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Quizartinib

产品编号 T2066 CAS 950769-58-1

别名: AC220, 奎扎替尼

Quizartinib (AC220) 是一种具有口服活性的高选择性Ⅱ 型 FLT3酪氨酸激酶抑制剂，可诱导细胞凋亡。它抑制 Wt FLT3 和突变型 FLT3-ITD 自磷酸化，IC50分别为 4.1 nM 和 1.1 nM。它可通过优化的 linker 与 VHL 配体连接，从而形成 PROTAC Flt3 降解剂。

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Quizartinib, CAS 950769-58-1

规格	价格/CNY	货期
1 mg	￥ 297	现货
5 mg	￥ 727	现货
10 mg	￥ 1,080	现货
25 mg	￥ 1,980	现货
50 mg	￥ 3,520	现货
100 mg	￥ 4,710	现货
200 mg	￥ 6,710	现货
500 mg	￥ 9,990	现货
1 mL * 10 mM (in DMSO)	￥ 877	现货

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其他形式的 Quizartinib:

Quizartinib HCl
询价

选择批次

纯度: 99.42%

纯度: 98.87%

纯度: 98%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Quizartinib (AC220) is an inhibitor of FLT3 (Kd: 1.6 nM) and demonstrates high selectivity for FLT3 when tested against a panel of 227 additional kinases.
靶点活性	FLT3:1.6 nM (Kd, cell free)
体外活性	The highest affinity target identified for Quizartinib (AC220) was FLT3. The only other kinases with binding constants within 10-fold that for FLT3 were the closely related receptor tyrosine kinases (RTKs) KIT, PDGFRA, PDGFRB, RET, and CSF1R, and only 4 additional kinases, also related RTKs (FLT1, FLT4, DDR1, VEGFR2), bound with Kds within 100-fold of that for FLT3. In primary cells, treatment with AC220 for 1 hour inhibited FLT3 autophosphorylation (IC50: 2 nM), comparable with the activity observed in the MV4-11 cell line. The primary cells were sensitive to AC220 (IC50: 0.3 nM), again comparable with the activity observed in the MV4-11 cell line [1]. It inhibits the proliferation of the human leukemia cell line MV4-11, which harbors a homozygous FLT3-ITD mutation, with an IC50 value of 0.56 nM [2].
体内活性	Treatment with AC220 at 10 mg/kg resulted in rapid and complete regression of tumors in all animals, and no tumor regrowth was observed during the 60-day posttreatment observation period. AC220 prolonged survival in a dose-dependent manner. At 10 mg/kg, 80% of animals treated survived until the study was terminated on day 172, 119 days after discontinuation of treatment, corresponding to at least a 250% increase in life span (ILS). At the time the study was terminated the animals did not exhibit any signs of disease. At 1 mg/kg a significant increase in the mean survival time was observed, to 77 days. At the lowest dose tested of 0.1 mg/kg, a marginal 10% ILS relative to vehicle was observed [1]. At 1 mg/kg of AC220, tumor growth was completely inhibited during the dosing period, after which growth resumed. At 3 and 10 mg/kg of AC220, tumors regressed almost completely and the tumor volume stayed suppressed after dosing was halted. At 3 mg/kg, tumors appeared to regrow after day 49 (21 days post last dose), while there was no sign of tumor regrowth until day 60 (32 days post last dose) in the animals treated with 10 mg/kg of AC220 [2].
激酶实验	KinomeScan kinase binding assays were performed as previously described. For the FLT3 assay, we used a kinase construct that spanned the catalytic domain only (amino acids 592 to 969 in NP_004110.2). This construct does not include the juxtamembrane domain and is designed to measure the intrinsic binding affinity of the open FLT3 active site for inhibitors [1].
细胞实验	MV4-11 and RS4;11 cells were cultured in Iscove media with 10% fetal bovine serum (FBS) and RPMI complete with 10% FBS, respectively. For proliferation assays, cells were cultured overnight in low serum media (0.5% FBS), then seeded in a 96-well plate at 40 000 cells per well. Inhibitors were added to the cells and incubated at 37°C for 72 hours. Cell viability was measured using the Cell Titer-Blue Cell Viability Assay. To measure inhibition of FLT3 autophosphorylation, cells were cultured in low serum media (0.5% FBS) overnight and seeded at a density of 400 000 cells per well in a 96-well plate the following day. The cells were incubated with inhibitors for 2 hours at 37°C. To induce FLT3 autophosphorylation in RS4;11 cells, 100 ng/mL FLT3 ligand was added for 15 minutes after the 2-hour compound incubation. Cell lysates were prepared and incubated in 96-well plates pre-coated with a total FLT3 capture antibody. The coated plates were incubated with either a biotinylated antibody against FLT3 to detect total FLT3 or an antibody against phosphotyrosines to detect FLT3 autophosphorylation. In both cases, a SULFO-tagged streptavidin secondary antibody was used for electrochemiluminescence detection on the Meso Scale Discovery platform [1].
动物实验	The model was performed according to published procedures.20 For intravenous bone marrow engraftment, nonobese diabetic/severe combined immunodeficient mice were acclimated for 2 weeks before pretreatment with 150 mg/kg cyclophosphamide delivered intraperitoneally once a day for 2 days. After a 48-hour rest period, animals were given an intravenous injection of 5 × 10^6 MV4-11 cells into the tail vein. AC220 was formulated and delivered as described for pharmacokinetic studies [1].

别名	AC220, 奎扎替尼
化合物与蛋白结合的复合物	Crystal structure of the FLT3 kinase domain bound to the inhibitor quizartinib (AC220)
分子量	560.67
分子式	C29H32N6O4S
CAS No.	950769-58-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 33.2 mg/mL (59.21 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7836 mL	8.9179 mL	17.8358 mL	44.5895 mL
	5 mM	0.3567 mL	1.7836 mL	3.5672 mL	8.9179 mL
	10 mM	0.1784 mL	0.8918 mL	1.7836 mL	4.459 mL
	20 mM	0.0892 mL	0.4459 mL	0.8918 mL	2.2295 mL
	50 mM	0.0357 mL	0.1784 mL	0.3567 mL	0.8918 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

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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. 2. Chao Q, et al. Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor. J Med Chem. 2009 Dec 10;52(23):7808-16.

文献引用

1. Zhang Y, Wang P, Wang Y, et al.Sitravatinib as a potent FLT3 inhibitor can overcome gilteritinib resistance in acute myeloid leukemia.Biomarker Research.2023, 11(1): 1-16. 2. Huang F, Liang J, Lin Y, et al.Repurposing of Ibrutinib and Quizartinib as potent inhibitors of necroptosis.Communications Biology.2023, 6(1): 972. 3. Wang P, Zhang Y, Xiang R, et al.Foretinib is effective in acute myeloid leukemia by inhibiting FLT3 and overcoming secondary mutations that drive resistance to quizartinib and gilteritinib.Cancer Research.2024

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Quizartinib 950769-58-1 Angiogenesis Apoptosis Autophagy PROTAC Tyrosine Kinase/Adaptors FLT Ligands for Target Protein for PROTAC AC-220 Inhibitor myeloid FLT3-ITD oral Fms like tyrosine kinase 3 AC220 Target Protein-binding Moiety mutation inhibit CD135 AML leukemia 奎扎替尼 acute AC 220 Cluster of differentiation antigen 135 FLT3 selective inhibitor

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Quizartinib

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

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