计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
Quizartinib (AC220), 集落刺激因子 1 受体抑制剂；FMS 相关受体酪氨酸激酶 3 抑制剂；KIT 原癌基因受体酪氨酸激酶抑制剂；血小板衍生生长因子受体 alpha 抑制剂；血小板衍生生长因子受体 beta 抑制剂；ret 原癌基因抑制剂
有货
概述
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。Phase 3。An Flt-3/Flk-2 inhibitor.
Information
Quizartinib (AC220) is a second-generation FLT3 inhibitor for Flt3(ITD/WT) with IC50 of 1.1 nM/4.2 nM in MV4-11 and RS4;11 cells, respectively, 10-fold more selective for Flt3 than KIT, PDGFRα, PDGFRβ, RET, and CSF-1R. Quizartinib (AC220) induces apoptosi
In vitro
AC220, a unique, potent and selective inhibitor of FLT3, has high affinity for FLT3 with a Kd value of 1.6 nM. AC220 inhibits the autophosphorylation of FLT3 in the human leukemia cell lines MV4-11 which harbor a homozygous FLT3-ITD mutation and is FLT3 dependent, and RS4;11 which expresses wild-type FLT3 with IC50 values of 1.1 nM and 4.2 nM, respectively. AC220 is the most potent cellular FLT3-ITD inhibitor, leading to the most significant inhibition of MV4-11 cell proliferation with IC50 of 0.56 nM compared to all other FLT3 inhibitors whose IC50 values range from 0.87 nM to 64 nM. AC220 has no inhibitory activity against the proliferation of A375 cells which harbor an activating mutation in BRAF and are not FLT3 dependent, indicating a large window between FLT3 inhibition and general cytotoxic effects.
In vivo
Oral administration of AC220 (10 mg/kg) induces time-dependent inhibition of FLT3 autophosphorylation in the FLT3-ITD–dependent MV4-11 tumor xenograft mouse model; the inhibition being 90% at 2 hours and 40% at 24 hours. AC220 significantly extends survival in a mouse model of FLT3-ITD AML with doses as low as 1 mg/kg given orally once a day. Treatment with AC220 at 10 mg/kg for 28 days results in rapid and complete regression of tumors in all mice with no tumor regrowth during the 60-day posttreatment period. AC220 displays more significant efficacy compared to sunitinib treatment which causes tumors to shrink slowly and resume growth immediately upon discontinuation of treatment in all but one of the mice.
Cell Data
cell lines：
Concentrations：Dissolved in DMSO, final concentration ~20 μM
Incubation Time：72 hours
Powder Purity:≥98%
规格
别名
奎扎替尼 (AC220)
英文别名
Urea, N-[5-(1,1-dimethylethyl)-3-isoxazolyl]-N'-[4-[7-[2-(4-morpholinyl)ethoxy]imidazo[2,1-b]benzothiazol-2-yl]phenyl]-
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Quizartinib (AC220)
生化机理
Quizartinib（AC220）是第二代FLT3抑制剂，在MV4-11和RS4;11细胞中对Flt3(ITD/WT)的IC50分别为1.1 nM/4.2 nM，对Flt3的选择性是KIT、PDGFRα、PDGFRβ、RET和CSF-1R的10倍。Quizartinib（AC220）可诱导肿瘤细胞凋亡。第 3 阶段
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
集落刺激因子 1 受体抑制剂；FMS 相关受体酪氨酸激酶 3 抑制剂；KIT 原癌基因受体酪氨酸激酶抑制剂；血小板衍生生长因子受体 alpha 抑制剂；血小板衍生生长因子受体 beta 抑制剂；ret 原癌基因抑制剂
名称和识别符
EC号
107-677-2
分子类型
小分子
Isomeric SMILES
CC(C)(C)C1=CC(=NO1)NC(=O)NC2=CC=C(C=C2)C3=CN4C5=C(C=C(C=C5)OCCN6CCOCC6)SC4=N3
PubChem CID
分子量
560.68
高级数据
关联靶点（人）
CSF1R
Tclin
巨噬细胞集落刺激因子 1 受体(Macrophage colony-stimulating factor 1 receptor)
(7 活性数据)
RET
Tclin
原癌基因酪氨酸蛋白激酶受体 Ret(Proto-oncogene tyrosine-protein kinase receptor Ret)
(13 活性数据)
FLT3
Tclin
受体型酪氨酸蛋白激酶 FLT3(Receptor-type tyrosine-protein kinase FLT3)
(43 活性数据)
PDGFRA
Tclin
血小板衍生生长因子受体α(Platelet-derived growth factor receptor alpha)
(7 活性数据)
PDGFRB
Tclin
血小板衍生的生长因子受体β(Platelet-derived growth factor receptor beta)
(7 活性数据)
KIT
Tclin
肥大细胞/干细胞生长因子受体试剂盒(Mast/stem cell growth factor receptor Kit)
(14 活性数据)
MYH10
Tchem
肌球蛋白-10(Myosin-10)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 100 mg/mL (194.35 mM);
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
技术文档和文章
此产品的引用文献
溶液计算器
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