1. PROTAC Apoptosis
  2. Ligands for Target Protein for PROTAC MDM-2/p53
  3. MI-2103

MI-2103 is a MDM2 inhibitor with an IC50 of 48.1 nM. MI-2103 inhibits the growth of leukemia and breast cancer cells; it exerts no growth-inhibitory effect on cancer cells with p53 mutation or deletion. MI-2103 serves as a target protein ligand for the synthesis of MG-277 (HY-130122). MI-2103 is applicable to the research of leukemia and breast cancer.

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

MI-2103

MI-2103 Chemical Structure

CAS No. : 1410738-11-2

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Description

MI-2103 is a MDM2 inhibitor with an IC50 of 48.1 nM. MI-2103 inhibits the growth of leukemia and breast cancer cells; it exerts no growth-inhibitory effect on cancer cells with p53 mutation or deletion. MI-2103 serves as a target protein ligand for the synthesis of MG-277 (HY-130122). MI-2103 is applicable to the research of leukemia and breast cancer[1].

Cellular Effect
Cell Line Type Value Description References
MDA-MB-231 IC50
>10 nM
Compound: MI-2103
Antiproliferative activity against human MDA-MB-231 cells harboring mutant p53 assessed as cell growth inhibition without interaction with cereblon after 4 days by WST-8 assay
Antiproliferative activity against human MDA-MB-231 cells harboring mutant p53 assessed as cell growth inhibition without interaction with cereblon after 4 days by WST-8 assay
[PMID: 31560543]
MDA-MB-231 IC50
>10 μM
Compound: MI-2103
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 2 days followed by compound treatment by WST-8 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 2 days followed by compound treatment by WST-8 assay
[PMID: 31560543]
MDA-MB-231 IC50
>3 μM
Compound: MI-2103
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 3 days followed by compound treatment by WST-8 assay
Antiproliferative activity against human MDA-MB-231 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 3 days followed by compound treatment by WST-8 assay
[PMID: 31560543]
MDA-MB-468 IC50
>10 nM
Compound: MI-2103
Antiproliferative activity against human MDA-MB-468 cells harboring mutant p53 assessed as cell growth inhibition without interaction with cereblon after 4 days by WST-8 assay
Antiproliferative activity against human MDA-MB-468 cells harboring mutant p53 assessed as cell growth inhibition without interaction with cereblon after 4 days by WST-8 assay
[PMID: 31560543]
MDA-MB-468 IC50
>10 μM
Compound: MI-2103
Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 2 days followed by compound treatment by WST-8 assay
Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 2 days followed by compound treatment by WST-8 assay
[PMID: 31560543]
MDA-MB-468 IC50
>3 μM
Compound: MI-2103
Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 3 days followed by compound treatment by WST-8 assay
Antiproliferative activity against human MDA-MB-468 cells assessed as cell growth inhibition after 4 days in presence of control siRNA for 3 days followed by compound treatment by WST-8 assay
[PMID: 31560543]
MOLM-13 IC50
1238 nM
Compound: MI-2103
Antiproliferative activity against human MOLM13 cells expressing wild type p53 assessed as cell growth inhibition after 4 days by WST-8 assay
Antiproliferative activity against human MOLM13 cells expressing wild type p53 assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 31560543]
MV4-11 IC50
898 nM
Compound: MI-2103
Antiproliferative activity against human MV4-11 cells expressing wild type p53 assessed as cell growth inhibition after 4 days by WST-8 assay
Antiproliferative activity against human MV4-11 cells expressing wild type p53 assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 31560543]
RS4-11 IC50
1111 nM
Compound: MI-2103
Antiproliferative activity against human RS4:11 cells expressing wild type p53 assessed as cell growth inhibition without interaction with cereblon after 4 days by WST-8 assay
Antiproliferative activity against human RS4:11 cells expressing wild type p53 assessed as cell growth inhibition without interaction with cereblon after 4 days by WST-8 assay
[PMID: 31560543]
RS4-11 IC50
1493 nM
Compound: MI-2103
Antiproliferative activity against human RS4:11 cells expressing wild type p53 assessed as MDM2-independent cell growth inhibition after 4 days by WST-8 assay
Antiproliferative activity against human RS4:11 cells expressing wild type p53 assessed as MDM2-independent cell growth inhibition after 4 days by WST-8 assay
[PMID: 31560543]
RS4-11 IC50
669 nM
Compound: MI-2103
Antiproliferative activity against human RS4:11 cells expressing wild type p53 assessed as cell growth inhibition after 4 days by WST-8 assay
Antiproliferative activity against human RS4:11 cells expressing wild type p53 assessed as cell growth inhibition after 4 days by WST-8 assay
[PMID: 31560543]
In Vitro

MI-2103 (4 days) inhibits growth of p53 wild-type RS4;11, MOLM-13, and MV4;11 leukemia cells with IC50 values of 669 nM, 1238 nM, and 898 nM, respectively, and is ineffective in p53 mutated/deleted RS4;11/IRMI-2, HL-60, MDA-MB-231, and MDA-MB-468 cells[1].
MI-2103 (1-2 h) upregulates MDM2 and p53 protein levels in p53 wild-type RS4;11 cells after 1 h and 2 h of treatment and does not affect GSPT1 protein levels[1].
MI-2103 (excess amount) does not interfere with MG-277-induced GSPT1 degradation in MDA-MB-231 cells, indicating its binding to MDM2 is not required for GSPT1 degradation by MG-277[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

476.37

Formula

C24H24Cl2FN3O2

CAS No.
SMILES

O=C([C@H](N1)[C@H](C2=CC=CC(Cl)=C2F)[C@]3(C(NC4=C3C=CC(Cl)=C4)=O)C51CCCCC5)NC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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  • 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.

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Product Name:
MI-2103
Cat. No.:
HY-131217
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