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RRD-251

Catalog No. T60475 CAS 72214-67-6

RRD-251 is an Rb-Raf-1 interaction inhibitor that induces apoptosis in metastatic melanoma cells and synergizes with dacarbazine[1].

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RRD-251, CAS 72214-67-6

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Description	RRD-251 is an Rb-Raf-1 interaction inhibitor that induces apoptosis in metastatic melanoma cells and synergizes with dacarbazine[1].
In vitro	RRD-251, at concentrations ranging from 10-50 µM over 24 hours, effectively inhibits melanoma growth in vitro, as demonstrated through Cell Proliferation Assays conducted on SK-MEL-28, SK-MEL-5, and SK-MEL-2 cells. Additionally, at a concentration of 50 µM for 2 hours, it disrupts the interaction between Rb and Raf-1 and reduces Rb phosphorylation in non-small cell lung cancer cells, indicative of its ability to hinder cell cycle progression and promote apoptosis, as further evidenced by Western Blot Analysis which showed reduced phosphorylated-Rb levels. Furthermore, with a concentration of 50 µM over 18 hours, RRD-251 triggers apoptosis and at 20-50 µM for 4 hours, it induces cell cycle arrest in a dose-dependent manner in SK-MEL-28 and SK-MEL-5 cells, altering the expression of key proteins regulating the cell cycle and apoptosis, as highlighted in Apoptosis Analysis and Cell Cycle Analysis reports. These findings underscore RRD-251's potential as a therapeutic agent in the treatment of melanoma and non-small cell lung cancer by modifying crucial cellular processes.
In vivo	RRD-251, administered at a dosage of 50 mg/kg intraperitoneally every other day for a duration of 14 days, exhibits anti-cancer effects in vivo, specifically targeting melanomas. This was observed in an animal model using 8-week-old female athymic nude mice implanted with SK-ME-28 xenografts. The result was a significant inhibition of SK-ME-28 xenograft growth in the mice.

Molecular Weight	271.59
Formula	C8H9Cl3N2S
CAS No.	72214-67-6

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

RRD-251 72214-67-6 inhibitor inhibit

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