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

MGD-22，一种分子胶，是一种口服活性的 IKZF1/2/3 降解剂，其 DC50 值分别为 8.33 nM、9.91 nM 和 5.74 nM。MGD-22 对多种血液癌症细胞表现出极强的抗增殖活性。MGD-22 诱导癌症细胞凋亡 (apoptosis)。MGD-22 在NCI-H929 异种移植瘤或 WSU-DLCL-2 异种移植瘤的小鼠中展示出强大的抗肿瘤效能。MGD-22 可用于研究血液癌症，包括多发性骨髓瘤 (MM)、急性髓系白血病 (AML) 和弥漫大 B 细胞淋巴瘤 (DLBCL)。

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MGD-22

MGD-22 Chemical Structure

CAS No. : 2991818-12-1

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MGD-22 相关抗体

Top Publications Citing Use of Products

查看 IKZF Family 亚型特异性产品:

查看所有亚型
IKZF1 IKZF2 IKZF3 IKZF4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(In Vitro)

MGD-22 (0-100 μM, 96 h) 对多发性骨髓瘤 (MM) 细胞系表现出极强的抗增殖活性，包括 NCI-H929 (IC50 = 7.93 nM)、RPMI-8226 (IC50 = 83.2 nM)、OPM-2 (IC50 = 7.87 nM)；急性髓系白血病 (AML) 细胞系，包括 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)；弥漫大 B 细胞淋巴瘤 (DLBCL) 细胞系，包括 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)；而对正常外周血单核细胞 (PBMCs) 和原代 B 细胞的活性可忽略不计 (IC50 > 33 μM)[1]。
MGD-22 (0.01-10 μM, 72 h) 在 NCI-H929 和 MV-4-11 细胞中诱导剂量依赖性的细胞凋亡[1]。
MGD-22 (0.001-1000 nM, 24 h) 在转染 IKZF1/2/3-HiBit 标签的 HEK293T 细胞中选择性地诱导 IKZF1/2/3 的强效降解，其 DC50 值分别为 8.33 nM (IKZF1)、9.91 nM (IKZF2) 和 5.74 nM (IKZF3)，最大降解率 (Dmax) 分别为 94.33%、91.58% 和 92.26%[1]。
MGD-22 (1 μM, 24 h) 在 NCI-H929 细胞中促进 IKZF1/2/3 与 CRBN 形成三元复合物[1]。

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

MGD-22 相关抗体:

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.
体内研究
(In Vivo)

MGD-22 (3-10 mg/kg，口服给药，每日一次，14 天) 在 NCI-H929 异种移植瘤的 NOD/SCID 小鼠中展示出强大的抗肿瘤效能[1]。
MGD-22 (5 mg/kg，口服给药，每日一次，36 天) 与 Ibrutinib (HY-10997) 或 Venetoclax (HY-15531) 联合使用 36 天，在 WSU-DLCL-2 异种移植瘤的 NOD/SCID 小鼠中表现出协同抗肿瘤效能[1]。

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.
分子量

577.68

Formula

C33H35N7O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MGD-22 相关分类

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  • Do most proteins show cross-species activity?

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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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