TAE226 (NVP-TAE226)

製品コードS2820 バッチS282002

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C23H25ClN6O3
分子量 468.94 CAS No. 761437-28-9
Solubility (25°C)* 体外 DMSO 47 mg/mL (100.22 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
0.5% methylcellulose
10.0mg/ml Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% methylcellulose clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 TAE226 (NVP-TAE226) is a potent FAK inhibitor with IC50 of 5.5 nM and modestly potent to Pyk2, ~10- to 100-fold less potent against InsR, IGF-1R, ALK, and c-Met. TAE226 (NVP-TAE226) induces apoptosis.
in vitro NVP-TAE226 (< 1 μM) inhibits extracellular matrix-induced autophosphorylation of FAK (Tyr397) in serum-starved U87 cells. NVP-TAE226 (< 1 μM) also inhibits IGF-I-induced phosphorylation of IGF-1R and activity of its downstream target genes such as MAPK and Akt in both U87 and U251 cells. NVP-TAE226 (<10 μM) retards tumor cell growth and attenuats G(2)-M cell cycle progression associated with a decrease in cyclin B1 and phosphorylated cdc2 (Tyr15) protein expression in both U87 and U251 cells. NVP-TAE226 (1 μM) inhibits tumor cell invasion by at least 50% compared with the control in an in vitro Matrigel invasion assay in glioma cell lines. NVP-TAE226 (1 μM) treatment of glioma cell lines containing wild-type p53 mainly exhibits G(2)-M arrest, whereas glioma cell lines bearing mutant p53 undergoes apoptosis, as evidence by detection of caspase-3/7 activation and poly(ADP-ribose) polymerase cleavage and by an Annexin V apoptosis assay. [1] NVP-TAE226 (5 μM) inhibits phosphorylation of FAK in the human neuroblastoma cell line SK-N-AS. NVP-TAE226 (<10 μM) treatment of the human neuroblastoma cell line SK-N-AS leads to decrease in cellular viability, cell cycle arrest, and an increase in apoptosis. [2] NVP-TAE226 (0.1 μM-10 μM) inhibits tube formation of HMEC1 cells. [3]
in vivo NVP-TAE226 (75 mg/kg) significantly increases the survival rate of mice bearing intracranial glioma xenografts. [1] NVP-TAE226 (100 mg/kg, oral) exerts significant decrease in microvessel density in a human colon cancer model in SCID mice. [3] NVP-TAE226 (100 mg/kg, oral) efficiently inhibits MIA PaCa-2 human pancreatic tumor growth without body weight loss in vivo model. [4] NVP-TAE226 inhibits 4T1 murine breast tumor growth and metastasis to the lung in a dose-dependent manner in vivo model, associated with inhibition of FAK autophosphorylation at Y397 and Akt phosphorylation at Serine473. [5]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 U87 and U251 cell lines
濃度 10 μM
反応時間 5 days
実験の流れ Cell cultures are harvested with 0.05% trypsin and seeded in triplicate at 2 × 104 in 24-well culture plates for 24 h before drug treatment. Culture medium is used for mock treatment. Cells are harvested at the indicated day after treatment, and viable cells are counted using the Vi-cell viability analyze
動物実験 動物モデル Male nude mice bearing intracranial glioma xenografts
投薬量 75 mg/kg
投与方法 Administered via oral gavage

カスタマーフィードバック

Data from [Cell Death Dis, 2014, 5, e1134]

Data from [Data independently produced by , , J Inorg Biochem, 2016, 160:225-35]

Data from [Data independently produced by , , Neurosci Lett, 2018, 672:96-102]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Overexpression of BACH1 mediated by IGF2 facilitates hepatocellular carcinoma growth and metastasis via IGF1R and PTK2 [ Theranostics, 2022, 12(3):1097-1116] PubMed: 35154476
Mechanical coupling of supracellular stress amplification and tissue fluidization during exit from quiescence [ Proc Natl Acad Sci U S A, 2022, 119(32):e2201328119] PubMed: 35914175
Integrin αvβ3 Induces HSP90 Inhibitor Resistance via FAK Activation in KRAS-Mutant Non-Small Cell Lung Cancer [ Cancer Res Treat, 2022, 54(3):767-781] PubMed: 34607394
Three subtypes of lung cancer fibroblasts define distinct therapeutic paradigms [ Cancer Cell, 2021, S1535-6108(21)00492-X] PubMed: 34624218
TLR4 signalling via Piezo1 engages and enhances the macrophage mediated host response during bacterial infection [ Nat Commun, 2021, 12(1):3519] PubMed: 34112781
Focal adhesion kinase inhibition synergizes with nab-paclitaxel to target pancreatic ductal adenocarcinoma [ J Exp Clin Cancer Res, 2021, 91-2021)] PubMed: None
Focal adhesion kinase inhibition synergizes with nab-paclitaxel to target pancreatic ductal adenocarcinoma [ J Exp Clin Cancer Res, 2021, 40(1):91] PubMed: 33750427
A first-in-class anticancer dual HDAC2/FAK inhibitors bearing hydroxamates/benzamides capped by pyridinyl-1,2,4-triazoles [ Eur J Med Chem, 2021, 222:113569] PubMed: 34111829
Campylobacter jejuni Triggers Signaling through Host Cell Focal Adhesions To Inhibit Cell Motility [ mBio, 2021, 12(4):e0149421] PubMed: 34425711
Modulation of Akt vs Stat3 activity by the focal adhesion kinase in non-neoplastic mouse fibroblasts [ Exp Cell Res, 2021, S0014-4827(21)00133-6] PubMed: 33957118

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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