1. PROTAC Protein Tyrosine Kinase/RTK Immunology/Inflammation
  2. PROTACs Molecular Glues FLT3 IKZF Family
  3. PROTAC FLT3/GSPT1/IKZF1/3 degrader-1

PROTAC FLT3/GSPT1/IKZF1/3 degrader-1 

目录号: HY-175040
产品使用指南 技术支持

PROTAC FLT3/GSPT1/IKZF1/3 degrader-1 是一种 FLT3 PROTAC 降解剂 (DC50 = 1.2 nM)。PROTAC FLT3/GSPT1/IKZF1/3 degrader-1 作为分子胶降解大脑底物 PROTAC FLT3/GSPT1/IKZF1/3 degrader-1 对耐药性急性髓系白血病 (AML) 细胞表现出抗增殖活性,在 AML 研究中具有潜在应用。(粉色:FLT3/GSPT1/IKZF1/3 配体:(HY-169374);蓝色:沙利度胺配体:(HY-14658);黑色:Kinker;沙利度胺配体 + 连接子:(HY-W1123823))

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PROTAC FLT3/GSPT1/IKZF1/3 degrader-1

PROTAC FLT3/GSPT1/IKZF1/3 degrader-1 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC FLT3/GSPT1/IKZF1/3 degrader-1 is a FLT3 PROTAC degrader (DC50 = 1.2 nM). PROTAC FLT3/GSPT1/IKZF1/3 degrader-1 functions as a molecular glue to degrade cereblon substrates GSPT1 and IKZF1/3. PROTAC FLT3/GSPT1/IKZF1/3 degrader-1 exhibits antiproliferative activity against drug-resistant acute myeloid leukemia (AML) cells and is potentially useful in AML research. (Pink: FLT3/GSPT1/IKZF1/3 ligand: (HY-169374); Blue: Thalidomide ligand: (HY-14658); Black: Kinker; Thalidomide ligand + linker: (HY-W1123823))[1].

IC50 & Target[1]

Cereblon

 

IKZF1

 

IKZF3

 

体外研究
(In Vitro)

PROTAC FLT3/GSPT1/IKZF1/3 degrader-1 (Compound A2) 对 MV-4-11 FLT3-ITD、MV-4-11 FLT3-ITD-F691L、MV-4-11 FLT3-ITD-D835Y、MOLM-13 FLT3-ITD、MOLM-13 FLT3-ITD-F691L 和 MOLM-13-D835Y 表现出抗增殖活性,IC50 分别为 1.67、4.74、3.70、3.16、5.61、7.55 nM,对 FLT3 野生型细胞的增殖没有影响 (IC50 > 1000)[1]
PROTAC FLT3/GSPT1/IKZF1/3 degrader-1 (0-100 nM,24 小时) 降低 MV-4-11 和 MOLM-13 细胞中的 FLT3、GSPT1、IKZF1、IKZF3 蛋白表达[1]

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

Western Blot Analysis[1]

Cell Line: MV-4-11 cells, MOLM-13 cells
Concentration: 0 nM, 1.5 nM, 3.1 nM, 6.2 nM, 12.5 nM,25 nM, 50 nM, 100 nM
Incubation Time: 24 h
Result: Reduced FLT3, GSPT1, IKZF1, IKZF3 protein expression, degraded FLT3 protein through the proteasome-dependent fashion.
分子量

878.03

Formula

C46H59N11O7

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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.

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产品名称:
PROTAC FLT3/GSPT1/IKZF1/3 degrader-1
目录号:
HY-175040
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