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CAS No.: 1254053-43-4

Gilteritinib/吉列替尼 Catalog No. CSN13926

Synonyms: ASP2215

Gilteritinib is a potent FLT3/AXL inhibitor with IC50 of 0.29 nM/< 1 nM respectively and shows potent antileukemic activity against AML with either or both FLT3-ITD and FLT3-D835 mutations.

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生物活性

实验方案

技术信息

生物活性

描述Gilteritinib is a FLT3 inhibitor with IC50 value of 0.29 nM for FLT3, and inhibited FLT3, LTK, ALK, and AXL kinases with IC50 values less than 1nM. Gilteritinib exhibited anti-proliferative effect on MV4-11 cells, harboring FLT3-ITD, with IC50 value of 0.92nM post 5 days and accompanied with inhibition of pFLT3, pAKT, pSTAT5, pERK, and pS6 at concentration>1nM post 2h. Also, it inhibited the growth of Ba/F3 cells expressing FLT3-ITD and/or FLT3-D835 mutation with similar activity. Oral administration of Gilteritinib for 28 days achieved complete MV4-11 tumor regression at dose more than 6mg/kg in mice. Further, it decreased tumor burden in bone marrow and prolonged the survival of mice intravenously transplanted with MV4-11 cells.
作用机制Gilteritinib binds to FLT3 at the ATP-binding site.^[2]
动物研究
剂量
Nude Mice: 3 mg/kg^[3] (p.o.), 30 mg/kg^[3] (p.o.)

给药途径
p.o.

动物药代数据
Animal Nude mice^[3]
Dose 3 mg/kg
Administration p.o.
C_max 21.33 ng/ml
T_max 2 h
AUC_{24 h} 156.3 ng·h/ml
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
NCT03680677	Leukemia, Acute ... more >> MDS Collapse <<	Not Applicable	Not yet recruiting	November 2025	United States, Pennsylvania ... more >> Abramson Cancer Center of the University of Pennsylvania Not yet recruiting Philadelphia, Pennsylvania, United States, 19104 Collapse <<
NCT02622932	Advanced Solid Tumors	Phase 1	Active, not recruiting	April 2017	China, Jiangsu ... more >> Jiangsu Province Hospital Nanjing, Jiangsu, China, 210029 Collapse <<
NCT02421939	Leukemia, Acute Myeloid (AML)	Phase 3	Active, not recruiting	December 2020	-

更多
参考文献

[1] ASP2215, a novel FLT3/AXL inhibitor: Preclinical evaluation in acute myeloid leukemia (AML)
[2] Mori M, Kaneko N, et al. Gilteritinib, a FLT3/AXL inhibitor, shows antileukemic activity in mouse models of FLT3 mutated acute myeloid leukemia. Invest New Drugs. 2017 Oct;35(5):556-565.
[3] Ueno Y, Mori M, et al. Evaluation of gilteritinib in combination with chemotherapy in preclinical models of FLT3-ITD+ acute myeloid leukemia. Oncotarget. 2019 Apr 2;10(26):2530-2545.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.8093 mL
- 9.0463 mL
- 18.0926 mL
- 5 mM
- 0.3619 mL
- 1.8093 mL
- 3.6185 mL
- 10 mM
- 0.1809 mL
- 0.9046 mL
- 1.8093 mL

技术信息

CAS号

1254053-43-4

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H44N8O3

运输

蓝冰

分子量

552.71

别名

ASP2215

溶解度

DMSO	10.0 mg/mL (18.1 mM)
Water	Insoluble
Ethanol	6.0 mg/mL (10.9 mM)

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT03680677	Leukemia, Acute ... more >> MDS Collapse <<	Not Applicable	Not yet recruiting	November 2025	United States, Pennsylvania ... more >> Abramson Cancer Center of the University of Pennsylvania Not yet recruiting Philadelphia, Pennsylvania, United States, 19104 Collapse <<
NCT02622932	Advanced Solid Tumors	Phase 1	Active, not recruiting	April 2017	China, Jiangsu ... more >> Jiangsu Province Hospital Nanjing, Jiangsu, China, 210029 Collapse <<
NCT02421939	Leukemia, Acute Myeloid (AML)	Phase 3	Active, not recruiting	December 2020	-
NCT02236013	Acute Myeloid Leukemia	Phase 1	Recruiting	July 2022	United States, California ... more >> Site US10003 Recruiting Los Angeles, California, United States, 90095 United States, Connecticut Site US10013 Recruiting New Haven, Connecticut, United States, 06520 United States, Illinois Site US10004 Recruiting Chicago, Illinois, United States, 60611 United States, Kansas Site US10009 Recruiting Westwood, Kansas, United States, 66205 United States, Maryland Site US10001 Recruiting Baltimore, Maryland, United States, 21231 United States, New York Site US10002 Recruiting New York, New York, United States, 10032 United States, Ohio Site US10014 Recruiting Cleveland, Ohio, United States, 44106 Site US10008 Withdrawn Columbus, Ohio, United States, 43201 United States, Oklahoma Site US10019 Recruiting Oklahoma City, Oklahoma, United States, 73104 United States, Pennsylvania Site US10006 Recruiting Philadelphia, Pennsylvania, United States, 19104 United States, Texas Site US10010 Recruiting San Antonio, Texas, United States, 78229 Collapse <<
NCT03013998	Previously Untreated Acute Mye... more >>loid Leukemia Collapse <<	Phase 1 Phase 2	Recruiting	December 2021	United States, Arizona ... more >> Mayo Clinic Arizona Recruiting Phoenix, Arizona, United States, 85054 Principal Investigator: Lisa Sproat, MD United States, California UCLA Ronald Reagan Medical Center Recruiting Los Angeles, California, United States, 90095 Principal Investigator: Gary Schiller, MD University of California, San Francisco Recruiting San Francisco, California, United States, 94143 Principal Investigator: Gabriel Mannis, MD United States, Colorado University of Colorado Recruiting Denver, Colorado, United States, 80203 Principal Investigator: Dan Pollyea, MD United States, Florida Mayo Clinic Florida Recruiting Jacksonville, Florida, United States, 32224 Principal Investigator: James Foran, MD United States, Georgia Emory University Recruiting Atlanta, Georgia, United States, 30308 Principal Investigator: William Blum, MD United States, Illinois University of Chicago Recruiting Chicago, Illinois, United States, 60637 Principal Investigator: Wendy Stock, MD United States, Maryland University of Maryland Medical Center Recruiting Baltimore, Maryland, United States, 21201 Principal Investigator: Maria Baer, MD United States, New York Memorial Sloan Kettering Cancer Center Recruiting New York, New York, United States, 10065 Principal Investigator: Eytan M Stein, MD United States, Ohio Ohio State University Recruiting Columbus, Ohio, United States, 43210 Principal Investigator: John C Byrd, MD Principal Investigator: Alice Mims, MD Principal Investigator: Alison R Walker, MD, MPH United States, Oregon Oregon Health & Science University Recruiting Portland, Oregon, United States, 97239 Principal Investigator: Uma Borate, MD United States, Texas University of Texas Southwestern Recruiting Dallas, Texas, United States, 75390 Principal Investigator: Prapti Patel, MD United States, Utah Huntsman Cancer Institute, University of Utah Recruiting Salt Lake City, Utah, United States, 84112 Principal Investigator: Michael Deininger, MD, PhD Collapse <<
NCT02310321	Acute Myeloid Leukemia	Phase 1	Active, not recruiting	April 2020	Japan ... more >> Site JP00003 Aichi, Japan Site JP00001 Fukuoka, Japan Site JP00002 Gunma, Japan Site JP00007 Hyogo, Japan Site JP00006 Kanagawa, Japan Site JP00005 Tokyo, Japan Collapse <<
NCT03182244	Acute Myeloid Leukemia With FM... more >>S-like Tyrosine Kinase (FLT3) Mutation Collapse <<	Phase 3	Recruiting	June 2020	-
NCT02561455	Advanced Solid Tumors ... more >> Acute Myeloid Leukemia Collapse <<	Phase 1 Phase 2	Active, not recruiting	July 2023	United States, Arizona ... more >> Site US10005 Phoenix, Arizona, United States, 85084 United States, Maryland Site US10003 Baltimore, Maryland, United States, 21201 United States, New York Site US10006 New York, New York, United States, 10032 Site US10007 New York, New York, United States, 10065 United States, Ohio Site US10001 Cleveland, Ohio, United States, 44195 United States, Pennsylvania Site US10004 Hershey, Pennsylvania, United States, 17033 Site US10008 Philadelphia, Pennsylvania, United States, 19104 Collapse <<
NCT02181660	Acute Myeloid Leukemia (AML)	Phase 1	Completed	-	Japan ... more >> Site JP00002 Aichi, Japan Site JP00003 Fukuoka, Japan Site JP00001 Gunma, Japan Site JP00004 Tokyo, Japan Site JP00005 Tokyo, Japan Collapse <<
NCT02014558	Acute Myeloid Leukemia	Phase 1 Phase 2	Completed	-	-
NCT02752035	Acute Myeloid Leukemia (AML) ... more >> Acute Myeloid Leukemia With FMS-like Tyrosine Kinase (FLT3) Mutation Collapse <<	Phase 2 Phase 3	Recruiting	December 2021	-
NCT02927262	Acute Myeloid Leukemia (AML) ... more >> Acute Myeloid Leukemia With FMS-like Tyrosine Kinase (FLT3) / Internal Tandem Duplication (ITD) Mutation Collapse <<	Phase 3	Recruiting	March 2024	-
NCT03409081	-	-	-	-	Australia ... more >> Site AU61001 Canberra, Australia Italy Site IT39001 Milan, Italy Site IT39003 Milan, Italy United Kingdom Site UK44001 Birmingham, United Kingdom Site UK44003 Bristol, United Kingdom Site UK44002 London, United Kingdom Collapse <<
NCT03315299	-	-	-	-	United States, California ... more >> Children's Hospital Los Angeles Los Angeles, California, United States, 90027 Collapse <<
NCT02456883	Advanced Solid Tumors ... more >> Pharmacokinetics of 14C-labeled Gilteritinib Collapse <<	Phase 1	Completed	-	United States, Ohio ... more >> Site US10001 Cleveland, Ohio, United States, 44195 Collapse <<
NCT03730012	Acute Myeloid Leukemia (AML) ... more >> Acute Myeloid Leukemia With FMS-like Tyrosine Kinase (FLT3) Mutation Collapse <<	Phase 1 Phase 2	Not yet recruiting	September 2022	-
NCT03070093	-	-	-	-	-
NCT03625505	Acute Myeloid Leukemia (AML)	Phase 1	Recruiting	October 11, 2021	United States, California ... more >> David Geffen School of Medicin /ID# 200166 Not yet recruiting Los Angeles, California, United States, 90095 UC San Francisco Medical Center-Parnassus /ID# 200205 Not yet recruiting San Francisco, California, United States, 94143-2202 United States, Florida Sylvester Comprehensive Cancer /ID# 200268 Not yet recruiting Miami, Florida, United States, 33136-1002 United States, Illinois Northwestern Memorial Hospital /ID# 200230 Not yet recruiting Chicago, Illinois, United States, 60611-2927 United States, Kentucky Norton Cancer Institute /ID# 200623 Recruiting Louisville, Kentucky, United States, 40202-3700 United States, Maryland Johns Hopkins University /ID# 200349 Not yet recruiting Baltimore, Maryland, United States, 21287 United States, Minnesota Mayo Clinic - Rochester /ID# 200346 Not yet recruiting Rochester, Minnesota, United States, 55905-0001 United States, New Jersey Hackensack Univ Med Ctr /ID# 200229 Not yet recruiting Hackensack, New Jersey, United States, 07601 United States, New York Weill Cornell Medical College /ID# 200109 Not yet recruiting New York, New York, United States, 10021 United States, Pennsylvania Hosp of the Univ of Penn /ID# 200348 Not yet recruiting Philadelphia, Pennsylvania, United States, 19104 United States, Texas MD Anderson Cancer Center /ID# 206686 Not yet recruiting Houston, Texas, United States, 77030 Collapse <<
NCT02997202	Acute Myeloid Leukemia	Phase 3	Recruiting	August 2024	-

Gilteritinib/吉列替尼 Catalog No. CSN13926

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