URMC-099

产品说明书

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Chemical Structure| 1229582-33-5 同义名 : -
CAS号 : 1229582-33-5
货号 : A521108
分子式 : C27H27N5
纯度 : 99%+
分子量 : 421.54
MDL号 : MFCD28168077
存储条件：

Pure form Sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(83.03 mM)，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
生物活性
靶点

  • LRRK2

    LRRK2, IC50:11 nM

  • MLK1

    MLK1, IC50:19 nM

  • MLK3

    MLK3, IC50:14 nM

  • MLK2

    MLK2, IC50:42 nM
描述 The impact of URMC-099 (URMC099) on the in vitro proliferation of "brain homing" MDA-MB-231 BR cells expressing eGFP (eGFP8.4) and their parental cell line, MDA-MB-231, is assessed. Both cell groups are exposed to either 200 nM URMC-099 or vehicle alone. Cells treated with URMC-099 exhibit comparable growth rates to those treated with the vehicle. Cell viability exceeds 99% in all instances[2].
作用机制 URMC-099 inhibits MLK3 by interacting with MLK3 ATP binding site.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.37mL

0.47mL

0.24mL

11.86mL

2.37mL

1.19mL

23.72mL

4.74mL

2.37mL
参考文献

[1]Goodfellow VS, et al. Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. J Med Chem. 2013 Oct 24;56(20):8032-48.

[2]Rhoo KH, et al. Pharmacologic inhibition of MLK3 kinase activity blocks the in vitro migratory capacity of breast cancer cells but has no effect on breast cancer brain metastasis in a mouse xenograft model. PLoS One. 2014 Sep 29;9(9):e108487.