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RRD-251

Names

[ CAS No. ]:
131916-62-6

[ Name ]:
RRD-251

[Synonym ]:
MFCD01242444
2,4-Dichlorobenzyl carbamimidothioate hydrochloride (1:1)
Rb/Raf-1 disruptor 251 hydrochloride
S-(2,4-Dichlorobenzyl)-isothiouronium hydrochloride
Rrd-251 hydrochloride
2-(2,4-Dichlorobenzyl)-2-thiopseudourea hydrochloride
MFCD00035047
(2,4-Dichlorophenyl)carbamimidothioic acid methyl ester hydrochloride
Carbamimidothioic acid, (2,4-dichlorophenyl)methyl ester, hydrochloride (1:1)

Biological Activity

[Description]:

RRD-251 hydrochloride is a small molecule disruptor of Rb/Raf-1 interaction, potently and selectively disrupts the Rb/Raf-1 (IC50=77 nM) but not Rb/E2F, Rb/prohibitin, Rb/cyclin E, and Rb/HDAC binding; inhibits Rb to recruit Raf-1 to proliferative promoters and inhibited E2F1-dependent transcriptional activity; inhibits anchorage-dependent and anchorage-independent growth of human cancer cells; significantly inhibits tumor growth in tumors with functional Rb in vivo.

[References]

References 1. Kinkade R, et al. Cancer Res. 2008 May 15;68(10):3810-8. 2. Singh S, et al. Mol Cancer Ther. 2010 Dec;9(12):3330-41. 3. Treviño JG, et al. Mol Cancer Ther. 2013 Dec;12(12):2722-34. 4. Wallace AS, et al. Oncotarget. 2016 Jul 19;7(29):46401-46418. View Related Products by Target Raf

Chemical & Physical Properties

[ Molecular Formula ]:
C8H8Cl2N2S

[ Molecular Weight ]:
271.595

[ Exact Mass ]:
269.955200

Related Compounds