Metarrestin (Synonyms: ML246) |
カタログ番号GC38201
One-Click Copy Product Info
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メタレスチン (ML246) は、経口で活性なファーストインクラスの特定の核周囲コンパートメント阻害剤です。メタレスチンは、翻訳伸長因子 eEF1A2 と相互作用することにより、核小体構造を破壊し、RNA ポリメラーゼ (Pol) I 転写を少なくとも部分的に阻害します。メタレスチンは、マウス癌モデルの転移発生をブロックし、生存期間を延長します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1443414-10-5
Sample solution is provided at 25 µL, 10mM.
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Metarrestin (ML246) disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2. Metarrestin is a first-in-class perinucleolar compartment inhibitor with a favorable PK profile, which effectively suppresses metastasis[1][2].
[1]. Vilimas T, et al. Pharmacokinetic evaluation of the PNC disassembler metarrestin in wild-type and Pdx1-Cre;LSL-KrasG12D/+;Tp53R172H/+ (KPC) mice, a genetically engineered model of pancreatic cancer. Cancer Chemother Pharmacol. 2018 Dec;82(6):1067-1080. [2]. Frankowski KJ, et al. Metarrestin, a perinucleolar compartment inhibitor, effectively suppresses metastasis. Sci Transl Med. 2018 May 16;10(441).
| Cas No. | 1443414-10-5 | SDF | |
| 同義語 | ML246 | ||
| Canonical SMILES | O[C@H]1CC[C@H](N(C=NC2=C3C(C4=CC=CC=C4)=C(C5=CC=CC=C5)N2CC6=CC=CC=C6)C3=N)CC1 | ||
| Formula | C31H30N4O | M.Wt | 474.6 |
| 溶解度 | DMSO: 31.25 mg/mL (65.84 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.107 mL | 10.5352 mL | 21.0704 mL |
| 5 mM | 421.4 μL | 2.107 mL | 4.2141 mL |
| 10 mM | 210.7 μL | 1.0535 mL | 2.107 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 32 reference(s) in Google Scholar.)