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.
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- Pureté : 99.43%
- CAS No.: 868169-64-6
- Masse moléculaire:4610.00
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
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.
In Vivo
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.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 868169-64-6
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Appearance Solid
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Masse moléculaire 4610.00
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Color White to off-white
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SMILES
[Imetelstat]
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Synonyms
GRN163L
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
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Fiche technique (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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Instruction de manipulation (2242 KB)
Références
[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
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Imetelstat Related Classifications
HY-12854 Related Classifications
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