2. Membrane Transporter/Ion Channel
  3. BCRP
  4. 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.

For research use only. We do not sell to patients.

MBL-II-141

MBL-II-141 Chemical Structure

CAS No. : 1353747-12-2

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MBL-II-141 Related Antibodies

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Description

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].

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 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.

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.
Molecular Weight

547.40

Formula

C28H23BrN2O5
CAS No.
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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Please store the product under the recommended conditions in the Certificate of Analysis.
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MBL-II-141 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MBL-II-1411353747-12-2BCRPBreast cancer resistance proteinABCG2MDR phenotypeInhibitorsChemosensitizationInhibitorinhibitorinhibit

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