货号:A475775
同义名:
奎扎替尼 (AC220)
/ AC220
Quizartinib (AC220) 是一种口服活性、高选择性和强效的第二代 II 型 FLT3 酪氨酸激酶抑制剂,Kd 为 1.6 nM。Quizartinib 抑制 MV4-11 细胞中野生型 FLT3 和 FLT3-ITD 自磷酸化的 IC50 值分别为 4.2 nM 和 1.1 nM,并可通过优化连接子与 VHL 配体连接形成 PROTAC FLT3 降解剂,诱导凋亡。
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产品名称 | FLT3 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
R406 | ✔ | Syk | 99%+ | ||||||||||||||||
Go6976 | ✔ | 99%+ | |||||||||||||||||
Quizartinib |
+++
FLT3 (WT), IC50: 4.2 nM FLT3 (ITD), IC50: 1.1 nM |
99%+ | |||||||||||||||||
Gilteritinib |
++++
FLT3, IC50: 0.29 nM |
99%+ | |||||||||||||||||
Amuvatinib |
+
FLT3 (D835Y), IC50: 81 nM |
99%+ | |||||||||||||||||
Pacritinib |
++
FLT3, IC50: 22 nM FLT3 (D835Y), IC50: 6 nM |
97% | |||||||||||||||||
Dovitinib |
++++
FLT3, IC50: 1 nM |
c-Kit | 99%+ | ||||||||||||||||
Denfivontinib |
++++
FLT3, IC50: 0.4 nM FLT3 (D835Y), IC50: 0.4 nM |
RET | 99%+ | ||||||||||||||||
TAK-659 HCl |
++
FLT3, IC50: 4.6 nM |
Syk | 99%+ | ||||||||||||||||
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。 |
靶点 |
|
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]. |
体内研究 | Quizartinib (AC220) inhibits FLT3 activity in vivo, significantly prolonging survival in a mouse model of FLT3-ITD AML at doses as low as 1 mg/kg when administered orally once daily. It eradicates tumors in a FLT3-dependent mouse xenograft model at 10 mg/kg and potently inhibits FLT3 activity in primary patient cells. The oral bioavailability of Quizartinib, determined in rats by comparing oral and intravenous pharmacokinetics at 3 mg/kg, is approximately 40%. Following administration of a single 10 mg/kg dose of Quizartinib via oral gavage, mice are euthanized at 2 time points after dosing, with groups of 4 animals each. Quantification of total FLT3 and phospho-FLT3 in tumor samples reveals time-dependent inhibition of FLT3 autophosphorylation. FLT3 activity is inhibited by 90% at 2 hours and 40% at 24 hours post-administration. The degree of inhibition correlates well with the expected free Quizartinib plasma levels, as determined by pharmacokinetic experiments[1]. |
体外研究 | Quizartinib (AC220) is a newly developed compound specifically optimized as a FLT3 inhibitor for the treatment of acute myeloid leukemia (AML). It effectively inhibits FLT3-WT and FLT3-ITD autophosphorylation, with IC50 values of 4.2±0.3 nM and 1.1±0.1 nM, respectively. Furthermore, Quizartinib demonstrates inhibition of MV4-11 and A375 cells, with IC50 values of 0.56±0.3 nM and >10,000 nM, respectively. In cellular assays, Quizartinib displays potent inhibition of FLT3 at low nanomolar concentrations and exhibits high selectivity when screened against the majority of the human protein kinome[1]. |
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 | |
EOL-1 | Growth Inhibition Assay | IC50=1 nM | 23497317 | ||
Dose | Nonhuman primates: 10 mg/kg - 200 mg/kg[3] (p.o.) Mice: 1 mg/kg, 10 mg/kg[2] (p.o.) | ||||||||||||
Administration | p.o. | ||||||||||||
Pharmacokinetics |
|
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 << |
计算器 | ||||
存储液制备 | ![]() |
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 |
CAS号 | 950769-58-1 |
分子式 | C29H32N6O4S |
分子量 | 560.667 |
别名 | 奎扎替尼 (AC220) ;AC220 |
运输 | 蓝冰 |
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 |