Anagrelide
Modify Date: 2024-01-03 14:53:20
Anagrelide structure
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Common Name | Anagrelide | ||
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| CAS Number | 68475-42-3 | Molecular Weight | 256.088 | |
| Density | 1.8±0.1 g/cm3 | Boiling Point | 376.5±52.0 °C at 760 mmHg | |
| Molecular Formula | C10H7Cl2N3O | Melting Point | 280 °C | |
| MSDS | N/A | Flash Point | 181.5±30.7 °C | |
Use of AnagrelideAnagrelide, an inhibitor of phosphodiesterase type III (PDEIII) (IC50=36 nM), inhibits platelet production. Anagrelide, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide plays in the antithrombopoietic action. The platelet-lowering agent[1]. |
| Name | anagrelide |
|---|---|
| Synonym | More Synonyms |
| Description | Anagrelide, an inhibitor of phosphodiesterase type III (PDEIII) (IC50=36 nM), inhibits platelet production. Anagrelide, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide plays in the antithrombopoietic action. The platelet-lowering agent[1]. |
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| Related Catalog | |
| Target |
PDEIII[1] |
| In Vitro | Anagrelide potently inhibits the development of marrow megakaryocytes (IC50=26 nM)[1]. Anagrelide is a distinct pharmacological agent that inhibit bone marrow megakaryocytopoiesis. Anagrelide (0.05, 0.3, 1 µM) inhibits only megakaryocytic cell growth not non-megakaryocytic cells. Anagrelide shifts cell growth to the non-megakaryocytic compartment, an effect that suggested that it was devoid of cytotoxic activity[2]. Anagrelide induces a cytotoxic effect in the GIST882 cell line at a submicromolar concentration (IC50= 16 nM), but Anagrelide is only weakly active in the GIST48 cell line[3].Anagrelide decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro[3]. Cell Proliferation Assay[2] Cell Line: Megakaryocytic and non-megakaryocytic cells Concentration: 0.05, 0.3, 1 µM Incubation Time: 12-day Result: Inhibited only megakaryocytic cell growth at every concentration tested |
| In Vivo | Anagrelide is effective in a GIST xenograft mouse model with KIT exon 9 mutation that may pose a therapeutic challenge, as these GISTs require a high daily dose of Imatinib[3].Anagrelide inhibits GIST growth in patient-derived mouse xenograft models. Anagrelide has therapeutic value in the treatment of GIST.Anagrelide has antitumoral activity in GIST xenograft models[3]. Anagrelide (5 mg/kg/bid) inhibits or reduces tumor growth in GIST2B, GIST9, GIST882 model models[3]. Animal Model: Adult female athymic mice bearing GIST2B, GIST3, GIST9, GIST882 model[3] Dosage: 5 mg/kg/bid Administration: Treated with 5 mg/kg/bid or with the combination of Anagrelide and Imatinib (given at the same dose and schedule as the single agents); for 10 days Result: Inhibited or reduced tumor growth in three (GIST2B, GIST9, GIST882) of these four models. The most potent effect was observed in the GIST2B model that harbors a KIT exon 9 mutation leading to p.A502_Y503 duplication. Reduced the tumor volume 68% after 10 days of therapy in this model. |
| References |
| Density | 1.8±0.1 g/cm3 |
|---|---|
| Boiling Point | 376.5±52.0 °C at 760 mmHg |
| Melting Point | 280 °C |
| Molecular Formula | C10H7Cl2N3O |
| Molecular Weight | 256.088 |
| Flash Point | 181.5±30.7 °C |
| Exact Mass | 254.996613 |
| PSA | 44.70000 |
| LogP | 1.96 |
| Vapour Pressure | 0.0±0.9 mmHg at 25°C |
| Index of Refraction | 1.791 |
| Storage condition | 2-8°C |
| Water Solubility | slightly soluble |
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATAACUTE TOXICITY DATA
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| Safety Phrases | S3-S7 |
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| RIDADR | 3163 |
| Hazard Class | 2.2 |
| HS Code | 2933990090 |
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Anagrelide CAS#:68475-42-3 |
| Literature: US5391737 A1, ; |
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Anagrelide CAS#:68475-42-3 |
| Literature: US5391737 A1, ; |
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Anagrelide CAS#:68475-42-3 |
| Literature: WO2008/96145 A1, ; Page/Page column 14 ; |
![ethyl 2-[5,6-dichloro-2-(cyanoamino)-4H-quinazolin-3-yl]acetate structure](https://image.chemsrc.com/caspic/095/146374-56-3.png)
| Precursor 2 | |
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| DownStream 1 | |
CAS#:58579-51-4| HS Code | 2933990090 |
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| Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
| [14C]-Anagrelide |
| BL 4162A |
| Anagrelide (INN/BAN) |
| 6,7-di-chloro-1,5-dihydroimidazo[2,1-b]quinazolin-2[3 H ]-one base |
| Imidazo[2,1-b]quinazolin-2(3H)-one, 6,7-dichloro-5,10-dihydro- |
| Anagrelida |
| UNII-K9X45X0051 |
| 6,7-Dichloro-1,5-dihydroimidazo[2,1-b]quinazolin-2(3H)-one |
| Anagrelide |
| 6,7-Dichloro-5,10-dihydroimidazo[2,1-b]quinazolin-2(3H)-one |
| Anagrelidum |
| 6,7-dichloro-5,10-dihydro-3H-imidazo[2,1-b]quinazolin-2-one |
| Anagrelidum [INN-Latin] |
| Agrelin |
| MFCD00866794 |
| 6,7-dichloro-1,5-dihydro-imidazo[2,1-b]quinazolin-2-one |
| 6,7-Dichloro-1,2,3,5-tetrahydroimidazo[2,1-b]quinazolin-2-one |
| Anagrelida [INN-Spanish] |