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Quizartinib

奎扎替尼; AC220

Quizartinib (AC220)是一种二代FLT3抑制剂，作用于Flt3(ITD/WT)，IC50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。

目录号
EY0967
EY0967
EY0967
EY0967
纯度
99.18%
99.18%
99.18%
99.18%
规格
1 mg
5 mg
10 mg
50 mg
原价
389
890
1400
4000
售价
389
890
1400
4000
库存
现货
现货
现货
现货
订购
订购
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  • 生物活性

    Quizartinib (AC-220) is a second-generation FLT3 receptor tyrosine kinase inhibitor, which has high affinity for FLT3 in a binding assay (Kd = 1.6 nM) and is a potent inhibitor in cellular autophosphorylation assays (IC50 = 1.1 nM for FLT3-ITD and 4.2 nM for wt FLT3). In binding assays, quizartinib has demonstrated a high affinity for FLT3 (Kd = 1.6 nM). in vitro assays examining FLT3 internal tandem duplicate mutations and wild-type FLT3 demonstrate the ability of quizartinib to inhibit FLT3 autophosphorylation (IC50 = 1.1 nM for FLT3-ITD and 4.2 nM for wt FLT3).

  • 体外研究

  • 体内研究

    15% Captisol

  • 激酶实验

  • 细胞实验

    0-100 nM

  • 动物实验

    10 mL/kg 口服饲喂处理

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Zarrinkar PP, et al. Blood, 2009, 114(14), 2984-2992.
    [2] Pratz, Keith W., et al., 2010. FLT3-mutant allelic burden and clinical status are predictive of response to FLT3 inhibitors in AML. Blood. 115(7): 1425-32.
    [3] Sato, Takashi., et al., 2011. FLT3 ligand impedes the efficacy of FLT3 inhibitors in vitro and in vivo. Blood. 117(12): 3286-93.

    分子式
    C29H32N6O4S    		 分子量
    560.67    		 CAS号
    950769-58-1    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    >20 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT02984995 Leukemia, Myeloid, Acute Drug: Quizartinib Daiichi Sankyo Co., Ltd.|Daiichi Sankyo Inc. 2016-12-01 2016-12-13
    NCT02039726 AML Drug: Quizartinib|Drug: Salvage Chemotherapy Daiichi Sankyo Inc. Phase 3 2014-04-01 2016-12-09
    NCT01892371 Leukemia Drug: Quizartinib|Drug: Cytarabine|Drug: AZA M.D. Anderson Cancer Center|Ambit Biosciences Corporation|Celgene|National Cancer Institute (NCI) Phase 1|Phase 2 2013-11-01 2017-03-09
    NCT02668653 Acute Myeloid Leukemia|Leukemia Drug: Cytarabine|Drug: Daunorubicin|Drug: Idarubicin|Drug: Quizartinib|Drug: Placebo Daiichi Sankyo Inc. Phase 3 2016-09-01 2016-10-18
    NCT02834390 Acute Myeloid Leukemia Drug: quizartinib|Drug: Cytarabine|Drug: Idarubicin|Drug: Daunorubicin Daiichi Sankyo Co., Ltd.|Daiichi Sankyo Inc. Phase 1 2016-07-01 2016-08-23
    NCT01565668 Leukemia, Myeloid, Acute Drug: AC220 Daiichi Sankyo Inc.|Ambit Biosciences Corporation Phase 2 2012-04-01 2017-03-17
    NCT02675478 Relapsed AML|Refractory AML Drug: AC220 Daiichi Sankyo Co., Ltd.|Daiichi Sankyo Inc. Phase 1 2016-02-01 2017-02-20
    NCT01576185 Childhood Acute Myeloid Leukemia/Other Myeloid Malignancies Other: laboratory biomarker analysis|Drug: quizartinib|Drug: sorafenib tosylate Children's Oncology Group|National Cancer Institute (NCI) 2012-05-01 2016-05-13
    NCT00462761 Acute Myeloid Leukemia|Leukemia|Myelodysplastic Syndrome|AML|MDS Drug: AC220 Daiichi Sankyo Inc. Phase 1 2007-01-01 2015-10-29
    NCT01468467 Leukemia, Myeloid, Acute Drug: AC220 Daiichi Sankyo Inc.|Ambit Biosciences Corporation Phase 1 2012-04-01 2016-11-30
    NCT01390337 Leukemia, Myeloid, Acute Drug: AC220|Drug: daunorubicin|Drug: cytarabine Daiichi Sankyo Inc.|Ambit Biosciences Corporation Phase 1 2011-10-01 2015-10-29
    NCT02428543 Acute Myeloid Lukemia Drug: Ponatinib and Cytarabine Versailles Hospital Phase 1|Phase 2 2013-07-01 2016-08-19
    NCT02829840 Leukemia|FLT3-Mutated Acute Myeloid Leukemia|FLT3-Mutated High-Risk Myelodysplastic Syndrome Drug: Ponatinib|Drug: 5-azacytidine|Behavioral: Phone Calls M.D. Anderson Cancer Center|Ariad Pharmaceuticals Phase 1|Phase 2 2016-09-01 2016-08-05

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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