428201

LDN-211904

LDN-211904 modulates the biological activity of EphB3 receptor tyrosine kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• 别名: LDN-211904, N-(2-chlorophenyl)-6-(piperidin-4-yl)imidazo[1,2-a]pyridine-3-carboxamide oxalate, EphB3 inhibitor, LDN-211904
• 经验公式（希尔记法）: C₂₁H₂₁ClN₄O₅
• CAS号: 1198408-78-4
• 分子量: 444.87
• MDL號碼: MFCD28023573
• 分類程式碼代碼: 12352200
• NACRES: NA.77

属性

• 品質等級: 100
• 化驗: ≥99% (HPLC)
• 形狀: solid
• 效力: 79 nM IC₅₀
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: off-white
• 溶解度: DMSO: 50 mg/mL, clear, nearly colorless
• 運輸包裝: ambient
• 儲存溫度: 2-8°C
• SMILES 字串: O=C(NC1=CC=CC=C1Cl)C2=CN=C3C=CC(C4CCNCC4)=CN32.OC(C(O)=O)=O

说明

一般說明

A pyrazolo[1,5-a]pyridine derivative that acts as an potent and reversible EphB3 receptor tyrosine kinase inhibitor with an IC₅₀ of 79 nM with good mouse liver microsomal stability and aqueous solubility. Shown to suppress EphB3-induced autophosphorylation of EphB3 receptor at 10 µM in cells. When profiled against a panel of 288 kinases at 5 µM, found to also inhibit most of the Eph (Erythropoietin-producing hepatocellular carcinoma) receptor kinases including EphA1, EphA2, EphA3, EphA4, EphA5, EphA8, EphB1, EphB2, EphB3, EphB4 and other tyrosine kinases, but not EphA6 and EphA7, and is non-inhibitory towards non-RTK kinases screened except for p38α, p38β, and Qik.

生化／生理作用

Cell permeable: yes

Primary Target
Erythropoietin-producing hepatocellular carcinoma (Eph)

Reversible: yes

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他說明

Qiao, L., et al. 2011, Bioorg. Med. Chem. Lett.19, 6122

法律資訊

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

安全信息

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 2
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable