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Merck
CN

R7532

RRD-251 hydrochloride

≥98% (HPLC)

Synonym(s):

(2,4-Dichlorophenyl)carbamimidothioic acid methyl ester hydrochloride, 2-(2,4-Dichlorobenzyl)-2-thiopseudourea hydrochloride, Rb/Raf-1 disruptor 251 hydrochloride, S-(2,4-Dichlorobenzyl)-isothiouronium hydrochloride

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About This Item

Empirical Formula (Hill Notation):
C8H8Cl2N2S· HCl
CAS Number:
72214-67-6
Molecular Weight:
271.59
NACRES:
NA.77
PubChem Substance ID:
329823647
UNSPSC Code:
12352200
MDL number:
MFCD00035047

Key Documents

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InChI key

COMNQRICZGJVLE-UHFFFAOYSA-N

SMILES string

Cl.NC(=N)SCc1ccc(Cl)cc1Cl

InChI

1S/C8H8Cl2N2S.ClH/c9-6-2-1-5(7(10)3-6)4-13-8(11)12;/h1-3H,4H2,(H3,11,12);1H

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to off-white

solubility

DMSO: >10 mg/mL, H2O: >2 mg/mL

storage temp.

room temp

Quality Level

100

Biochem/physiol Actions

RRD-251 hydrochloride is a reversible, potent, and selective disruptor of Rb/Raf-1 interaction.
RRD-251 hydrochloride is a reversible, potent, and selective disruptor of Rb/Raf-1 interaction. The retinoblastoma tumor suppressor protein (Rb) controls the G1-S boundary by repressing the transcriptional activity of the E2F family of transcription factors. Raf-1 kinase binds and phosphorylates Rb early in the G1 phase. RRD-251 significantly inhibits angiogenesis and tumor growth in vivo in an Rb-dependent manner. RRD-251 does not inhibit the binding of B-Raf to Rb and Raf-1 to Mek1/2. Also, RRD-251 does not affect the kinase activities associated with cyclin D, cyclin E, or Raf-1.

Storage Class

11 - Combustible Solids

wgk

WGK 3

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Certificates of Analysis (COA)

Lot/Batch Number
059K4702V
030M4736V
059K47021
059K4702

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Sandeep Singh et al.
Molecular cancer therapeutics, 9(12), 3330-3341 (2010-12-09)
Metastatic melanoma is an aggressive cancer with very low response rate against conventional chemotherapeutic agents such as dacarbazine (DTIC). Inhibitor of Rb-Raf-1 interaction RRD-251 was tested against the melanoma cell lines SK-MEL-28, SK-MEL-5, and SK-MEL-2. RRD-251 was found to be
Debora Stelitano et al.
Oncotarget, 8(40), 67422-67438 (2017-10-06)
GTSE1 over-expression has been reported as a potential marker for metastasis in various types of malignancies, including breast cancer. Despite this, the transcriptional regulation of this protein and the causes of its misregulation in tumors remain largely unknown. The aims

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