PROTAC FLT3/CDK9 degrader-1

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

PROTAC FLT3/CDK9 degrader-1 是一种有效的FLT3和CDK9双 PROTAC 降解剂。PROTAC FLT3/CDK9 degrader-1 诱导细胞凋亡 (Apoptosis) 并有效降解靶蛋白 FLT3 和 CDK9。PROTAC FLT3/CDK9 degrader-1具有研究 FLT3-ITD 突变型 AML 的潜力。

生物活性

PROTACFLT3/CDK9 degrader-1 is a potentFLT3andCDK9dualPROTACdegrader.PROTACFLT3/CDK9 degrader-1 inducesApoptosisand effective degradation of target proteinsFLT3andCDK9.PROTACFLT3/CDK9 degrader-1 has the potential for the research of FLT3-ITD mutated AML^[1].

体外研究
(In Vitro)

PROTAC FLT3/CDK9 degrader-1 (compound PROTAC 13) (0.004, 0.02, 0.1, 0.5, 2.5 μM; 16 h) 降低 p-FLT3 Y589/591、p-STAT5 Y694、p-ERK1/2 T202/Y204 的表达,并以剂量依赖性方式诱导 MV4-11 细胞凋亡^[1]。
在 MV4-11 细胞中用MG132(HY-13259) (0.2 μM) 预处理 90 分钟后，PROTAC FLT3/CDK9 degrader-1 (0, 0.1, 0.5 μM; 16 h) 的蛋白降解能力减弱^[1]。

Cell Proliferation Assay^[1]

Cell Line:	MV4-11, MV4-11 CRBN-def., MOLM-13, RS4-11, HL60, U937, THP-1, Kasumi-1, CEM, K562 cells
Concentration:	0-10 μM
Incubation Time:	72 h
Result:	Showed antiproliferative activity with IC₅₀s of 0.047, 0.119, 0.042, 1.014, 6.122, 9.507, 9.993, >10, >10, >10 μM for MV4-11, MV4-11 CRBN-def., MOLM-13, RS4-11, HL60, U937, THP-1, Kasumi-1, CEM, K562 cells, respectively.

Western Blot Analysis^[1]

Cell Line:	MV4-11 cells
Concentration:	0.004, 0.02, 0.1, 0.5, 2.5 μM
Incubation Time:	16 h
Result:	Decreased the expression of p-FLT3 Y589/591, p-STAT5 Y694, p-ERK1/2 T202/Y204 in a dose-depent manner.

Apoptosis Analysis^[1]

Cell Line:	MV4-11, CRBN-deficient MV4-11 cells
Concentration:	0.004, 0.02, 0.1, 0.5, 2.5 μM
Incubation Time:	16 h
Result:	Induced apoptosis with the activities of caspases 3 and 7 increased in a concentration-dependent manner in MV4-11 cells.

分子量

919.08

Formula

C₄₈H₆₂N₁₂O₇

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.