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DEL-22379

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Chemical Structure| 181223-80-3 同义名 : -
CAS号 : 181223-80-3
货号 : A315608
分子式 : C26H28N4O3
纯度 : 98%
分子量 : 444.526
MDL号 : MFCD00950163
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(236.21 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • ERK5

    ERK, IC50:0.5 μM

  • ERK

    ERK, IC50:0.5 μM
描述 The extracellular regulated protein kinases (ERK) play important roles in regulating cellular proliferation and survival. DEL-22379 is a small molecule inhibitor of ERK dimerization with an IC50 value of ~0.5μM. It inhibited ERK dimerization in DLD1 (KRAS mutant), RKO (BRAF mutant) and T47D (WT/WT) cell lines at concentrations of 0.1-10μM. Treatment with DEL-22379 (10μM) for 12 h induced apoptosis in tumor cell lines harboring oncogenic RAS or BRAF. In mouse xenograft models, the treatment with DEL-22379 (15mg/kg/day) for 15 days significantly inhibited the progression of tumors derived from A375 cells (BRAF mutant) but not in mice injected with CHL cells (WT/WT). In a mouse model of BRAF mutant colorectal cancer patient-derived xenograft, the treatment with DEL-22379 (15mg/kg/day) for 21 days markedly suppressed tumor growth compared to the control group[2].
作用机制 DEL-22379 inhibits ERK dimerization by binding to ERK2 within the dimerization interface[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.25mL

0.45mL

0.22mL

11.25mL

2.25mL

1.12mL

22.50mL

4.50mL

2.25mL
参考文献

[1]Herrero A, Pinto A, et al. Small Molecule Inhibition of ERK Dimerization Prevents Tumorigenesis by RAS-ERK Pathway Oncogenes. Cancer Cell. 2015 Aug 10;28(2):170-82.

[2]Herrero A, Pinto A, Colón-Bolea P, et al. Small Molecule Inhibition of ERK Dimerization Prevents Tumorigenesis by RAS-ERK Pathway Oncogenes. Cancer Cell. 2015;28(2):170-182. doi:10.1016/j.ccell.2015.07.001