1. Apoptosis Metabolic Enzyme/Protease Others
  2. Phosphodiesterase (PDE) Apoptosis Isotope-Labeled Compounds
  3. Anagrelide-13C2,15N,d2

Anagrelide-13C2,15N,d2 is 15N and deuterated labeled Anagrelide (HY-B0523). Anagrelide is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36?nM). Anagrelide, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide inhibits bone marrow megakaryocytopoiesis. Anagrelide decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide is a platelet-lowering agent and plays in the antithrombopoietic action.

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

Anagrelide-<sup>13</sup>C<sub>2</sub>,<sup>15</sup>N,d<sub>2</sub> Chemical Structure

Anagrelide-13C2,15N,d2 Chemical Structure

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Description

Anagrelide-13C2,15N,d2 is 15N and deuterated labeled Anagrelide (HY-B0523). Anagrelide is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36?nM). Anagrelide, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide inhibits bone marrow megakaryocytopoiesis. Anagrelide decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide is a platelet-lowering agent and plays in the antithrombopoietic action[1][2][3].

In Vitro

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
Anagrelide potently inhibits the development of marrow megakaryocytes (IC50=26?nM)[2].
Anagrelide (0.05, 0.3, 1 μM; 12-day) inhibits only megakaryocytic cell growth not non-megakaryocytic cells[3].
Anagrelide (0.1-10000 nM) induces a cytotoxic effect in the GIST882 cell line[4].

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

In Vivo

Anagrelide (5 mg/kg/bid; for 10 days) inhibits or reduces tumor growth in GIST2B, GIST9, GIST882 model models[4].

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

Molecular Weight

262.11

Formula

C913C2H8D2Cl2N15NO

SMILES

O=[13C]1CC2NC3=C(C(Cl)=C(Cl)C=C3)C([2H])([2H])[15N]2[13CH2]1

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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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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Product Name:
Anagrelide-13C2,15N,d2
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HY-B0523S
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