RRD-251 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

RRD-251 盐酸盐是 Rb/Raf-1 相互作用的小分子破坏剂，有效且选择性地破坏 Rb/Raf-1 (IC50=77 nM)。

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.

RRD-251 (10-50 μM; 24 hours) inhibits melanoma growth in-vitro.RRD-251 (50 μM; 2 hours) inhibits Rb-Raf-1 interaction and Rb phosphorylation in non-small cell lung cancer cells. RRD-251 induces apoptosis (50 μM; 18 hours) and cell cycle arrest (20-50 μM; 4 hours).RRD-251 alters the expression of cell cycle and apoptosis regulatory protein. Cell Proliferation Assay Cell Line:SK-MEL-28 cells , SK-MEL-5 cells, SK-MEL-2 cells Concentration:10 μM, 20 μM, 50 μM Incubation Time:24 hours Result:Inhibited melanoma growth in-vitro.Western Blot AnalysisCell Line:SK-MEL-28 cells , SK-MEL-5 cells, SK-MEL-2 cells Concentration:50 μM Incubation Time:2 hours Result:Showed the depletion of phosphorylated-Rb in RRD-251 treated cells.Apoptosis Analysis Cell Line:SK-MEL-28 cells , SK-MEL-5 cells, SK-MEL-2 cells Concentration:50 μM Incubation Time:18 hours Result:Induced apoptosis.Cell Cycle Analysis Cell Line:SK-MEL-28 cells , SK-MEL-5 cells Concentration:20 μM, 50 μM Incubation Time:4 hours Result:Resulted in a dose dependent inhibition of cell cycle progression in SK-MEL-28 and SK-MEL-5 cells, respectively.

RRD-251 (50 mg/kg; i.p.; q.o.d; for 14 days) has anti-cancer activities in vivo on melanomas. Animal Model:8-wk-old female athymic nude mice, with SK-ME-28 xenograft Dosage:50 mg/kg Administration:Intraperitoneal administration, qod, for 14 days Result:Inhibits the growth of SK-ME-28 xenograft in nude mice.

RRD251 hydrochloride

MAPK/ERK Signaling

Raf

Raf

——

——

72214-67-6

271.584

C8H9Cl3N2S

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (460.25 mM)

C1=CC(=C(C=C1Cl)Cl)CSC(=N)N.Cl

Carbamimidothioic acid, (2,4-dichlorophenyl)methyl ester, monohydrochloride (9CI)

(-20℃)

With Ice Pack

≥ 2 years