Anagrelide-¹³C₂,¹⁵N,d₂

Cat. No.: HY-B0523S: FAQs
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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.

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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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1 mg		Get quote	Estimated Time of Arrival: December 31

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Other Forms of Anagrelide-¹³C₂,¹⁵N,d₂:

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Biological Activity
Purity & Documentation
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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. Anagrelide-¹³C₂,¹⁵N,d₂ Related Antibodies
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
Unlabeled CAS	68475-42-3
SMILES	O=[13C]1CC2NC3=C(C(Cl)=C(Cl)C=C3)C([2H])([2H])[15N]2[13CH2]1
Shipping	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation	Data Sheet (274 KB) Handling Instructions (2659 KB)
References	[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief] [2]. Guosu Wang, et al. Comparison of the biological activities of Anagrelide and its major metabolites in haematopoietic cell cultures. Br J Pharmacol. 2005 Oct;146(3):324-32. [Content Brief] [3]. Y Hong, et al. Comparison between Anagrelide and hydroxycarbamide in their activities against haematopoietic progenitor cell growth and differentiation: selectivity of Anagrelide for the megakaryocytic lineage. Leukemia. 2006 Jun;20(6):1117-22. [Content Brief] [4]. Olli-Pekka Pulkka, et al. Anagrelide for Gastrointestinal Stromal Tumor. Clin Cancer Res. 2019 Mar 1;25(5):1676-1687. [Content Brief]