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SI-2

Names

[ CAS No. ]:
380537-35-9

[ Name ]:
SI-2

[Synonym ]:
Ethanone, 1-(2-pyridinyl)-, 2-(1-methyl-1H-benzimidazol-2-yl)hydrazone, (1E)-
(1E)-N-(1-Methyl-1H-benzoimidazol-2-yl)-N'-(1-pyridin-2-yl-ethylidene)-hydrazine
(1E)-1-(2-Pyridinyl)ethanone 1-(1-methyl-1H-benzoimidazol-2-yl)-hydrazone
1-Methyl-2-{(2E)-2-[1-(2-pyridinyl)ethylidene]hydrazino}-1H-benzimidazole
SI-2

Biological Activity

[Description]:

SI-2 (EPH-116) is a potent small-molecule inhibitor of steroid receptor coactivator-3 (SRC-3 or AIB1) that can selectively inhibit the intrinsic transcriptional activities of SRC-3, also inhibits SRC-1 and SRC-2; selectively reduces cellular protein levels of SRC-3, but not that of CARM-1, blocks MDA-MB-468 cell growth with an IC50 value of 3.4 nM, but spares normal cells; significantly inhibit primary tumor growth and reduce SRC-3 protein levels in a breast cancer mouse model; "first-in-class" compound that targets oncogenic coactivator.

[References]

References 1. Song X, et al. Proc Natl Acad Sci U S A. 2016 May 3;113(18):4970-5. 2. Rohira AD, et al. Cancer Res. 2017 Aug 15;77(16):4293-4304. View Related Products by Target Other Targets

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
459.9±37.0 °C at 760 mmHg

[ Molecular Formula ]:
C15H15N5

[ Molecular Weight ]:
265.313

[ Flash Point ]:
231.9±26.5 °C

[ Exact Mass ]:
265.132751

[ LogP ]:
2.39

[ Vapour Pressure ]:
0.0±1.1 mmHg at 25°C

[ Index of Refraction ]:
1.659

[ Storage condition ]:
2-8°C

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds