中文名:T-3775440 HCl
英文名:T-3775440 HCl
纯度:≥99%
货号:T414009
Cas号:1422535-52-1
存储温度:-20°C储存
运输条件:超低温运输
产品介绍:
Information
T-3775440 HCl T-3775440 HCl is an irreversible LSD1 inhibitor that is highly selective for LSD1 relative to other monoamine oxidases (e.g., MAO-A and MAO-B), with an IC50 value of 2.1 nmol/L.
Targets
LSD1 2.1 nM
In vitro
T-3775440 treatment enforces transdifferentiation of erythroid/megakaryocytic lineages into granulomonocytic-like lineage cells. T-3775440 disrupts the interaction between LSD1 and growth factor-independent 1B (GFI1B), a transcription factor critical for the differentiation processes of erythroid and megakaryocytic lineage cells. 48-hour T-3775440 treatment induces cell-cycle arrest and apoptosis in AEL (TF-1a, HEL92.1.7) and AMKL cell lines (CMK11-5, M07e). T-3775440 treatment increases the G1 and sub-G1 phase populations in TF-1a and CMK11-5 cells.
In vivo
T-3775440 exerts tumor growth suppression in in vivo mouse xenograft models of AML. In mice, T-3775440 treatment results in a transient reduction in platelets, followed by a significant rebound. There is no obvious effect on red blood cell counts following a single administration. T-3775440 also exhibits potent antitumor effects in an additional AEL model of HEL 92.1.7 and an AMKL model of CMK11-5, possessing profound anti-AEL and anti-AMKL activity.
Cell Research(from reference)
Cell lines:TF-1a and CMK11-5 cells
Concentrations:0, 10, 50 nM (TF-1a cells); 0, 20, 100 nM (CMK11-5 cells)
Incubation Time:24 and 48 h
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关键字: 1H-?Pyrazole-?4-?carboxamide,N-?[4-?[(1R,?2S)?-?2-?[(cyclopropylmethyl)?amino]?cyclopropyl]?phenyl]?-?1-?methyl-?,hydrochloride (1:1)?,rel-
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