1. MAPK/ERK Pathway
    Apoptosis
  2. Raf
    Apoptosis
  3. RRD-251

RRD-251 

Cat. No.: HY-117737A Purity: 99.55%
Handling Instructions

RRD-251 is an inhibitor of retinoblastoma tumor suppressor protein (Rb)-Raf-1 interaction, with potent anti-proliferative, anti-angiogenic and anti-tumor activities.

For research use only. We do not sell to patients.

RRD-251 Chemical Structure

RRD-251 Chemical Structure

CAS No. : 72214-67-6

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Description

RRD-251 is an inhibitor of retinoblastoma tumor suppressor protein (Rb)-Raf-1 interaction, with potent anti-proliferative, anti-angiogenic and anti-tumor activities[1].

IC50 & Target

Rb-Raf-1 interaction, apoptosis[1]

In Vitro

RRD-251 (10-50 μM; 24 hours) inhibits melanoma growth in-vitro[1].
RRD-251 (50 μM; 2 hours) inhibits Rb-Raf-1 interaction and Rb phosphorylation in non-small cell lung cancer cells[1].
RRD-251 induces apoptosis (50 μM; 18 hours) and cell cycle arrest (20-50 μM; 4 hours)[1].
RRD-251 alters the expression of cell cycle and apoptosis regulatory protein[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

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 Analysis[1]

Cell 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[1]

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[1]

Cell Line: SK-MEL-28 cells , SK-MEL-5 cells
Concentration: 20μM, 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.
In Vivo

RRD-251 (50 mg/kg; i.p.; qod, for 14 days) has anti-cancer activities in vivo on melanomas[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 8-wk-old female athymic nude mice, 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.
Molecular Weight

271.59

Formula

C₈H₉Cl₃N₂S

CAS No.

72214-67-6

SMILES

NC(SCC1=CC=C(Cl)C=C1Cl)=N.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
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Keywords:

RRD-251RRD251RRD 251RafApoptosisRaf kinasesmelanomaanticancerretinoblastomatumorsuppressorproteinRb-Raf-1Inhibitorinhibitorinhibit

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RRD-251
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