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

Metarrestin  (Synonyms: ML246)

Cat. No.: HY-120118 Purity: 99.96%
COA 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.

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

Metarrestin Chemical Structure

Metarrestin Chemical Structure

CAS No. : 1443414-10-5

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Solution
10 mM * 1 mL in DMSO USD 196 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
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Solid
5 mg USD 187 In-stock
10 mg USD 319 In-stock
25 mg USD 638 In-stock
50 mg USD 1089 In-stock
100 mg USD 1870 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].

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

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

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

Appearance

Solid

Formula

C31H30N4O
CAS No.
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 available by MCE.
Purity & Documentation
References
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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.

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Keywords:

Metarrestin1443414-10-5ML246ML 246ML-246DNA/RNA SynthesisorallyperinucleolarcompartmentnucleolartranscriptioneEF1A2metastaticPC3M-GFP-PTBPANC1PC3MHeLapancreaticbreastInhibitorinhibitorinhibit

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