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/ PDE / Anagrelide HCl/盐酸阿那格雷

Anagrelide HCl/盐酸阿那格雷 {[allProObj[0].p_purity_real_show]}

货号：A139945 同义名： BL4162A; Anagrelide (hydrochloride)

Anagrelide hydrochloride (BL4162A) 为高效 III 型磷酸二酯酶 (PDE3) 抑制剂，IC50 达 36 nM；作为咪唑并喹唑啉衍生物，可阻断血小板聚集，抑制骨髓巨核细胞生成。体外实验显示，该化合物能抑制胃肠道间质瘤 (GIST) 细胞增殖并诱导其凋亡，同时兼具降低血小板水平及抗血栓形成活性。

Anagrelide HCl/盐酸阿那格雷 化学结构 CAS号：58579-51-4
Anagrelide HCl/盐酸阿那格雷 化学结构
CAS号：58579-51-4
Anagrelide HCl/盐酸阿那格雷 3D分子结构
CAS号：58579-51-4
Anagrelide HCl/盐酸阿那格雷 化学结构 CAS号：58579-51-4
Anagrelide HCl/盐酸阿那格雷 3D分子结构 CAS号：58579-51-4
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Anagrelide HCl/盐酸阿那格雷 纯度/质量文件 产品仅供科研

货号：A139945 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
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• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
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更多 >
产品名称 PDE ↓ PDE1 ↓ PDE10A ↓ PDE2 ↓ PDE3 ↓ PDE4 ↓ PDE5 ↓ PDE6 ↓ 其他靶点 纯度
Doxofylline ✔ 99+%
Deltarasin +++

PDEδ , Kd: 38 nM

 		95%
7-(2,3-Dihydroxypropyl)theophylline ✔ 98%
Aminophylline +

PDE, IC50: 0.12 mM

 		98+%
Anagrelide HCl ✔ 99%+
Irsogladine ✔ mAChR,AChR 99%
PF-8380 +++

Autotaxin, IC50: 2.8 nM

 		99%+
Dipyridamole ✔ 98%
Balipodect ++++

PDE10A, IC50: 0.3 nM

 		99%+
Luteolin +

PDE1, Ki: 15.0 μM

 		++

PDE2, Ki: 6.4 μM

 		+

PDE3, Ki: 13.9 μM

 		+

PDE4, Ki: 11.1 μM

 		+

PDE5, Ki: 9.5 μM

 		98%
Milrinone ++

PDE2, IC50: 5.2 μM

 		++

PDE3, IC50: 2.1 μM

 		ATPase 99%
Pimobendan ++

PDE3, IC50: 0.32 μM

 		98%
Cilostazol ++

PDE3, IC50: 0.2 μM

 		98%
Fenspiride HCl +

PDE3, pIC50: 3.44

 		+

PDE4, pIC50: 4.16

 		99% (HPLC)
(S)-(+)-Rolipram ++

PDE4, IC50: 0.75 μM

 		99% (HPLC)
Apremilast +++

PDE4, IC50: 74 nM

 		98%
GSK256066 ++++

PDE4B, IC50: 3.2 pM

 		98+%
Roflumilast ++++

PDE4A1, IC50: 0.7 nM

PDE4A4, IC50: 4.3 nM

 		99%
Rolipram +++

PDE4B, IC50: 130 nM

 		99%+
Cilomilast +++

LPDE4, IC50: 100 nM

HPDE4, IC50: 120 nM

 		99%
Avanafil ++++

PDE5, IC50: 1 nM

 		98%
Vardenafil HCl Trihydrate ++++

PDE5, IC50: 0.7 nM

 		98%
Tadalafil ++++

PDE5, IC50: 1.8 nM

 		98%
Icariin ++

PDE5, IC50: 0.432 μM

 		98%
Sildenafil ✔ +++

PDE6, IC50: 33 nM

 		98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Anagrelide HCl/盐酸阿那格雷 生物活性

靶点

  • PDE
描述 Anagrelide Hydrochloride is a drug used for the treatment of essential thrombocytosis (ET; essential thrombocythemia), or overproduction of blood platelets, and also has been used in the treatment of chronic myeloid leukemia. It inhibits cyclic AMP phosphodiesterase, as well as ADP- and collagen-induced platelet aggregation[3]. Anagrelide was effective in patients with ET which had similar hematologic remission rate to hydroxyurea and could take effect more quickly than hydroxyurea[4]. Only at anagrelide concentrations of 10 to 500 times therapeutic doses did anagrelide inhibit megakaryocyte colony development: an anagrelide concentration of 5 micrograms/mL reduced colony numbers by 57% and colony size by 31%. Therapeutic concentrations of anagrelide influence primarily the postmitotic phase of megakaryocyte development, decreasing platelet production by reducing megakaryocyte size and ploidy, as well as by disrupting full megakaryocyte maturation[5]. In addition, food/caffeine delayed absorption of anagrelide. Anagrelide was generally well tolerated and had small effects on ECG (electrocardiogram) parameters and heart rate[6].

Anagrelide HCl/盐酸阿那格雷 细胞实验

Cell Line
Concentration Treated Time Description References
CD34+ haematopoietic progenitor cells 26-44 nM 12 days To evaluate the effects of Anagrelide and its metabolites on megakaryocyte development, results showed that Anagrelide and BCH24426 significantly inhibited megakaryocyte development, while RL603 had no significant effect. Br J Pharmacol. 2005 Oct;146(3):324-32.
HeLa cells 300 nM 12 hours To investigate the mechanism of Anagrelide-induced cell death, results showed that Anagrelide treatment increased SLFN12 protein levels, and this increase depended on the PDE3A-SLFN12 interaction. Nat Commun. 2021 Oct 27;12(1):6204.
Megakaryocytes (MKs) 300 nM 2 days To investigate the effect of Anagrelide on megakaryocytes, results showed that Anagrelide induced MK cell death, and this death could be completely blocked by co-treatment with the PDE3 inhibitor Treq. Nat Commun. 2021 Oct 27;12(1):6204.
Bel7404 cells 100 nM 24 or 36 hours ANA induced G0/G1 cell cycle arrest in Bel7404 cells Am J Cancer Res. 2019 Sep 1;9(9):1905-1921.
HeLa cells 300 nM 36 hours To evaluate the effect of Anagrelide on cell survival, results showed that Anagrelide dose-dependently induced HeLa cell death. Nat Commun. 2021 Oct 27;12(1):6204.
ImMKCL (differentiated state) 1 µM and 10 µM 48 hours To evaluate the effect of Anagrelide on imMKCL DNA synthesis, results showed significant inhibition of DNA synthesis. Haematologica. 2020 May;105(5):e216-e220.
ImMKCL (undifferentiated state) 1 µM and 10 µM 96 hours To evaluate the effect of Anagrelide on imMKCL proliferation, results showed significant inhibition of cell proliferation. Haematologica. 2020 May;105(5):e216-e220.

Anagrelide HCl/盐酸阿那格雷 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice H4 cell xenograft model Oral 10 mg/kg or 30 mg/kg Once daily for 15 days ANA significantly inhibited the growth of H4 cell xenografts Am J Cancer Res. 2019 Sep 1;9(9):1905-1921.
BALB/c nude mice HeLa cells xenograft model Oral gavage 5 mg/kg and 1 mg/kg Once daily for 8 days, then twice daily for 6 days To evaluate the anti-tumor effect of Anagrelide analog A6 in vivo, results showed that the A6 (5 mg/kg) treatment group exhibited the most dramatic tumor growth inhibition. Nat Commun. 2021 Oct 27;12(1):6204.

Anagrelide HCl/盐酸阿那格雷 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00306202 Leukemia Phase 1 Active, not recruiting October 4, 2022 Austria ... 展开 >> Local Institution Vienna, Austria, 1090 France Local Institution Nantes, France, 44093 Local Institution Paris Cedex 10, France, 75475 Local Institution Paris Cedex 12, France, 75571 Germany Local Institution Berlin, Germany, 13353 Local Institution Frankfurt, Germany, 60590 Local Institution Hannover, Germany, 30625 Italy Local Institution Monza (mi), Italy, 20052 Netherlands Local Institution Rotterdam, Netherlands, 3015 GJ United Kingdom Local Institution Manchester, Greater Manchester, United Kingdom, M27 4HA Local Institution Bristol, Somerset, United Kingdom, BS2 8BJ Local Institution Sutton, Surrey, United Kingdom, SM2 5PT Local Institution Birmingham, West Midlands, United Kingdom, B4 6NH 收起 <<
NCT01243944 Polycythemia Vera Phase 3 Completed - -
NCT00481052 Chronic Myeloid Leukemia Phase 2 Active, not recruiting December 2018 Italy ... 展开 >> Dipartimento Area Medica P.O. Ascoli Piceno, Italy, 63100 Unità Operativa Ematologica - Università degli Studi di Bari Bari, Italy, 70124 Ospedali Riuniti Bergamo, Italy, 24100 stituto di Ematologia "Lorenzo e A. Seragnoli" - Università degli Studi di Bologna - Policlinico S. Orsola - Malpighi Bologna, Italy Sezione di Ematologia e Trapianti Spedali Civili Brescia, Italy, 21125 Azienda Spedali Civili Brescia, Italy, 25100 ASL N.8 - Ospedale "A. Businco" - Struttura Complessa di Ematologia e CTMO Cagliari, Italy Ospedale Ferrarotto Catania, Italy, 95124 Azienda Ospedaliera Pugliese Ciaccio Catanzaro, Italy, 88100 Sezione di Ematologia e Fisiopatologia delle Emostasi - Azienda Ospedaliera - Arcispedale S. Anna Ferrara, Italy Azienda Ospedaliera Universitaria - Università degli Studi di Napoli "Federico II" - Facoltà di Medicina e Chirurgia Napoli, Italy Ospedale S. Luigi Gonzaga Orbassano, Italy, 10043 La Maddalena Casa di Cura di Alta Specialità Dipartimento Oncologico di III Livello Palermo, Italy Unità Operativa Ematologia e Centro Trapianti - Dipartimento di Oncologia ed Ematologia - AUSL Ospedale di Piacenza Piacenza, Italy Ospedale S.Maria delle Croci Ravenna, Italy, 48100 Calabria Dipartimento Emato-Oncologia A.O."Bianchi-Melacrino-Morelli" Reggio Calabria, Italy Università La Cattolica del Sacro Cuore Roma, Italy, 00168 Complesso Ospedaliero S. Giovanni Addolorata Roma, Italy, 00184 Università degli Studi "Sapienza" - Dip Biotecnologie Cellulari ed Ematologia - Divisione di Ematologia Roma, Italy U.O. Ematologia, Azienda Ospedaliera Universitaria Senese Siena, Italy, 53100 Policlinico Universitario - Clinica Ematologia Udine, Italy, 33100 Policlinico G.B. Rossi Verona, Italy, 37134 收起 <<

Anagrelide HCl/盐酸阿那格雷 参考文献

[1]Tefferi A, Silverstein MN, et al. Anagrelide as a new platelet-lowering agent in essential thrombocythemia: mechanism of actin, efficacy, toxicity, current indications. Semin Thromb Hemost. 1997;23(4):379-83.

[2]Silverstein MN, Petitt RM, et al. Anagrelide: a new drug for treating thrombocytosis. N Engl J Med. 1988 May 19;318(20):1292-4.

[3]Pescatore SL, Lindley C. Anagrelide: a novel agent for the treatment of myeloproliferative disorders. Expert Opin Pharmacother. 2000 Mar;1(3):537-46

[4]Ge X, Yang L, Jin J, Qian W, Li J, Yang R, Cao X, Jiang B, Wang Z, Hou M, Zhang W, Xiao Z, Zhao Y, Gao D, Zhang X, Wang S, Sun A, Fu J, Su L, Li K. [Efficacy and safety of anagrelide in treatment of essential thrombocythemia: multicenter, randomized controlled clinical trial]. Zhonghua Xue Ye Xue Za Zhi. 2015 Jul;36(7):547-52. Chinese

[5]Mazur EM, Rosmarin AG, Sohl PA, Newton JL, Narendran A. Analysis of the mechanism of anagrelide-induced thrombocytopenia in humans. Blood. 1992 Apr 15;79(8):1931-7

[6]Martínez-Sellés M, Datino T, Figueiras-Graillet L, Gama JG, Jones C, Franklin R, Fernández-Avilés F. Cardiovascular safety of anagrelide in healthy subjects: effects of caffeine and food intake on pharmacokinetics and adverse reactions. Clin Drug Investig. 2013 Jan;33(1):45-54

Anagrelide HCl/盐酸阿那格雷 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.42mL

0.68mL

0.34mL

17.09mL

3.42mL

1.71mL

34.18mL

6.84mL

3.42mL

Anagrelide HCl/盐酸阿那格雷 技术信息

CAS号58579-51-4
分子式C10H8Cl3N3O
分子量 292.55
SMILES Code O=C1N=C2NC3=C(C(Cl)=C(Cl)C=C3)CN2C1.[H]Cl
MDL No. MFCD01720337
别名 BL4162A; Anagrelide (hydrochloride); Thromboreductin; GALE-401; Xagrid; Agrylin; BMY 26538-01; Anagrelide hydrochloride
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C
溶解方案

DMSO: 6 mg/mL(20.51 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: Anagrelide | 58579-51-4 | BL4162A | PDEIII Inhibitor | Metabolic Enzyme/Protease | Apoptosis | Phosphodiesterase (PDE) | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Anagrelide HCl/盐酸阿那格雷 纯度/质量文件 | Anagrelide HCl/盐酸阿那格雷 亚型比较 | Anagrelide HCl/盐酸阿那格雷 生物活性 | Anagrelide HCl/盐酸阿那格雷 临床数据 | Anagrelide HCl/盐酸阿那格雷 参考文献 | Anagrelide HCl/盐酸阿那格雷 实验方案 | Anagrelide HCl/盐酸阿那格雷 技术信息

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