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首页-抗体药物偶连体和PROTACs-PROTAC-MA191
MA191

Chemical Structure : MA191

CAS No.: 3127228-40-1

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MA191 (MA-191)

货号: PC-28746Not For Human Use, Lab Use Only.

MA191 is a potent, von Hippel-Lindau (VHL) E3 ubiquitin ligase-based PROTAC degrader of FLT3 with DC50 of 10 nM, also degrades MAPK14 (p38α).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

MA191 is a potent, von Hippel-Lindau (VHL) E3 ubiquitin ligase-based PROTAC degrader of FLT3 with DC50 of 10 nM, also degrades MAPK14 (p38α).
MA191 demonstrate superior degradation of FLT3-ITD in MV4-11 AML cells at 50 nM, achieving >95% reduction in FLT3-ITD levels.
MA191 induces apoptosis in cultured and primary AML patient cells harboring FLT3-ITD (IC50=9.6-11 nM, EC50=0.001-0.883 µM).
MA191 requires VHL, neddylation, proteasome activity, and the pro-apoptotic BH3-only protein BIM.
MA191 reduces FLT3-ITD prior to apoptosis, uncovering apoptosis-independent roles of BIM for protein stability.
MA191 also depletes MAPK14 in FLT3 negative K562 chronic myeloid leukemia cells, in RS4-11 acute T cell lymphatic leukemia cells with wild-type FLT3, and in MV4-11 and MOLM-13 cells.

物理化学性质&存储条件

分子量 1088.34
分子式 C57H73N11O9S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

4-(4-(3-(5-(tert-Butyl)isoxazol-3-yl)ureido)phenoxy)-N-(2-(4-(trans-4-(((S)-1-((2S,4R)-4-hydroxy-2-(((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)carbamoyl)cyclohexanecarbonyl)piperazin-1-yl)ethyl)picolinamide

参考文献

1. Melisa Halilovic, et al. Leukemia. 2026 Oct 28. doi: 10.1038/s41375-026-03168-x.

2. Abdelsalam M, et al. Pharmaceuticals (Basel). 2026 May 12;19(5):756.

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