Imetelstat
Based on 1 Customer Validation
Imetelstat (GRN163L) is a 13-mer oligonucleotide and competitive Telomerase inhibitor. Imetelstat binds with high affinity to the template region of the RNA component of human telomerase. Imetelstat induces Apoptosis. Imetelstat is capable of selectively eliminating myelofibrosis hematopoietic stem cells. Imetelstat leads to the loss of a cancer cell's ability to maintain telomere length, resulting in the inhibition of cell proliferation.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.43%
- CAS 番号: 868169-64-6
- 分子量:4610.00
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
体外実験
Imetelstat is a telomerase inhibitor that leads to the loss of a cancer cell's ability to maintain telomere length, resulting in the inhibition of cell proliferation[1].
Imetelstat (1.8-7.5 μM; 2-7 d) inhibits proliferation of primary myelofibrosis CD34+ cells, induces apoptosis but has no significant effect on normal cord blood CD34+ cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Myelofibrosis CD34+ cells; Cord
blood CD34+ cells -
Concentration:7.5 μM
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Incubation Time:2 days
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Result:Did not induce Apoptosis of cord
blood CD341 cells; Increased the percentage of MF CD34+ Annexin V+ PI- cells.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD/SCID/IL2Rgnull (NSG) (8- to 9-week-old; sublethally irradiated)[2]
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Dosage:5 mg/kg; 15 mg/kg; 30 mg/kg
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Administration:i.p.; 3 times weekly; 4 weeks or 8 weeks
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Result:Resulted in a 15.4% reduction in the number of hCD34+ cells at 15 mg/kg for 8 weeks.\nDid not result in a greater reduction in hCD45+ or hCD34+ cells at 30 mg/kg for 8 weeks.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 868169-64-6
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性状 Solid
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分子量 4610.00
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Color White to off-white
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SMILES
[Imetelstat]
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別名
GRN163L
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
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データシート (270 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2242 KB)
参考文献
[1]. Lennox AL, et al. Imetelstat, a novel, first-in-class telomerase inhibitor: Mechanism of action, clinical, and translational science. Clin Transl Sci. 2024;17(11):e70076. [Content Brief]
[2]. Wang X, et al. Imetelstat, a telomerase inhibitor, is capable of depleting myelofibrosis stem and progenitor cells. Blood Adv. 2018;2(18):2378-2388. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)