1. Cell Cycle/DNA Damage Apoptosis
  2. Telomerase Apoptosis
  3. Imetelstat

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.

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

DNA, d(3'-amino-3'-deoxy-P-thio)(T-A-G-G-G-T-T-A-G-A-C-A-A), 5'-[O-[2-hydroxy-3-[(1-oxohexadecyl)amino]propyl] hydrogen phosphorothioate]

Imetelstat Chemical Structure

CAS No. : 868169-64-6

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Description

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[1][2].

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.

Apoptosis Analysis[2]

Cell Line: Myelofibrosis CD34+ cells; Cord
blood CD34+ cells
Concentration: 7.5 μM
Incubation Time: 2 days
Result: Did not induce Apoptosis of cord
blood CD341 cells; Increased the percentage of MF CD34+ Annexin V+ PI- cells.
In Vivo

Imetelstat (5-30 mg/kg; i.p.; 3 times weekly; 4-8 weeks) exerts a dose-dependent modest inhibitory effect on normal hematopoietic stem cells in sublethally irradiated NSG mice, with the 30 mg/kg dose causing the most significant reduction in normal hCD34+ cells[2].

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

Animal Model: NOD/SCID/IL2Rgnull (NSG) (8- to 9-week-old; sublethally irradiated)[2]
Dosage: 5 mg/kg; 15 mg/kg; 30 mg/kg
Administration: i.p.; 3 times weekly; 4 weeks or 8 weeks
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.
Clinical Trial
Molecular Weight

4610.00

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

[Imetelstat]

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
Purity & Documentation

Purity: 99.43%

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    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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Imetelstat
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HY-12854
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