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DEL-22379

CAS号

181223-80-3

分子式

C26H28N4O3

主要靶点

Apoptosis|ERK

仅限科研使用

Cat No : CM03994

Print datasheet

Synonyms

Inhibitor|inhibit|Extracellular signal regulated kinases|ERK|DEL 22379|DEL22379|DEL-22379|Apoptosis

验证数据展示

  • CAS No.: 181223-80-3

    DEL-22379
    CAS#: 181223-80-3

产品信息

CAS号 181223-80-3
分子式 C26H28N4O3
主要靶点 Apoptosis|ERK
主要通路 MAPK 信号通路|凋亡
分子量 444.53
纯度 99.53%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 Inhibitor|inhibit|Extracellular signal regulated kinases|ERK|DEL 22379|DEL22379|DEL-22379|Apoptosis

靶点活性

ERK:0.5 μM

体内活性

DEL-22379（15 mg/kg，i.p.）在携带A375（BRAF突变）和HCT116（KRAS突变）肿瘤的小鼠中阻止了肿瘤生长和转移，但未能阻止注射CHL细胞（WT/WT）的小鼠中肿瘤的形成。[1]

体外活性

DEL-22379抑制了ERK二聚体的形成，但不影响其磷酸化。在携带突变BRAF (V600E)或RAS (Q61L或G12V)的人类细胞系中，DEL-22379显示出强大的抗增殖效果，并诱导凋亡。[1]

溶解度

DMSO:22.2 mg/mL (50 mM)

细胞实验

Cellular proliferation is analyzed by Alamar blue assays. Briefly, Cells are plated in 96-well plates at a density of 1000-2000 cells per well. Cells are treated with drug concentrations prepared by serial dilution ranging from 0.1 nM to 10 μM. 48 hr after drug treatment cells are exposed to Alamar Blue and the colorimetric change is measured at 570 and 600 nm. GI50 is estimated by nonlinear regression using GraphPad5 Prism Software.(Only for Reference)

参考文献

1.Herrero A, et al. Cancer Cell. 2015, 28(2), 170-182.

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