2. PROTAC Protein Tyrosine Kinase/RTK Apoptosis
  3. PROTACs FLT3 Apoptosis
  4. PROTAC FLT-3 degrader 4

PROTAC FLT-3 degrader 4 是一种具有口服活性的基于 CRBN 的 FLT3-PROTAC 降解剂，可通过泛素-蛋白酶体系统有效诱导 FLT3-ITD 降解。PROTAC FLT-3 degrader 4 对 FLT3-ITD 突变型急性髓系白血病 (AML) 细胞具有高度选择性。（蓝色：CRBN 配体，黑色：连接子；粉色：FLT3 抑制剂）。

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PROTAC FLT-3 degrader 4 Chemical Structure

PROTAC FLT-3 degrader 4 Chemical Structure

CAS No. : 2956722-48-6

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PROTAC FLT-3 degrader 4 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC FLT-3 degrader 4 is an orally active CRBN-based FLT3-PROTAC degrader that potently induces FLT3-ITD degradation through the ubiquitin-proteasome system. PROTAC FLT-3 degrader 4 shows highly selective to FLT3-ITD mutant acute myeloid leukemia (AML) cells. (Blue: CRBN ligand, Black: linker; Pink: FLT3 inhibitor)[1].

IC50 & Target[1]

Cereblon

 

体外研究
(In Vitro)

PROTAC FLT-3 degrader 4 (compound A20) 对 MV4-11 和 MOLM-13 细胞具有抗增殖活性（IC50 分别为 39.9 nM 和 169.9 nM）[1].
PROTAC FLT-3 degrader 4（0.25-100 nM；24 小时）显示 MV4-11 和 MOLM-13 细胞中 FLT3-ITD 蛋白水平大幅降低[1]。
PROTAC FLT-3 degrader 4（20 nM；12 h）可抑制 MV4-11 和 MOLM-13 细胞中的 FLT3-ITD 磷酸化及其下游信号介质，包括 STAT5、S6K 和 ERK[1]。
PROTAC FLT-3 degrader 4 (20 nM; 12 h) 剂量依赖性地诱导 G1 期周期停滞。PROTAC FLT-3 degrader 4 还可剂量依赖性地诱导 MV4-11 和 MOLM-13 细胞凋亡[1]。

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

PROTAC FLT-3 degrader 4 相关抗体:

Western Blot Analysis[1]

Cell Line: MV4-11 and MOLM-13 cells
Concentration: 0.25 nM, 0.5 nM, 1 nM, 5 nM, 10 nM, 20 nM, 50 nM, 80 nM, 100 nM
Incubation Time: 24 h
Result: Showed potent FLT3-ITD degradation activity with DC50 values of 7.4 nM and 20.1 nM for MV4-11 and MOLM-13 cells, respectively.

Apoptosis Analysis[1]

Cell Line: MV4-11 and MOLM-13 cells
Concentration: 1 nM, 5 nM, 50 nM
Incubation Time: 24 h
Result: Blocked AML cell cycle in G1 phase and induced apoptosis.
体内研究
(In Vivo)

PROTAC FLT-3 degrader 4（compound A20；1.235-10 mg/kg；口服；每天；持续 2 周）在 1.25 mg/kg 剂量下显着抑制肿瘤生长。5 mg/kg 时观察到肿瘤消退（TGI = 97.5%），10 mg/kg 时观察到肿瘤完全消退[1]。
PROTAC FLT-3 degrader 4 在Sprague-Dawley大鼠体内的药代动力学参数[1]。
1.19

parameter iv (1 mg/kg) po (10 mg/kg)
AUC0-t (h·ng/mL) 2768.1 14705.3
Cmax (ng/mL) - 1117.5
Tmax (h) - 6.2
T1/2 (h) 6.5 3.8
Vss (L/kg) 3.5 5.7
CL (mL/min/kg) 5.5 11.2
F (%) - 53

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

Animal Model: Four week old male nu/nu mice injected with MV4-11 cells[1]
Dosage: 1.25 mg/kg, 2.5 mg/kg, 5 mg/kg, 10 mg/kg
Administration: po; daily; for 2 weeks
Result: Significantly inhibited tumor growth at 1.25 mg/kg.
分子量

736.79

Formula

C39H41FN8O6
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

PROTAC FLT-3 degrader 4 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

PROTAC FLT-3 degrader 42956722-48-6PROTACsFLT3ApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3antiproliferative activitiesPROTAC FLT-3 degradercycle arrestSTAT5S6KERKInhibitorinhibitorinhibit

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