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Varlitinib (ARRY334543)ErbB抑制剂

Varlitinib (ARRY334543)

产品编号:A8365
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Sample solution is provided at 25 µL, 10mM.

质量控制

质量控制和MSDS

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化学结构

Varlitinib(ARRY334543)

Varlitinib (ARRY334543) Dilution Calculator

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化学性质

CAS号 845272-21-1 SDF Download SDF
别名 ARRY-334543; ARRY 334543
化学名 4-N-[3-chloro-4-(1,3-thiazol-2-ylmethoxy)phenyl]-6-N-[(4R)-4-methyl-4,5-dihydro-1,3-oxazol-2-yl]quinazoline-4,6-diamine
SMILES CC1COC(=N1)NC2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=NC=CS5)Cl
分子式 C22H19ClN6O2S 分子量 466.94
溶解度 ≥23.35mg/mL in DMSO 储存条件 Store at -20°C
运输条件 试用装:蓝冰运输。
其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

生物活性

Description Varlitinib is a selective and potent inhibitor of ErbB1(EGFR) and ErbB2(HER2) with IC50 values of 7 nM and 2 nM, respectively.
Targets ErbB2 ErbB1        
IC50 2 nM 7 nM        

产品描述

Varlitinib is an orally bioavailable inhibitor of the epidermal growth factor receptor family with potential antineoplastic activity. Varlitinib selectively and reversibly binds to both EGFR (ErbB-1) and Her-2/neu (ErbB-2) and prevents their phosphorylation and activation, which may result in inhibition of the associated signal transduction pathways, inhibition of cellular proliferation and cell death. EGFR and Her-2 play important roles in cell proliferation and differentiation and are upregulated in various human tumor cell types. Due to the dual inhibition of both EGFR and Her-2, this agent may be therapeutically more effective than agents that inhibit EGFR or Her-2 alone.