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Ko 143

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Chemical Structure| 461054-93-3 同义名 : -
CAS号 : 461054-93-3
货号 : A414772
分子式 : C26H35N3O5
纯度 : 99+%
分子量 : 469.573
MDL号 : MFCD11042273
存储条件:

粉末 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: 105 mg/mL(223.61 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:
生物活性
描述 Ko 143, a potent inhibitor specific to ATP-binding cassette subfamily G member 2 (ABCG2/BCRP), exhibits over 200-fold selectivity against P-gp and MRP-1 transporters[1][2]. At a concentration of 10 nM, Ko 143 notably reduces the IC50 of MTX for HEK G2 cells and mouse G2 cells by 2.5 times. However, Ko143 metabolites, ranging from 1-100 μM, do not affect the function of ABC Transporters[1]. The drug resistance reversal in Topotecan-selected mouse MEF3.8/T6400 cells and human IGROV1/T8 cells is achieved by the FTC analogue Ko 143, applied at 0, 1, or 8 times the EC90 concentration of 25 nM[2]. Ko 143 also blocks the BCRP-mediated transport of ZD 4522 in both wild type Madin-Darby Canine Kidney (MDCK) 2-BCRP421CC cells and mutant MDCK2-BCRP421AA cells[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.65mL

2.13mL

1.06mL

21.30mL

4.26mL

2.13mL

参考文献

[1]Weidner LD, et al. The Inhibitor Ko143 Is Not Specific for ABCG2. J Pharmacol Exp Ther. 2015 Sep;354(3):384-93.

[2]JD Allen et al. Potent and Specific Inhibition of the Breast Cancer Resistance Protein Multidrug Transporter in Vitro and in Mouse Intestine by a Novel Analogue of Fumitremorgin C. Mol. Cancer Ther. 2002, 1, 417-425.

[3]Wen JH, et al. Effect of Ursolic Acid on Breast Cancer Resistance Protein-mediated Transport of ZD 4522 In Vivo and Vitro. Chin Med Sci J. 2015 Dec;30(4):218-25.