Xcess/AC220-Xcessbio Biosciences Inc/10mg/M60435-10s,Xcess,,Xcess,xcessbio,Xcess Biosciences Inc,+,,Array.Array蚂蚁淘厂家直采.

产品名称：Xcess/AC220-Xcessbio Biosciences Inc/10mg/M60435-10s

产品编号：M60435-10s

市场价：¥4180.00

场地：美国(厂家直采)

产品分类：蛋白类>聚合物>

联系QQ：1570468124

电话号码：4000-520-616

邮箱： info@ebiomall.com

美元价：$209.00

品牌： Xcess

公司：Xcess Biosciences, Inc

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商品介绍

Details

Product Information

Molecular Weight:	560.67
Formula:	C₂₉H₃₂N₆O₄S
Purity:	>98%
CAS#:	950769-58-1
Solubility:	DMSO: ≥ 33 mg/mL
Chemical Name:	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
Storage:	Powder -20^oC 3 years 4^oC 2 yearsIn solvent -80^oC 6 months-20^oC 1 month

Biological Activity:

Quizartinib is a uniquely potent and selective Flt3 inhibitor with Kd (FLT3 binding affinity) of 1.6±0.7 nM in Biochemical assay.

How to use:

In Vitro: Quizartinib (AC220) is a novel compound expressly optimized as a FLT3 inhibitor for the treatment of acute myeloid leukemia (AML). Quizartinib inhibits FLT3-WT and FLT3-ITD autophosphorylation with IC50 of 4.2±0.3 nM and 1.1±0.1 nM, respectively. Quizartinib inhibits MV4-11 and A375 cells with IC50 of 0.56±0.3 nM and >10 000 nM, respectively. Quizartinib inhibits FLT3 with low nanomolar potency in cellular assays and is highly selective when screened against the majority of the human protein kinome[1].

In Vivo: Quizartinib (AC220) inhibits FLT3 activity in vivo, significantly extends survival in a mouse model of FLT3-ITD AML at doses as low as 1 mg/kg when dosed orally once a day, eradicates tumors in a FLT3-dependent mouse xenograft model at 10 mg/kg, and potently inhibits FLT3 activity in primary patient cells. The oral bioavailability of Quizartinib, determined in rats by comparing oral and intravenous pharmacokinetics at 3 mg/kg, is approximately 40%. A single 10 mg/kg dose of Quizartinib is administered by oral gavage, and mice are killed at 2 time points after dosing, using groups of 4 animals each. Quantitation of total FLT3 and phospho-FLT3 in tumor samples revealed time-dependent inhibition of FLT3 autophosphorylation. FLT3 activity is inhibited by 90% at 2 hours, and 40% at 24 hours after administration. The extent of inhibition therefore correlated well with the expected free Quizartinib plasma levels, based on pharmacokinetic experiments[1].

Reference:

[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]. Puissant A, et al. SYK is a critical regulator of FLT3 in acute myeloid leukemia. Cancer Cell. 2014 Feb 10;25(2):226-42.

品牌介绍

Xcess Biosciences，Inc.（XcessBio）由一群来自学术界和制药/生物技术行业的顶尖科学家于2008年成立，他们在药物化学，生物化学，分子和细胞生物学领域拥有丰富的专业知识。结合我们的合作者和顾问网络，我们致力于开发高质量的产品并提供最佳的服务，以满足生物医学研究中未满足的需求。

XcessBio的总部位于加利福尼亚州圣地亚哥，在最先进的研发设施中运营，设有化学合成实验室，分子和细胞生物学实验室以及分析质量控制实验室。

XcessBio一直为美国许多顶级制药，生物技术和试剂公司提供CRO服务和OEM产品，现在，我们将最好的产品和服务直接扩展到整个生命科学界。

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