XMU-MP-5

Chemical Structure : XMU-MP-5

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货号: PC-38244Not For Human Use, Lab Use Only.

XMU-MP-5 is a new-generation potent and selective ALK inhibitor (IC50=4.15 nM) to overcome crizotinib resistance mutations, including L1196M and G1202R.

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生物&药学活性

XMU-MP-5 is a new-generation potent and selective ALK inhibitor (IC50=4.15 nM) to overcome crizotinib resistance mutations, including L1196M and G1202R.
XMU-MP-5 significantly induced apoptosis in EML4-ALK Ba/F3 cells did not affect apoptosis in wild-type Ba/F3 cells.
XMU-MP-5 shows highest binding affinities for ALK and its mutants ALK(C1156Y) and ALK(L1196M), with K d values of 0.57, 0.4, and 0.77 nM, respectively.
XMU-MP-5 blocks ALK signaling pathways and inhibits the proliferation of cells harboring either wild-type or mutant EML4-ALK in vitro and suppresses tumor growth in xenograft mouse models in vivo.
XMU-MP-5 induces significant regression of lung tumors in two genetically engineered mouse (GEM) models.

物理化学性质&存储条件

分子量	563.677
分子式	C28H33N7O4S
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	2-(dimethylamino)-1-(6-((4-((2-(isopropylsulfonyl)phenyl)amino)-5H-pyrrolo[3,2-d]pyrimidin-2-yl)amino)-5-methoxyindolin-1-yl)ethan-1-one

参考文献

1. Yue Lu, et al. EMBO Mol Med. 2022 Jan 11;14(1):e14296.

XMU-MP-5

生物&药学活性

物理化学性质&存储条件

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XMU-MP-5

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物理化学性质&存储条件

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