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

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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Based on 1 publication(s) in Google Scholar

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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].

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

RRD-251 Related Antibodies

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: 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.
In Vivo

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

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

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.
Molecular Weight

271.59

Formula

C8H9Cl3N2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (460.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6820 mL 18.4101 mL 36.8202 mL
5 mM 0.7364 mL 3.6820 mL 7.3640 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.94%

COA (247 KB) HNMR (248 KB) LCMS (257 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6820 mL 18.4101 mL 36.8202 mL 92.0505 mL
5 mM 0.7364 mL 3.6820 mL 7.3640 mL 18.4101 mL
10 mM 0.3682 mL 1.8410 mL 3.6820 mL 9.2051 mL
15 mM 0.2455 mL 1.2273 mL 2.4547 mL 6.1367 mL
20 mM 0.1841 mL 0.9205 mL 1.8410 mL 4.6025 mL
25 mM 0.1473 mL 0.7364 mL 1.4728 mL 3.6820 mL
30 mM 0.1227 mL 0.6137 mL 1.2273 mL 3.0684 mL
40 mM 0.0921 mL 0.4603 mL 0.9205 mL 2.3013 mL
50 mM 0.0736 mL 0.3682 mL 0.7364 mL 1.8410 mL
60 mM 0.0614 mL 0.3068 mL 0.6137 mL 1.5342 mL
80 mM 0.0460 mL 0.2301 mL 0.4603 mL 1.1506 mL
100 mM 0.0368 mL 0.1841 mL 0.3682 mL 0.9205 mL
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RRD-251 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

RRD-25172214-67-6RRD251RRD 251RafApoptosisRaf kinasesmelanomaanticancerretinoblastomatumorsuppressorproteinRb-Raf-1Inhibitorinhibitorinhibit

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