Quizartinib (AC220)

中文名称：奎扎替尼

目录号：S1526 Purity: 99.52%

Quizartinib (AC220)是一种二代FLT3抑制剂，作用于Flt3(ITD/WT)，在MV4-11和 RS4;11细胞中IC50分别为1.1 nM/4.2 nM，作用于Flt3比作用于KIT，PDGFRA，PDGFRB，RET，和CSF-1R选择性高10倍。Quizartinib (AC220)可诱导肿瘤细胞的凋亡。Phase 3。

Quizartinib (AC220) Chemical Structure

CAS: 950769-58-1

规格	价格	库存
10mM (1mL in DMSO)	1056.51	现货
5mg	876.33	现货
50mg	4234.23	现货
200mg	10565.1	现货
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产品质控

批次：纯度： 99.52%

99.52

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细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
MV4-11	Function assay	0.01 to 100 nM	1 hr	Inhibition of FLT3 ITD mutant in human MV4-11 cells assessed as decrease in MEK1/2 phosphorylation at S217/221 at 0.01 to 100 nM after 1 hr by immunoblot analysis	29672049
MV4-11	Function assay	0.01 to 100 nM	1 hr	Inhibition of FLT3 ITD mutant in human MV4-11 cells assessed as decrease in AKT phosphorylation at S473 at 0.01 to 100 nM after 1 hr by immunoblot analysis	29672049
BA/F3	Growth inhibition assay		72 hrs	Growth inhibition of mouse BA/F3 cells after 72 hrs by calcein AM dye-based fluorescence assay, GI50 = 1.452 μM.	29672049
Sf9	Function assay			Inhibition of N-terminal GST/His6-fused recombinant human FLT3 (R571 to S993 residues) D835Y mutant expressed in Sf9 insect cells using poly (Ala,Glu,Lys,Tyr) 6:2:5:1 hydrobromide as substrate in presence of [gamma-33P]ATP, IC50 = 0.136 μM.	29672049
Kasumi-1	Growth inhibition assay		72 hrs	Growth inhibition of human Kasumi-1 cells after 72 hrs by calcein AM dye-based fluorescence assay, GI50 = 0.064 μM.	29672049
Sf9	Function assay			Inhibition of N-terminal GST/His6-fused recombinant wild type human FLT3 (R571 to S993 residues) expressed in Sf9 insect cells using poly (Ala,Glu,Lys,Tyr) 6:2:5:1 hydrobromide as substrate in presence of [gamma-33P]ATP, IC50 = 0.036 μM.	29672049
Sf9	Function assay			Inhibition of N-terminal GST/His6-fused recombinant human FLT3 (R571 to S993 residues) ITD mutant expressed in Sf9 insect cells using poly (Ala,Glu,Lys,Tyr) 6:2:5:1 hydrobromide as substrate in presence of [gamma-33P]ATP, IC50 = 0.01 μM.	29672049
MV4-11	Growth inhibition assay		72 hrs	Growth inhibition of human MV4-11 cells after 72 hrs by calcein AM dye-based fluorescence assay, GI50 = 0.003 μM.	29672049
MOLM13	Growth inhibition assay		72 hrs	Growth inhibition of human MOLM13 cells after 72 hrs by calcein AM dye-based fluorescence assay, GI50 = 0.002 μM.	29672049
TC32	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells	29435139
NB-EBc1	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
SJ-GBM2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
U-2 OS	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
BT-37	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells	29435139
BT-12	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
Saos-2	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
MV4-11	Cell cycle assay	100 nM	12 hrs	Cell cycle arrest in human MV4-11 cells assessed as accumulation at G0/G1 phase at 100 nM after 12 hrs by propidium iodide staining based-FACS analysis	28956923
MV4-11	Apoptosis assay	100 nM	48 hrs	Induction of apoptosis in human MV4-11 cells assessed as cleavage of caspase-3 at 100 nM after 48 hrs by immunoblotting method	28956923
MOLM14	Apoptosis assay	100 nM	24 hrs	Induction of apoptosis in human MOLM14 cells assessed as cleavage of caspase-3 at 100 nM after 24 hrs by immunoblotting method	28956923
MOLM14	Apoptosis assay	100 nM	24 hrs	Induction of apoptosis in human MOLM14 cells assessed as cleavage of PARP at 100 nM after 24 hrs by immunoblotting method	28956923
MOLM13	Apoptosis assay	100 nM	12 hrs	Induction of apoptosis in human MOLM13 cells assessed as cleavage of caspase-3 at 100 nM after 12 hrs by immunoblotting method	28956923
MV4-11	Apoptosis assay	100 nM	48 hrs	Induction of apoptosis in human MV4-11 cells assessed as cleavage of PARP at 100 nM after 48 hrs by immunoblotting method	28956923
MOLM13	Apoptosis assay	100 nM	12 hrs	Induction of apoptosis in human MOLM13 cells assessed as cleavage of PARP at 100 nM after 12 hrs by immunoblotting method	28956923
MOLM14	Cell cycle assay	100 nM	12 hrs	Cell cycle arrest in human MOLM14 cells assessed as accumulation at G0/G1 phase at 100 nM after 12 hrs by propidium iodide staining based-FACS analysis	28956923
MOLM13	Cell cycle assay	100 nM	12 hrs	Cell cycle arrest in human MOLM13 cells assessed as accumulation at G0/G1 phase at 100 nM after 12 hrs by propidium iodide staining based-FACS analysis	28956923
SKM1	Antiproliferative assay		72 hrs	Antiproliferative activity against human SKM1 cells expressing FLT3 kinase after 72 hrs by CellTiter-Glo assay, GI50 = 1.3 μM.	28956923
U937	Antiproliferative assay		72 hrs	Antiproliferative activity against human U937 cells expressing FLT3 kinase after 72 hrs by CellTiter-Glo assay, GI50 = 1.2 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against TEL-fused LCK-transformed mouse BAF3 cells after 72 hrs by CellTiter-Glo assay, GI50 = 0.4 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells harboring FLT3-K663Q mutation after 72 hrs by CellTiter-Glo assay, GI50 = 0.37 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against TEL-fused FLT4-transformed mouse BAF3 cells after 72 hrs by CellTiter-Glo assay, GI50 = 0.27 μM.	28956923
HL60	Antiproliferative assay		72 hrs	Antiproliferative activity against human HL60 cells expressing FLT3 kinase after 72 hrs by CellTiter-Glo assay, GI50 = 0.13 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against TEL-fused RET-transformed mouse BAF3 cells after 72 hrs by CellTiter-Glo assay, GI50 = 0.13 μM.	28956923
CMK	Antiproliferative assay		72 hrs	Antiproliferative activity against human CMK cells expressing FLT3 kinase after 72 hrs by CellTiter-Glo assay, GI50 = 0.12 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against TEL-fused DDR1-transformed mouse BAF3 cells after 72 hrs by CellTiter-Glo assay, GI50 = 0.12 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against TEL-fused DDR2-transformed mouse BAF3 cells after 72 hrs by CellTiter-Glo assay, GI50 = 0.11 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD-D835I mutation after 72 hrs by CellTiter-Glo assay, GI50 = 0.056 μM.	28956923
Sf9	Function assay		1 hr	Inhibition of human HL60 cells-derived His-tagged FLT3 (564 to 993 residues) expressed in baculovirus infected sf9 cells using poly (4:1 Glu, Tyr) as substrate after 1 hr by ADP-Glo kinase assay, IC50 = 0.0304 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD-D835Y mutation after 72 hrs by CellTiter-Glo assay, GI50 = 0.028 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against TEL-fused CSF1R-transformed mouse BAF3 cells after 72 hrs by CellTiter-Glo assay, GI50 = 0.024 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against TEL-fused cKIT-transformed mouse BAF3 cells after 72 hrs by CellTiter-Glo assay, GI50 = 0.017 μM.	28956923
Sf9	Function assay		1 hr	Inhibition of human MV4-11 cells-derived His-tagged FLT3 ITD mutant (564 to 993 residues) expressed in baculovirus infected sf9 cells using poly (4:1 Glu, Tyr) as substrate after 1 hr by ADP-Glo kinase assay, IC50 = 0.0168 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD-D835del mutation after 72 hrs by CellTiter-Glo assay, GI50 = 0.012 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells harboring FLT3-D835V mutation after 72 hrs by CellTiter-Glo assay, GI50 = 0.011 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against TEL-fused PDGFRbeta-transformed mouse BAF3 cells after 72 hrs by CellTiter-Glo assay, GI50 = 0.0044 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells harboring FLT3-D835Y mutation after 72 hrs by CellTiter-Glo assay, GI50 = 0.002 μM.	28956923
MV4-11	Antiproliferative assay		72 hrs	Antiproliferative activity against human MV4-11 cells after 72 hrs by CellTiter-Glo assay, GI50 = 0.0003 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD mutation after 72 hrs by CellTiter-Glo assay, GI50 = 0.0003 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD-D835N mutation after 72 hrs by CellTiter-Glo assay, GI50 = 0.0003 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells expressing TEL-fused FLT3 kinase after 72 hrs by CellTiter-Glo assay, GI50 = 0.0003 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells harboring FLT3-D835H mutation after 72 hrs by CellTiter-Glo assay, GI50 = 0.0003 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD-D835A mutation after 72 hrs by CellTiter-Glo assay, GI50 = 0.0003 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against mouse BAF3 cells harboring FLT3-ITD-D835G mutation after 72 hrs by CellTiter-Glo assay, GI50 = 0.0003 μM.	28956923
THP1	Growth inhibition assay			Growth inhibition of human THP1 cells harboring wild-type FLT3 by XTT assay, GI50 = 2.125 μM.	28043794
Sf21	Function assay		10 mins	Inhibition of N-terminal GST-tagged recombinant human wild-type FLT3 (564 to end residues) D835Y mutant expressed in baculovirus infected sf21 cells using Abltide as substrate in presence of [gamma33P]ATP after 10 mins by scintillation counting method, IC50 = 0.2355 μM.	28043794
THP1	Growth inhibition assay		48 hrs	Growth inhibition of human THP1 cells expressing wild type FLT-3 after 48 hrs by XTT assay, GI50 = 2.125 μM.	27187860
HL60	Growth inhibition assay		48 hrs	Growth inhibition of human HL60 cells expressing wild type FLT-3 after 48 hrs by XTT assay, GI50 = 1.488 μM.	27187860
MV4-11	Growth inhibition assay		48 hrs	Growth inhibition of human MV4-11 cells expressing FLT3-ITD after 48 hrs by XTT assay, GI50 = 1.103 μM.	27187860
Sf21	Function assay		15 mins	Inhibition of recombinant human FLT3 expressed in insect Sf21 cells preincubated for 15 mins followed by poly(Glu:Tyr) substrate addition for 30 mins in presence of [gamma-32P]ATP by TR-FRET assay, IC50 = 0.02608 μM.	27187860
MV4-11	Antitumor assay	10 mg/kg	48 days	Antitumor activity against human MV4-11 cells xenografted in nude mouse assessed as tumor regression at 10 mg/kg, po qd administered on day 1 to 5 measured during 48 days post last dose	26081023
RS4:11	Function assay		72 hrs	Inhibition of wild type homozygous FLT3 in human RS4:11 cells assessed as cell growth inhibition after 72 hrs by MTS assay, GI50 = 2.2 μM.	26081023
Sf9	Function assay		120 mins	Inhibition of recombinant GST-tagged VEGFR2 kinase domain (V789 to V1356) (unknown origin) expressed in insect Sf9 cells using polyGlu4:Tyr peptide as substrate after 120 mins by Kinase-Glo assay, IC50 = 0.43 μM.	26081023
32D	Function assay		72 hrs	Inhibition of drug resistant human FLT3 ITD F691L mutant expressed in mouse 32D cells assessed as cell growth inhibition after 72 hrs by MTS assay, GI50 = 0.22 μM.	26081023
32D	Function assay		72 hrs	Inhibition of drug resistant human FLT3 ITD D835F mutant expressed in mouse 32D cells assessed as cell growth inhibition after 72 hrs by MTS assay, GI50 = 0.15 μM.	26081023
32D	Function assay		72 hrs	Inhibition of drug resistant human FLT3 ITD D835V mutant expressed in mouse 32D cells assessed as cell growth inhibition after 72 hrs by MTS assay, GI50 = 0.027 μM.	26081023
32D	Function assay		72 hrs	Inhibition of drug resistant human FLT3 ITD D835Y mutant expressed in mouse 32D cells assessed as cell growth inhibition after 72 hrs by MTS assay, GI50 = 0.016 μM.	26081023
MOLM-13	Function assay		72 hrs	Inhibition of FLT3 ITD heterozygous mutant in human MOLM-13 cells assessed as cell growth inhibition after 72 hrs by MTS assay, GI50 = 0.004 μM.	26081023
MV4-11	Function assay		72 hrs	Inhibition of FLT3 ITD homozygous mutant in human MV4-11 cells assessed as cell growth inhibition after 72 hrs by MTS assay, GI50 = 0.003 μM.	26081023
32D	Function assay		72 hrs	Inhibition of human FLT3 ITD mutant expressed in mouse 32D cells assessed as cell growth inhibition after 72 hrs by MTS assay, GI50 = 0.00001 μM.	26081023
HL60	Growth inhibition assay		48 hrs	Growth inhibition of human HL60 cells after 48 hrs by XTT assay, GI50 = 8.014 μM.	25108079
THP1	Growth inhibition assay		48 hrs	Growth inhibition of human THP1 cells after 48 hrs by XTT assay, GI50 = 5.574 μM.	25108079
MV411	Growth inhibition assay		48 hrs	Growth inhibition of human MV411 cells after 48 hrs by XTT assay, GI50 = 3.31 μM.	25108079
MOLM13	Antiproliferative assay			Antiproliferative activity against human MOLM13 cells expressing FLT3-ITD mutant, GI50 = 0.004 μM.	22726931
MV4-11	Antitumor assay	10 mg/kg	28 days	Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as inhibition of tumor growth at 10 mg/kg, po QD for 28 days measured after 32 days postdose	19754199
MV4-11	Antitumor assay	10 mg/kg	28 days	Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as suppression of tumor volume at 10 mg/kg, po QD for 28 days measured after dosing period	19754199
MV4-11	Antitumor assay	3 mg/kg	28 days	Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as suppression of tumor volume at 3 mg/kg, po QD for 28 days measured after dosing period	19754199
MV4-11	Antitumor assay	10 mg/kg	28 days	Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as tumor growth regression at 10 mg/kg, po QD for 28 days measured after dosing period	19754199
MV4-11	Antitumor assay	3 mg/kg	28 days	Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as tumor growth regression at 3 mg/kg, po QD for 28 days measured after dosing period	19754199
MV4-11	Antitumor assay	1 mg/kg	28 days	Antitumor activity against human MV4-11 cells xenografted in athymic nude mouse assessed as inhibition of tumor growth at 1 mg/kg, po QD for 28 days measured during dosing period	19754199
HEK293	Function assay			Binding affinity to FLT3 catalytic domain expressed in HEK293 cells by competitive binding assay, Kd = 0.0016 μM.	19754199
MV4-11	Antiproliferative assay		72 hrs	Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer-blue cell viability assay, IC50 = 0.00056 μM.	19754199
MV4-11	Antitumor assay	10 mg/kg	60 days	Antitumor activity against human MV4-11 cells xenografted mouse model assessed as inhibition of tumor regrowth at at 10 mg/kg, po 60 days post treatment	19654408
RS4-11	Function assay		2 hrs	Inhibition of FLT3 autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay, IC50 = 0.0042 μM.	19654408
AML	Function assay			Inhibition of FLT3 autophosphorylation in human AML cells isolated from relapsed acute myeloid leukemia patient by Western blotting, IC50 = 0.002 μM.	19654408
RS4-11	Function assay		2 hrs	Inhibition of FLT3 ITD mutant autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay, IC50 = 0.0011 μM.	19654408
blast cells	Function assay		2 hrs	Inhibition of FLT3 ITD mutant autophosphorylation in human blast cells after 2 hrs by electrochemiluminescence, IC50 = 0.0008 μM.	19654408
MV4-11	Cytotoxicity assay		72 hrs	Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay, IC50 = 0.00056 μM.	19654408
THP-1	Growth Inhibition Assay		72 h	IC50>10,000 nM	23412931
RS4;11	Growth Inhibition Assay		72 h	IC50>10,000 nM	23412931
MOLM-14	Growth Inhibition Assay		72 h	IC50=0.1 nM	23412931
SEM-K2	Growth Inhibition Assay		72 h	IC50=0.4 nM	23412931
MV4-11	Growth Inhibition Assay		72 h	IC50=0.3 nM	23412931
Pat.368	Apoptosis Assay			IC50=2998 nM	23497317
Pat.601	Apoptosis Assay			IC50=876 nM	23497317
GIST822	Apoptosis Assay			IC50=109 nM	23497317
MV4;11	Apoptosis Assay			IC50=2 nM	23497317
M-07e + SCF	Apoptosis Assay			IC50=78 nM	23497317
EOL-1	Apoptosis Assay			IC50< 1 nM	23497317
p815	Apoptosis Assay			IC50=341 nM	23497317
Kasumi-1	Apoptosis Assay			IC50=67 nM	23497317
Pat.368	Growth Inhibition Assay			IC50=2700 nM	23497317
Pat.601	Growth Inhibition Assay			IC50=1153 nM	23497317
Pat.379	Growth Inhibition Assay			IC50=806 nM	23497317
HL60/VCR	Function Assay	0.1-10 μM	30 min	enhances uptake of substrates of ABCG2 and ABCB1 in a concentration-dependent manner	23967177
K562/ABCG2	Function Assay	0.1-10 μM	30 min	enhances uptake of substrates of ABCG2 and ABCB1 in a concentration-dependent manner	23967177
MCF-7 FLV1000	Kinase Assay	0–30 µM	5 min	decreases [125I]-IAAP photolabeling of ABCB1 at IC50 of 3.3 μM	23967177
MCF-7 FLV1000	Kinase Assay	0–30 µM	5 min	decreases [125I]-IAAP photolabeling of ABCB2 at IC50 of 0.07 μM	23967177
8226/MR20	Cell Viability Assays	0.1 µM	96 h	sensitizes K562/ABCG2 cells to	23967177
K562/ABCG2	Cell Viability Assays	0.1/0.5/1 µM	96 h	sensitizes K562/ABCG2 cells to	23967177
HMC1.1	Growth Inhibition Assay			IC50=14 nM	23497317
p815	Growth Inhibition Assay			IC50=445 nM	23497317
M-07e + SCF	Growth Inhibition Assay			IC50=77 nM	23497317
Kasumi-1	Growth Inhibition Assay			IC50=36 nM	23497317
MV4;11	Growth Inhibition Assay			IC50< 1 nM	23497317
Pat.221	Growth Inhibition Assay			IC50=675 nM	23497317
MOLM14	Growth Inhibition Assay			IC50< 1 nM	23497317
Pat.299	Growth Inhibition Assay			IC50=7248 nM	23497317
Pat.279	Growth Inhibition Assay			IC50=3434 nM	23497317
Pat.305	Growth Inhibition Assay			IC50=7079 nM	23497317
MV4-11	Function assay	1 nM	1 hr	Inhibition of FLT3 ITD mutant autophosphorylation at Y589/591 in human MV4-11 cells at 1 nM after 1 hr by immunoblot analysis	29672049
BA/F3	Function assay		72 hrs	Inhibition of FLT3 ITD mutant (unknown origin) transfected in mouse BA/F3 cells assessed as growth inhibition after 72 hrs by calcein AM dye-based fluorescence assay, GI50 = 0.007 μM.	29672049
OHS-50	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
LAN-5	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
NB4	Antiproliferative assay		72 hrs	Antiproliferative activity against human NB4 cells expressing FLT3 kinase after 72 hrs by CellTiter-Glo assay, GI50 = 7.3 μM.	28956923
BAF3	Antiproliferative assay		72 hrs	Antiproliferative activity against TEL-fused PDGFRalpha-transformed mouse BAF3 cells after 72 hrs by CellTiter-Glo assay, GI50 = 0.0003 μM.	28956923
MOLM14	Antiproliferative assay		72 hrs	Antiproliferative activity against human MOLM14 cells harboring FLT3-ITD mutation after 72 hrs by CellTiter-Glo assay, GI50 = 0.0003 μM.	28956923
MOLM13	Antiproliferative assay		72 hrs	Antiproliferative activity against human MOLM13 cells harboring FLT3-ITD mutation after 72 hrs by CellTiter-Glo assay, GI50 = 0.0003 μM.	28956923
MV4-11	Growth inhibition assay			Growth inhibition of human MV4-11 cells harboring FLT3-ITD mutant by XTT assay, GI50 = 1.103 μM.	28043794
Sf21	Function assay		10 mins	Inhibition of N-terminal GST-tagged recombinant human wild-type FLT3 (564 to end residues) expressed in baculovirus infected sf21 cells using Abltide as substrate in presence of [gamma33P]ATP after 10 mins by scintillation counting method, IC50 = 0.0255 μM.	28043794
K562	Growth inhibition assay		48 hrs	Growth inhibition of human K562 cells after 48 hrs by XTT assay, GI50 = 2.638 μM.	27187860
MV4-11	Cytotoxicity assay		72 hrs	Cytotoxicity against human MV4-11 cells incubated for 72 hrs by MTT assay, IC50 = 0.00068 μM.	26142317
MV4-11	Antitumor assay	10 mg/kg	48 days	Antitumor activity against human MV4-11 cells xenografted in nude mouse assessed as tumor regression at 10 mg/kg, po qd administered on day 8 to 12 measured during 48 days post last dose	26081023
Sf9	Function assay		4 hrs	Inhibition of wild type GST-tagged FLT3 kinase domain (Y567 to S993) (unknown origin) expressed in baculovirus infected insect Sf9 cells using Her2 peptide as substrate after 4 hrs by Kinase-Glo assay, IC50 = 0.069 μM.	26081023
MV4-11	Antitumor assay	1 mg/kg/day	30 days	Antitumor activity against human MV4-11 cells xenografted mouse bone marrow engraftment model assessed as increase mouse life span at 1 mg/kg/day, po for 30 days measured on day 77 post dose	19654408
AML	Cytotoxicity assay			Cytotoxicity against human AML cells isolated from relapsed acute myeloid leukemia patient harboring FLT3 ITD mutation by MTT assay, IC50 = 0.0003 μM.	19654408
SEM-K2	Apoptosis Assay		8/24 h	induces significant and dose-dependent PARP cleavage and accumulation of sub-2N DNA	23412931
MOLM-14	Apoptosis Assay		8/24 h	induces significant and dose-dependent PARP cleavage and accumulation of sub-2N DNA	23412931
MV4-11	Apoptosis Assay		8/24 h	induces significant and dose-dependent PARP cleavage and accumulation of sub-2N DNA	23412931
MOLM14	Apoptosis Assay			IC50=3 nM	23497317
HMC1.1	Apoptosis Assay			IC50=31 nM	23497317
K562/ABCB1	Function Assay	0.1-10 μM	30 min	enhances uptake of substrates of ABCG2 and ABCB1 in a concentration-dependent manner	23967177
8226/MR20	Function Assay	0.1-10 μM	30 min	enhances uptake of substrates of ABCG2 and ABCB1 in a concentration-dependent manner	23967177
HMC1.2	Growth Inhibition Assay			IC50=1727 nM	23497317
EOL-1	Growth Inhibition Assay			IC50=1 nM	23497317
Pat.375	Growth Inhibition Assay			IC50=503 nM	23497317
MV4-11	Function assay	1 nM	1 hr	Inhibition of FLT3 ITD mutant autophosphorylation at Y842 in human MV4-11 cells at 1 nM after 1 hr by immunoblot analysis	29672049
MV4-11	Function assay	0.01 to 100 nM	1 hr	Inhibition of FLT3 ITD mutant in human MV4-11 cells assessed as decrease in STAT5 phosphorylation at Y694 at 0.01 to 100 nM after 1 hr by immunoblot analysis	29672049
MV4-11	Function assay	0.01 to 100 nM	1 hr	Inhibition of FLT3 ITD mutant in human MV4-11 cells assessed as decrease in ERK1/2 phosphorylation at T202/Y204 at 0.01 to 100 nM after 1 hr by immunoblot analysis	29672049
MV4-11	Function assay	10 mg/kg	24 hrs	In vivo inhibition of FLT3 ITD mutant in human MV4-11 cells xenografted in athymic nu/nu mouse assessed as decrease in STAT5 phosphorylation at Y694 at 10 mg/kg, ip after 24 hrs by immunoblot method relative to control	29672049
MV4-11	Function assay	0.1 uM	4 hrs	Inhibition of FLT3 in human MV4-11 cells assessed as reduction in AKT phosphorylation at Ser473 residue at 0.1 uM after 4 hrs by Western blot analysis	29894944
MV4-11	Function assay	0.1 uM	4 hrs	Inhibition of FLT3 in human MV4-11 cells assessed as reduction in STAT5 phosphorylation at Tyr694 residue at 0.1 uM after 4 hrs by Western blot analysis	29894944
MV4-11	Function assay	0.1 uM	4 hrs	Inhibition of FLT3 in human MV4-11 cells assessed as reduction in ERK1/2 phosphorylation at Thr202/Tyr204 residues at 0.1 uM after 4 hrs by Western blot analysis	29894944
MV4-11	Function assay	0.1 uM	4 hrs	Inhibition of FLT3 phosphorylation at Tyr589/591 residues in human MV4-11 cells at 0.1 uM after 4 hrs by Western blot analysis	29894944
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生物活性

产品描述

特性

AC220是二代FLT3抑制剂，且作为临床FLT3抑制剂的第一候选药。

靶点

FLT3 (ITD) ^[1] (MV4-11 cells)	FLT3 (WT) ^[1] (RS4;11 cells)
1.1 nM	4.2 nM

体外研究(In Vitro)
体外研究活性	AC220是最有效的FLT3选择性抑制剂，可用于治疗急性骨髓性白血病(AML)。AC220在生化和细胞实验中具有低纳摩尔效果和特别的激酶选择性，抑制大部分人类蛋白激酶时具有高选择性。AC220是治疗急性骨髓性白血病(AML)的新型FLT3抑制剂。^[1]
激酶实验	激酶实验
激酶实验	为了测定AC220抑制无靶点激酶的效果，为了比较AC220和其他FLT抑制剂的选择性,使AC220作用于KinomeScan一组402种激酶进行结合试验，其中80%为典型的人类蛋白激酶。测定所有激酶的解离常数。计算绝对选择性和作用于FLT的相对选择性。
细胞实验	细胞系	MV4-11和RS4;11细胞
	浓度	0-100 nM
	孵育时间	72小时，及2小时
	方法	在增殖实验中，细胞培养在低血清培养基(含0.5% FBS)中过夜, 然后按每孔4×10⁴个细胞接种在96孔板上，然后加入AC220，37^oC下温育72小时。测定细胞活力。测定抑制FLT3自磷酸化的效果, 细胞培养在低血清培养基(含0.5% FBS)过夜，然后按每孔4×10⁵个细胞接种在96孔板上。细胞和AC220一起在37^oC下温育2小时，诱导 RS4;11细胞中FLT3自磷酸化, 加入100 ng/mL FLT3配位体，持续15分钟。转移细胞溶解物到用FLT3抗体包被的96孔板上。然后加入作用于FLT3的生物素化抗体，测定全部FLT3，或者作用于磷酸酪氨酸的抗体，测定FLT3自磷酸化。使用 SULFO标记的链霉亲和素二抗进行电化学发光测定。
实验图片	检测方法	检测指标	实验图片	PMID
	Western blot	p-STAT5 / STAT5 / β-catenin / p-AKT / AKT / p-ERK / ERK / p-S6 / S6 phospho-FLT3 / FLT3		28625976
	Immunofluorescence	WGA / FLT3		28895560
	Growth inhibition assay	Cell viability		23967177

体内研究(In Vivo)
体内研究活性	AC220作用于移植瘤模型，具有好的药品属性，极高的药效和耐受性。在体内，AC220作用于FLT3-ITD AML鼠模型，抑制FLT3活性,明显延长寿命；作用于依赖FLT3的移植瘤鼠模型时，根除肿瘤；作用于病人原代细胞时，有效抑制FLT3活性。^[1]
动物实验	Animal Models	雌性裸鼠或严重联合免疫缺陷鼠
	Dosages	10 mL/kg
	Administration	口服饲喂处理

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT04473664	Completed	Hepatic Impairment\|Moderate Impaired Hepatic Function	Daiichi Sankyo	September 22 2020	Phase 1
NCT04459585	Completed	Healthy Subjects\|Drug-drug Interaction\|Pharmacokinetics\|Quizartinib	Daiichi Sankyo Co. Ltd.\|Daiichi Sankyo	August 28 2020	Early Phase 1
NCT04459598	Completed	Healthy Subjects\|Drug-drug Interaction\|Pharmacokinetics\|Quizartinib	Daiichi Sankyo Co. Ltd.\|Daiichi Sankyo	August 19 2020	Phase 1
NCT04209725	Terminated	Leukemia Myeloid Acute	SCRI Development Innovations LLC	June 3 2020	Phase 2

参考文献
[1] Zarrinkar PP, et al. Blood, 2009, 114(14), 2984-2992.

参考文献

[1] Zarrinkar PP, et al. Blood, 2009, 114(14), 2984-2992.

化学信息&溶解度

分子量	560.67	分子式	C₂₉H₃₂N₆O₄S
CAS号	950769-58-1	SDF	Download Quizartinib (AC220) SDF
Smiles	CC(C)(C)C1=CC(=NO1)NC(=O)NC2=CC=C(C=C2)C3=CN4C5=C(C=C(C=C5)OCCN6CCOCC6)SC4=N3
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 100 mg/mL ( (178.35 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 100 mg/mL ( (178.35 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 33.2 mg/mL ( (59.21 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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操作手册

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* 必填项

常见问题及建议解决方法

问题 1:
Is it possible to alter the captisol concentration to make it more dissolvable i.e 20% or 25% captisol ?

回答：
In 15% Captisol, the compound forms s suspension at 30mg/ml. Increasing the percentage of Captisol will not convert the mixture into solution. You can use suspension for oral gavage feeding.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):