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Elacridar

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Chemical Structure| 143664-11-3 同义名 : GG918;GF120918;GW120918;GW0918
CAS号 : 143664-11-3
货号 : A351095
分子式 : C34H33N3O5
纯度 : 99%+
分子量 : 563.643
MDL号 : MFCD00912604
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 4 mg/mL(7.1 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+2% Tween80+40% PEG300+water 1 mg/mL clear

PO 0.5% CMC-Na 70 mg/mL suspension

生物活性
靶点

  • P-gp
描述 The multidrug resistance is an obstacle in the chemotherapy treatment for many solid and haematological tumours. Many factors can cause the multidrug resistance. Among them, the overexpression of P-gp (ABCB1), an ATP-binding cassette (ABC) drug efflux transporter, on the surface of resistant cells is considered as a key factor mediating multidrug resistance. Elacridar is a dual inhibitor of P-gp/BCRP, which can completely inhibit directed transport of crizotinib by P-gp at concentration of 5μM in MDCKII cells expressing human ABCB1. Elacridar is usually used combined with other anticancer drugs to increase the bio-available, achieve higher plasma concentration and improve brain accumulation of these anticancer drugs, such as tyrosine kinase inhibitor (TKI) . Coadministration of elacridar at dose of 100mg/kg could increase the plasma and brain concentrations and brain/plasma ratio of crizotinib in mice, suggesting that the effect of elacridar on increasement of crizotinib oral availability and delivery to the brain[1].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
Caco-2 cells Function assay Inhibition of human P-gp mediated [3H]vinblastine transport activity in human Caco-2 cells, EC50=2 μM 18276145
HEK293 cells Function assay Inhibition of ABCG2 expressed in HEK293 cells assessed as mitoxantrone-mediated efflux by flow cytometry, IC50=0.41 μM 17317193
Kb-V1 cells Function assay 10 mins Inhibition of ABCB1 expressed in Kb-V1 cells after 10 mins by calcein-AM assay, IC50=0.193 μM 21570282
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.77mL

0.35mL

0.18mL

8.87mL

1.77mL

0.89mL

17.74mL

3.55mL

1.77mL
参考文献

[1]Kuntner C, Bankstahl JP, et al. Dose-response assessment of tariquidar and elacridar and regional quantification of P-glycoprotein inhibition at the rat blood-brain barrier using (R)-[(11)C]verapamil PET. Eur J Nucl Med Mol Imaging. 2010 May;37(5):942-53.

[2]Sane R, Agarwal S, et al. Brain distribution and bioavailability of elacridar after different routes of administration in the mouse. Drug Metab Dispos. 2012 Aug;40(8):1612-9.