| Identification | Back Directory | [Name]
TIMTEC-BB SBB005393 | [CAS]
72214-67-6 | [Synonyms]
TIMTEC-BB SBB005393
RRD-251 hydrochloride
Rb/Raf-1 Disruptor 251
Rb/Raf-1 disruptor 251 hydrochloride
S-(2,4-Dichlorobenzyl)-isothiouronium hydrochloride
[(2,4-dichlorobenzyl)thio]formamidine hydrochloride
2,4-dichlorobenzyl imidothiocarbamate hydrochloride
2,4-Dichlorobenzyl carbamimidothioate hydrochloride
2-(2,4-Dichlorobenzyl)-2-thiopseudourea hydrochloride
[(2,4-dichlorophenyl)methylthio]formamidine hydrochloride
(2,4-dichlorophenyl)methylsulfanylformamidine hydrochloride
(2,4-dichlorophenyl)methylsulfanylmethanimidamide hydrochloride
2-(2,4-Dichlorobenzyl)thiourea hydrochloride RRD-251 hydrochloride
(2,4-Dichlorophenyl)carbamimidothioic acid methyl ester hydrochloride | [Molecular Formula]
C8H9Cl3N2S | [MDL Number]
MFCD00035047 | [MOL File]
72214-67-6.mol | [Molecular Weight]
271.6 |
| Chemical Properties | Back Directory | [Melting point ]
222-227 °C | [storage temp. ]
room temp | [solubility ]
DMSO: >10mg/mL | [form ]
White solid | [color ]
white to off-white | [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 | [InChIKey]
COMNQRICZGJVLE-UHFFFAOYSA-N | [SMILES]
Cl.NC(=N)SCc1ccc(Cl)cc1Cl |
| Hazard Information | Back Directory | [Uses]
RRD-251 Hydrochloride is a reversible selective disruptor of Rb-Raf-1 interaction. | [Biological Activity]
RRD-251 hydrochloride is a reversiblepotentand 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. AlsoRRD-251 does not affect the kinase activities associated with cyclin Dcyclin E or Raf-1. | [in vivo]
RRD-251 (50 mg/kg; i.p.; q.o.d; for 14 days) has anti-cancer activities in vivo on melanomas[1].
| Animal Model: | 8-wk-old female athymic nude mice, with SK-ME-28 xenograft[1] | | Dosage: | 50 mg/kg | | Administration: | Intraperitoneal administration, qod, for 14 days | | Result: | Inhibits the growth of SK-ME-28 xenograft in nude mice. |
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| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
| Company Name: |
Carbosynth
|
| Tel: |
+86 512 6260 5585 |
| Website: |
www.carbosynth.com |
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