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

Properties

• 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
• 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
• InChI key: COMNQRICZGJVLE-UHFFFAOYSA-N

Description

Biochem/physiol Actions

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.

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3