PLM-101 hydrochloride | FLT3/RET inhibitor | Probechem Biochemicals

Chemical Structure : PLM-101 hydrochloride

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PLM-101 hydrochloride (FLT3-IN-15)

货号: PC-25422Not For Human Use, Lab Use Only.

PLM-101 hydrochloride is a synthetic derivative of indirubin and potent, dual FLT3/RET inhibitor with IC50 of 0.565 nM and 0.849 nM for FLT3-ITD and RET kinase respectively.

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生物&药学活性

PLM-101 hydrochloride is a synthetic derivative of indirubin and potent, dual FLT3/RET inhibitor with IC50 of 0.565 nM and 0.849 nM for FLT3-ITD and RET kinase respectively.
PLM-101 inhibits the proliferation of Ba/F3 cells expressing FLT3-ITD-mutant kinases at the nanomolar (nM) concentration levels.
PLM-101 exhibits robust inhibitory activity against FLT3 D835Y and F691L secondary mutants.
PLM-101 exhibits anti-proliferation activities of PLM-101 against FLT3-ITD-positive AML cell lines (MV4–11, MOLM-14, and MOLM-13, IC50=3.26, 10.47 and 9.64 nM).
PLM-101 (3-100 nM) induces apoptosis and cell cycle arrest in FLT3-ITD-positive AML cell lines.
PLM-101 exerts anti-leukemic activity by inhibiting the signal transduction of the FLT3-ITD mutant protein, via inhibition of PI3K and Ras/ERK signaling pathways.
PLM-101 activates the autophagy degradation pathway, leading to degradation of both RET and FLT3, and additional inhibition of FLT3 sub-pathway activation.
PLM-101 (3-20 mg/kg, oral) demonstrates anti-leukemic effect in vivo orthotopic xenograft model.

物理化学性质&存储条件

分子量	443.91
分子式	C22H23ClFN5O2
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	(2Z,3E)-5'-fluoro-3-((2-(piperazin-1-yl)ethoxy)imino)-[2,3'-biindolinylidene]-2'-one hydrochloride

参考文献

1. Choi YJ, et al. Biomed Pharmacother. 2023 Sep;165:115066.

PLM-101 hydrochloride (FLT3-IN-15)

生物&药学活性

物理化学性质&存储条件

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PLM-101 hydrochloride (FLT3-IN-15)

生物&药学活性

物理化学性质&存储条件

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