1353747-12-2
Chemical Structure
MBL-II-141
- CAS No.: 1353747-12-2
- Formula:C28H23BrN2O5
- Molecular Weight:547.40
SMILES: O=C(C1=CC(C2=C(OCC3=CC=C(Br)C=C3)C=CC=C2O1)=O)NCCC4=CNC5=C4C=C(OC)C=C5
Biological Activity: MBL-II-141 is potent ABCG2 inhibitor with an IC50 of 0.11 μM. MBL-II-141 inhibits the transport function of ABCG2 in a non-competitive manner, preventing ABCG2 from pumping substrates (such as Irinotecan (HY-16562)) out of the cells, thereby increasing the accumulation of drugs within the cells. MBL-II-141 has no effect on ABCB1 (P-gp) and ABCC1 (MRP1) and has extremely low cytotoxicity (IG50 > 100 μM). MBL-II-141 can be used for the study of multidrug resistance (MDR) cancers[1][2].
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MBL-II-141 | MBL-II-141 is potent ABCG2 inhibitor with an IC50 of 0.11 μM. MBL-II-141 inhibits the transport function of ABCG2 in a non-competitive manner, preventing ABCG2 from pumping substrates (such as Irinotecan (HY-16562)) out of the cells, thereby increasing the accumulation of drugs within the cells. MBL-II-141 has no effect on ABCB1 (P-gp) and ABCC1 (MRP1) and has extremely low cytotoxicity (IG50 > 100 μM). MBL-II-141 can be used for the study of multidrug resistance (MDR) cancers. | |||||||||||||||||||||
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References
- [1]. Hénin E, et al. Pharmacokinetic interactions in mice between irinotecan and MBL-II-141, an ABCG2 inhibitor. Biopharm Drug Dispos. 2017 Jul;38(5):351-362. [Content Brief]
- [2]. Payen L, et al. MBL-II-141, a chromone derivative, enhances irinotecan (CPT-11) anticancer efficiency in ABCG2-positive xenografts. Oncotarget. 2014 Dec 15;5(23):11957-70. [Content Brief]
