘤细胞脱落和凋亡。

特点和优势

这种化合物是激酶磷酸酶生物学研究的特色产品。点击此处发现更多特色激酶磷酸酶生物产品。在sigma.com/discover-bsm可了解更多关于生物活性小分子的其他研究领域。
该化合物出现在受体分类和信号转导手册的Fak页，点击此处。

基本信息

产品性质

安全信息

基本信息

安全信息

图形或危害标志
危险性说明	H315: Causes skin irritation. H319: Causes serious eye irritation. H335: May cause respiratory irritation.
防范说明	P233: Keep container tightly closed. P260: Do not breathe . P261: Avoid breathing . P264: Wash hands thoroughly after handling. P271: Use only outdoors or in a well-ventilated area. P280: Wear . P302 + P352: IF ON SKIN: Wash with plenty of soap and water. P304: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing.. P304 + P340: IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P305 + P351 + P338: IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. P312: Call a POISON CENTER or doctor/physician if you feel unwell. P321: Specific treatment (see relevant procedures. on this label). P332 + P313: If skin irritation occurs: Get medical advice/ attention. P337 + P313: If eye irritation persists: Get medical advice/attention. P340: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P362: Take off contaminated clothing and wash before reuse. P403: Store in a well-ventilated place. P403 + P233: Store in a well-ventilated place. Keep container tightly closed. P405: Store locked up. P501: Dispose of contents/container to in accordance with local regulation .