2. PROTAC Immunology/Inflammation Apoptosis
  3. Molecular Glues IKZF Family Apoptosis
  4. MGD-22

MGD-22, a molecular glue, is an orally active IKZF1/2/3 degrader with DC50 values of 8.33 nM, 9.91 nM, and 5.74 nM, respectively. MGD-22 exhibits extremely potent anti-proliferative activity against diverse hematological cancer cells. MGD-22 induces apoptosis in cancer cells. MGD-22 demonstrates potent anti-tumor efficacy in mice bearing NCI-H929 xenografts or WSU-DLCL-2 xenografts. MGD-22 can be used for the study of hematological cancers, including multiple myeloma (MM), acute myeloid leukemia (AML), and diffuse large B-cell lymphoma (DLBCL).

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MGD-22

MGD-22 Chemical Structure

CAS No. : 2991818-12-1

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MGD-22 Related Antibodies

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Description

MGD-22, a molecular glue, is an orally active IKZF1/2/3 degrader with DC50 values of 8.33 nM, 9.91 nM, and 5.74 nM, respectively. MGD-22 exhibits extremely potent anti-proliferative activity against diverse hematological cancer cells. MGD-22 induces apoptosis in cancer cells. MGD-22 demonstrates potent anti-tumor efficacy in mice bearing NCI-H929 xenografts or WSU-DLCL-2 xenografts. MGD-22 can be used for the study of hematological cancers, including multiple myeloma (MM), acute myeloid leukemia (AML), and diffuse large B-cell lymphoma (DLBCL)[1].

IC50 & Target[1]

IKZF1

8.33 nM (DC50)

IKZF2

9.91 nM (DC50)

IKZF3

5.74 nM (DC50)

In Vitro

MGD-22 (0-100 μM, 96 h) exhibits extremely potent anti-proliferative activity against multiple myeloma (MM) cell lines including NCI-H929 (IC50 = 7.93 nM), RPMI-8226 (IC50 = 83.2 nM), OPM-2 (IC50 = 7.87 nM); acute myeloid leukemia (AML) cell lines including MV-4-11 (IC50 = 5.38±0.43 nM), U937 (IC50 = 15.1 nM), MOLM-13 (IC50 = 196 nM), KG-1 (IC50 = 78.9 nM), Skm-1 (IC50 = 218 nM), MUTZ-1 (IC50 = 148 nM); diffuse large B-cell lymphoma (DLBCL) cell lines including WSU-DLCL-2 (IC50 = 8.99 nM), Ocl-Ly3 (IC50 = 95.3 nM), SU-DHL-4 (IC50 = 452 nM), TMD8 (IC50 = 87.7 nM), U2932 (IC50 = 8.17 nM); while showing negligible activity against normal peripheral blood mononuclear cells (PBMCs) and primary B cells (IC50 > 33 μM[1].
MGD-22 (0.01-10 μM, 72 h) induces dose-dependent apoptosis in NCI-H929 and MV-4-11 cells[1].
MGD-22 (0.001-1000 nM, 24 h) selectively induces robust degradation of IKZF1/2/3 in HEK293T cells engineered with IKZF1/2/3-HiBit tags, with DC50 values of 8.33 nM (IKZF1), 9.91 nM (IKZF2), and 5.74 nM (IKZF3), and maximal degradation (Dmax) of 94.33%, 91.58%, and 92.26% respectively[1].
MGD-22 (1 μM, 24 h) promotes the formation of a ternary complex between IKZF1/2/3 and CRBN in NCI-H929 cells[1].

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

MGD-22 Related Antibodies

Apoptosis Analysis[1]

Cell Line: NCI-H929 and MV-4-11 cells
Concentration: 0.01, 0.1, 1, 10 μM
Incubation Time: 72 h
Result: Induced dose-dependent apoptosis in NCI-H929 and MV-4-11 cells.
In Vivo

MGD-22 (3-10 mg/kg, p.o., once daily, 14 days) demonstrates potent anti-tumor efficacy in NOD/SCID mice bearing NCI-H929 xenografts[1].
MGD-22 (5 mg/kg, p.o., once daily, 36 days) combined with Ibrutinib (HY-10997) or Venetoclax (HY-15531) for 36 days exhibits synergistic anti-tumor efficacy in NOD/SCID mice bearing WSU-DLCL-2 xenografts[1].

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

Animal Model: NCI-H929 cells (7.5 × 106) were subcutaneously inoculated into both sides of the dorsal back of 6-week-old NOD/SCID mice to establish the multiple myeloma (MM) xenograft model[1]
Dosage: 3, 10 mg/kg
Administration: p.o., once daily, 14 days
Result: Exhibited superior anti-tumor efficacy.
Caused only minor body weight reduction throughout the treatment period.
Reduced Ki67-positive proliferative cells and increases cleaved-caspase-3-positive apoptotic cells.
Degraded IKZF1/2/3 proteins in NCI-H929 xenograft tumor tissues.
Animal Model: WSU-DLCL-2 cells (1 × 107) were subcutaneously implanted into both sides of the dorsal back of 6-week-old NOD/SCID mice to construct the diffuse large B-cell lymphoma (DLBCL) xenograft model[1]
Dosage: 5 mg/kg combined with Ibrutinib (HY-10997) (10 mg/kg, p.o., once daily) or Venetoclax (HY-15531) (30 mg/kg, p.o., once daily)
Administration: p.o., once daily, 36 days
Result: Demonstrated anti-tumor efficacy in NOD/SCID mice bearing WSU-DLCL-2 xenografts.
Improved the survival rate of NOD/SCID mice.
Maintained stable body weight.
Molecular Weight

577.68

Formula

C33H35N7O3
CAS No.
SMILES

O=C(N1)C(N2N(CC3=C(C=CC=C3C2=O)NCC4=CC=C(CN5CCN(CC5)C6=CC=C(C=C6)C#N)C=C4)C)CCC1=O
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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MGD-22 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:

MGD-222991818-12-1MGD22MGD 22Molecular GluesIKZF FamilyApoptosisIkaros zinc finger protein familymultiple myelomaacute myeloid leukemiadiffuse large B-cell lymphomaIKZF1/2/3NCI-H92WSU-DLCL-2Inhibitorinhibitorinhibit

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