PROTAC FLT-3 degrader 4_product_DataBase

Bioactivity	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].
Invitro	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. 0 --> PROTAC FLT-3 degrader 4 相关抗体: Western Blot Analysis[1] Cell Line:
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
CAS	2956722-48-6
Formula	C39H41FN8O6
Molar Mass	736.79
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Junwei Wang, et al. Discovery of a Novel Orally Bioavailable FLT3-PROTAC Degrader for Efficient Treatment of Acute Myeloid Leukemia and Overcoming Resistance of FLT3 Inhibitors. J Med Chem. 2024 May 9;67(9):7197-7223.

PeptideDB

PROTAC FLT-3 degrader 4

CAS: 2956722-48-6 F: C39H41FN8O6 W: 736.79