产品说明书

Quizartinib

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Chemical Structure| 950769-58-1 同义名 : 奎扎替尼 (AC220) ;AC220
CAS号 : 950769-58-1
货号 : A475775
分子式 : C29H32N6O4S
纯度 : 98%
分子量 : 560.667
MDL号 : MFCD18074524
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(62.43 mM)，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

DMF: 10 mg/mL(17.84 mM)，配合低频超声助溶
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 2 mg/mL clear

PO 0.5% CMC-Na 45 mg/mL suspension

生物活性
靶点

  • FLT3

    FLT3 (WT), IC50:4.2 nM

    FLT3 (ITD), IC50:1.1 nM
描述 Quizartinib (AC220) is an orally bioavailable, highly selective, and potent second-generation type II FLT3 tyrosine kinase inhibitor, with a Kd of 1.6 nM. It effectively inhibits both wild-type FLT3 and FLT3-ITD autophosphorylation in MV4-11 cells, with IC50 values of 4.2 and 1.1 nM, respectively. Additionally, Quizartinib can be conjugated to the VHL ligand through an optimized linker to develop a PROTAC FLT3 degrader. Furthermore, Quizartinib induces apoptosis[1].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
8226/MR20 0.1-10 μM Function Assay 30 min enhances uptake of substrates of ABCG2 and ABCB1 in a concentration-dependent manner 23967177
8226/MR20 0.1 µM Cell Viability Assays 96 h sensitizes K562/ABCG2 cells to mitoxantrone topotecan  23967177
A375 Growth Inhibition Assay 72 h IC50> 10 000 nM 19654408
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
NCT01390337 Leukemia, Myeloid, Acute Phase 1 Completed - United States, Florida ... 展开 >> Mayo Clinic Jacksonville Jacksonville, Florida, United States, 32224 United States, Illinois Northwestern University Chicago, Illinois, United States, 60611 United States, Maryland Johns Hopkins Medical Institute Baltimore, Maryland, United States, 21231 United States, New York Memorial-Sloan Kettering Cancer Center New York, New York, United States, 10065 United States, Texas M.D. Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT02428543 Acute Myeloid Lukemia Phase 1 Phase 2 Recruiting September 2020 France ... 展开 >> Dr Abdelaziz CHAIB Recruiting Aix-en-Provence, France, 13600 Contact: Abdelaziz CHAIB       achaib@ch-aix.fr    Principal Investigator: Abdelaziz CHAIB          Chu Amiens Recruiting Amiens, France, 80054 Contact: MAROLLEAU Jean Pierre          Principal Investigator: MAROLLEAU Jean Pierre          CHU d'Angers Recruiting Angers, France, 49033 Contact: Martine GARDEMBAS       Magardembas@chu-angers.fr    Principal Investigator: Martine GARDEMBAS          Hôpital VICTOR DUPOUY Recruiting Argenteuil, France, 95107 Contact: AL JIJAKLI Ahmad       ahmad.aljijakli@ch-argenteuil.fr    Principal Investigator: AL JIJAKLI Ahmad          Dr Edouard RANDIAMALALA Recruiting Bayonne, France, 64100 Contact: Edouard RANDIAMALALA       erandiamalala@ch-cotebasque.fr    Principal Investigator: Edouard RANDIAMALALA          CHU de Besançon Recruiting Besançon, France, 25030 Contact: Fabrice LAROSA       flarosa@chu-besançon.fr    Principal Investigator: Fabrice LAROSA          Dr Thorsten BRAUN Recruiting Bobigny, France, 93000 Contact: Thorsten BRAUN       thorsten.braun@aphp.fr    Principal Investigator: Thorsten BRAUN          CHU Boulogne Sur Mer Recruiting Boulogne Sur Mer cedex, France, 62321 Contact: CHOUFI Bachra       b.choufi@ch-boulogne.fr    Principal Investigator: CHOUFI Bachra          Chr Clemenceau Recruiting Caen Cedex, France, 14033 Contact: REMAN Oumédaly       reman-o@chu-caen.fr    Principal Investigator: REMAN Oumédaly          Hôpital d'Instruction des Armées PERCY Recruiting Clamart, France, 92141 Contact: Jean Valère MALFUSSON       jvmalf@free.fr    Principal Investigator: Jean Valère MALFUSSON          Dr Stéphanie HAÏAT Recruiting Corbeil-essonnes, France, 91100 Contact: Stéphanie HAÏAT          Principal Investigator: Stéphanie HAÏAT          Hôpital Henri Mondor Recruiting Créteil, France, 94010 Contact: PAUTAS Cécile       cecile.pautas@hmn.aphp.fr    Principal Investigator: PAUTAS Cécile          CHU de Dijon Not yet recruiting Dijon, France, 21079 Contact: CAILLOT Denis       denis.caillot@chu-dijon.fr    Principal Investigator: CAILLOT Denis          Centre hospitalier de Versailles Recruiting Le Chesnay cedex, France, 78157 Contact: Rousselot Philippe    003339638622    phrousselot@ch-versailles.fr    Principal Investigator: Rousselot Philippe          Hôpital Claude Huriez Recruiting Lille cedex, France, 59037 Contact: QUESNEL Bruno       bquesnel@chru-lille.fr    Principal Investigator: QUESNEL Bruno          CHRU Dupuytren Not yet recruiting Limoges cedex, France, 87042 Contact: TURLURE Pascal       pascal.turlure@chu-limoges.fr    Principal Investigator: TURLURE Pascal          Hôpital Edouard Herriot Recruiting Lyon cedex 03, France, 69437 Contact: THOMAS Xavier       xavier.thomas@chu-lyon.fr    Principal Investigator: THOMAS Xavier          Dr Regis COSTELLO Recruiting Marseille, France, 13000 Contact: Regis COSTELLO       regis.costello@ap-hm.fr    Principal Investigator: Regis COSTELLO          Centre Hospitalier de Meaux Recruiting Meaux, France, 77104 Contact: FRAYFER Jamilé       j-frayfer@ch-meaux.fr    Principal Investigator: FRAYFER Jamilé          Dr Mario OJEDA-URIBE Recruiting Mulhouse, France, 68000 Contact: Mario OJEDA-URIBE       ojedam@ch-mulhouse.fr    Principal Investigator: Mario OJEDA-URIBE          Dr Jacques DELAUNAY Recruiting Nantes, France, 44000 Contact: Jacques DELAUNAY       jacques.delaunay@chu-nantes.fr    Principal Investigator: Jacques DELAUNAY          CHU Nice, Hôpital Archet 1 Recruiting Nice cedex 3, France, 06202 Contact: MANNONE Lionel       mannone.l@chu-nice.fr    Principal Investigator: MANNONE Lionel          CHU de Nîmes Recruiting Nîmes, France, 30029 Contact: Eric JOURDAN       eric.jourdan@chu-nimes.fr    Principal Investigator: Eric Jourdan          Hôpital Saint Antoine Recruiting Paris cedex 12, France, 75751 Contact: ISNARD Françoise       francoise.isnard@sat.aphp.fr    Principal Investigator: ISNARD Françoise          Hôpital Necker Enfants Malades Recruiting Paris cedex 15, France, 75743 Contact: SUAREZ Felipe       felipe.suarez@nck.aphp.fr    Principal Investigator: SUAREZ Felipe          Hôpital Saint Louis Recruiting Paris, France, 75010 Contact: RAFFOUX Emmanuel       emmanuel.raffoux@sls.ap-hop-paris.fr    Principal Investigator: RAFFOUX Emmanuel          Hôpital La Pitié Salpêtrière Recruiting Paris, France, 75013 Contact: UZUNOV Madalina       madalina.uzunov@psl.aphp.fr    Principal Investigator: UZUNOV Madalina          Dr Laurence SANHES Suspended Perpignan, France, 66000 Dr Arnaud PIGNEUX Recruiting Pessac, France, 33604 Contact: Arnaud PIGNEUX       arnaud.pigneux@chu-bordeaux.fr    Principal Investigator: Arnaud PIGNEUX          Centre Hospitalier René Dubos Recruiting Pontoise Cedex, France, 95303 Contact: VAIDA Iona Dana       ioana.vaida@ch-pontoise.fr    Principal Investigator: VAIDA Iona Dana          Marc BERNARD Recruiting Rennes, France, 35000 Contact: Marc BERNARD       marc.bernard@chu-rennes.fr    Principal Investigator: Marc BERNARD          Dr Emilie LEMASLE Recruiting Rouen, France, 76000 Contact: Emilie LEMASLE       emilie.lemasle@chb.unicancer.fr    Principal Investigator: Emilie LEMASLE          Centre Hospitalier René Huguenin Suspended Saint Cloud, France, 92210 Institut de Cancérologie de la Loire Recruiting Saint-Priest-en-Jarez, France, 42270 Contact: Emmanuelle TAVERNIER-TARDY       emmanuelle.tavernier@icloire.fr    Principal Investigator: Emmanuelle TAVERNIER-TARDY          Dr Réda GARIDI Recruiting Saint-Quentin, France, 02100 Contact: Réda GARIDI          Principal Investigator: Réda GARIDI          Dr Christian RECHER Recruiting Toulouse, France, 31000 Contact: Christian RECHER          Principal Investigator: Christian RECHER          Centre Hospitalier de Valenciennes Recruiting Valenciennes, France, 59322 Contact: FERNANDES José       fernandes-j@ch-valenciennes.fr    Principal Investigator: FERNANDES José 收起 <<
NCT00462761 Acute Myeloid Leukemia ... 展开 >> Leukemia Myelodysplastic Syndrome AML MDS 收起 << Phase 1 Completed - United States, Alabama ... 展开 >> University of Alabama at Birmingham Birmingham, Alabama, United States, 35294 United States, Nebraska University of Nebraska Medical Center Omaha, Nebraska, United States, 68198 United States, Texas MD Anderson Cancer Center Houston, Texas, United States, 77030 Georgia Chemotherapy and Immunotherapy Clinic T'Bilisi, Georgia Hematology and Chemotherapy Clinic T'bilisi, Georgia 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.78mL

0.36mL

0.18mL

8.92mL

1.78mL

0.89mL

17.84mL

3.57mL

1.78mL
参考文献

[1]Zarrinkar PP, et al. AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML). Blood, 2009, 114(14), 2984-2992.