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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- CAS No.: 1353747-12-2
- 화학식: C28H23BrN2O5
- 분자량:547.40
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.031 μM
Compound: 1
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Inhibition of ABCG2 (unknown origin) transfected in HEK293 cells assessed as inhibition of mitoxantrone efflux at 5 uM after 30 mins in presence of 0.1 uM (2E,2'E)-1,1'-(1,4-Phenylene)bis(3-(2,6-dimethoxyphenyl)-prop-2-en-1-one) by flow cytometry
Inhibition of ABCG2 (unknown origin) transfected in HEK293 cells assessed as inhibition of mitoxantrone efflux at 5 uM after 30 mins in presence of 0.1 uM (2E,2'E)-1,1'-(1,4-Phenylene)bis(3-(2,6-dimethoxyphenyl)-prop-2-en-1-one) by flow cytometry
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[PMID: 24611893] |
| HEK293 | EC50 |
0.094 μM
Compound: 1
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Inhibition of ABCG2 (unknown origin) transfected in HEK293 cells assessed as inhibition of mitoxantrone efflux after 30 mins by flow cytometry relative to control
Inhibition of ABCG2 (unknown origin) transfected in HEK293 cells assessed as inhibition of mitoxantrone efflux after 30 mins by flow cytometry relative to control
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[PMID: 24611893] |
| HEK293 | EC50 |
0.13 μM
Compound: 1
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Inhibition of ABCG2 (unknown origin)-mediated mitoxantrone efflux expressed in HEK293 cells after 30 mins by flow cytometric analysis
Inhibition of ABCG2 (unknown origin)-mediated mitoxantrone efflux expressed in HEK293 cells after 30 mins by flow cytometric analysis
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[PMID: 24304387] |
| HEK293 | EC50 |
0.26 μM
Compound: 4g; MBL-II-141
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Inhibition of ABCG2 (unknown origin) expressed in HEK293 cells assessed as reduction in mitoxantrone efflux after 30 mins by flow cytometric analysis
Inhibition of ABCG2 (unknown origin) expressed in HEK293 cells assessed as reduction in mitoxantrone efflux after 30 mins by flow cytometric analysis
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[PMID: 27376492] |
| HEK293 | IC50 |
0.11 μM
Compound: 6g
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Inhibition of ABCG2-mediated mitoxantrone efflux in HEK293 cells by flow cytometry
Inhibition of ABCG2-mediated mitoxantrone efflux in HEK293 cells by flow cytometry
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[PMID: 22165858] |
| HEK293 | IC50 |
0.13 μM
Compound: 1
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Inhibition of ABCG2 (unknown origin) expressed in HEK293 cells assessed as reduction in mitoxantrone efflux after 30 mins by FACS method
Inhibition of ABCG2 (unknown origin) expressed in HEK293 cells assessed as reduction in mitoxantrone efflux after 30 mins by FACS method
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[PMID: 25272055] |
| Sf9 | IC50 |
0.38 μM
Compound: 1
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Inhibition of human ABCG2 expressed in Sf9 insect cell membranes assessed as inhibition of quercetin-stimulated ATPase activity after 30 mins by colorimetric analysis in presence of sodium orthovanadate
Inhibition of human ABCG2 expressed in Sf9 insect cell membranes assessed as inhibition of quercetin-stimulated ATPase activity after 30 mins by colorimetric analysis in presence of sodium orthovanadate
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[PMID: 24304387] |
In Vivo
MBL-II-141 (10 mg/kg, i.p., single dose) decreases total apparent clearance and biliary clearance of Irinotecan and significantly increases the concentration of Irinotecan and SN-38 exposure in blood and brain tissue[1][2].
MBL-II-141 (10-50 mg/kg, i.p. or i.g., single dose) exhibits the relatively high predicted LD₅₀ (i.p.: 290 mg/kg, p.o.: 1200 mg/kg), and experiments have confirmed that there is no obvious toxicity or tissue damage even at a dose of 50 mg/kg[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HEK-ABCG2 or HEK-pcDNA3.1 cells transfer model established in SCID mice[2]
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Dosage:10 mg/kg alone or with 20 mg/kg Irinotecan (CPT-11)
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Administration:Intraperitoneal injection (i.p.), three times a week for 50-87 days
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Result:Completely inhibited ABCG2-negative tumors, but only delayed the growth of ABCG2-positive tumors in single-agent treatment.
Completely inhibited the growth of 90% of ABCG2-positive tumors and significantly prolonged the survival time of the mice in combined treatment.
Slowed down the growth rate of tumors, and prolonged the survival time of mice in the established tumor model (ABCG2-positive tumors grew to a diameter of 8 mm) in combined treatment.
Chemical Information
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CAS No. 1353747-12-2
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분자량 547.40
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화학식 C28H23BrN2O5
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SMILES
O=C(C1=CC(C2=C(OCC3=CC=C(Br)C=C3)C=CC=C2O1)=O)NCCC4=CNC5=C4C=C(OC)C=C5
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MBL-II-141 Related Classifications
HY-17648 Related Classifications
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