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Art. -Nr.: HY-17648

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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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CAS. Nr.: 1353747-12-2
Formel: C₂₈H₂₃BrN₂O₅
Molecular Weight:547.40

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

MBL-II-141 Chemical Structure

CAS. Nr.: 1353747-12-2

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vivo
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	0.031 μM Compound: 1	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	[PMID: 24611893]
HEK293	EC₅₀	0.094 μM Compound: 1	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	[PMID: 24611893]
HEK293	EC₅₀	0.13 μM Compound: 1	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	[PMID: 24304387]
HEK293	EC₅₀	0.26 μM Compound: 4g; MBL-II-141	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	[PMID: 27376492]
HEK293	IC₅₀	0.11 μM Compound: 6g	Inhibition of ABCG2-mediated mitoxantrone efflux in HEK293 cells by flow cytometry Inhibition of ABCG2-mediated mitoxantrone efflux in HEK293 cells by flow cytometry	[PMID: 22165858]
HEK293	IC₅₀	0.13 μM Compound: 1	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	[PMID: 25272055]
Sf9	IC₅₀	0.38 μM Compound: 1	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	[PMID: 24304387]

In Vivo

MBL-II-141 (10 mg/kg, i.p., three times a week for 50-87 days) with the anticancer agent Irinotecan (CPT-11) completely blocked the growth of 90% freshly implanted ABCG2-positive tumors^[2].
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 LD_₅₀ (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.

Animal Model:

HEK-ABCG2 or HEK-pcDNA3.1 cells transfer model established in SCID mice^[2]
Dosage:

10 mg/kg alone or with 20 mg/kg Irinotecan (CPT-11)
Administration:

Intraperitoneal injection (i.p.), three times a week for 50-87 days
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

CAS. Nr. 1353747-12-2
Molecular Weight 547.40
Formel C₂₈H₂₃BrN₂O₅
SMILES

O=C(C1=CC(C2=C(OCC3=CC=C(Br)C=C3)C=CC=C2O1)=O)NCCC4=CNC5=C4C=C(OC)C=C5
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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