1. Cell Cycle/DNA Damage
  2. DNA/RNA Synthesis
  3. Metarrestin

Metarrestin (Synonyms: ML246)

Cat. No.: HY-120118 Purity: 99.85%
Handling Instructions

Metarrestin (ML246) is an orally active, first-in-class and specific perinucleolar compartment inhibitor. Metarrestin disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2. Metarrestin blocks metastatic development and extends survival in mouse cancer models.

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Metarrestin Chemical Structure

Metarrestin Chemical Structure

CAS No. : 1443414-10-5

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1  mL in DMSO USD 178 In-stock
Estimated Time of Arrival: December 31
5 mg USD 170 In-stock
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10 mg USD 290 In-stock
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25 mg USD 580 In-stock
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50 mg USD 990 In-stock
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100 mg USD 1700 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Metarrestin (ML246) is an orally active, first-in-class and specific perinucleolar compartment inhibitor. Metarrestin disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2. Metarrestin blocks metastatic development and extends survival in mouse cancer models[1][2].

IC50 & Target

Perinucleolar compartment[1]

In Vitro

Metarrestin (ML246) disrupts perinucleolar compartments in PC3M-GFP-PTB cells with an IC50 of 0.39 μM[2].
Metarrestin (1 μM; 24 hours) reduces perinucleolar compartment prevalence in different human cancer cell lines. Metarrestin impacts cell growth in cancer cell line PC3M but not in normal fibroblasts (GM02153)[2].
Metarrestin (0.6 μM; 24 hours) effectively blocks the invasion of PC3M and PANC1 cells[2].
Metarrestin (1 μM; 24 hours) does not significantly change the amounts of Pol I large subunit RPA194 and UBF in the three cell lines, PANC1, PC3M, and HeLa. Metarrestin shows a substantial reduction of 5’ETS RNA in cells[2].

In Vivo

Metarrestin (ML246; 5-25 mg/kg; IP; once daily; continuing for six weeks) displays a decrease in metastatic burden in both liver (p <0.01) and lung with 25 mg/kg[2].
Metarrestin (drug-infused chow; 10 mg/kg; 70 ppm) extends survival in the NSG PANC1 pancreatic cancer metastasis mice model[2].
Metarrestin (5, 25 mg/kg; ip; for 4 additional week) reduces metastasis of prostate cancer (PC3M) and growth of metastatic breast cancer PDX mice models[2].
Metarrestin (5 and 25 mg/kg; IP) has a half-life of 4.6 to 5.5 hours[2].

Animal Model: NOD/IL2 gamma (null) PANC1 mice over primary tumor tissues[2]
Dosage: 5 and 25 mg/kg
Administration: IP; once daily; continuing for six weeks
Result: Displayed a decrease in metastatic burden in both liver (p <0.01) and lung with 25 mg/kg.
Demonstrated a significant reduction of perinucleolar compartment prevalence in metastatic and primary tumor tissues.
Animal Model: Female BALB/c mice[2]
Dosage: 5 and 25 mg/kg (Pharmacokinetic Analysis)
Administration: IP
Result: Indicated good exposure, distribution, and tolerability in vivo, with a half-life of 4.6 to 5.5 hours.
Clinical Trial
Molecular Weight

474.60

Formula

C₃₁H₃₀N₄O

CAS No.

1443414-10-5

SMILES

O[[email protected]]1CC[[email protected]](N(C=NC2=C3C(C4=CC=CC=C4)=C(C5=CC=CC=C5)N2CC6=CC=CC=C6)C3=N)CC1

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
Solvent & Solubility
In Vitro: 

DMSO : 31.25 mg/mL (65.84 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1070 mL 10.5352 mL 21.0704 mL
5 mM 0.4214 mL 2.1070 mL 4.2141 mL
10 mM 0.2107 mL 1.0535 mL 2.1070 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.08 mg/mL (4.38 mM); Suspended solution; Need ultrasonic

*All of the co-solvents are provided by MCE.
References
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Keywords:

MetarrestinML246ML 246ML-246DNA/RNA SynthesisorallyperinucleolarcompartmentnucleolartranscriptioneEF1A2metastaticPC3M-GFP-PTBPANC1PC3MHeLapancreaticbreastInhibitorinhibitorinhibit

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Metarrestin
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