T-3775440 HCl

製品コードS8438 バッチS843801

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C18H23ClN4O
分子量 346.85 CAS No. 1422535-52-1
Solubility (25°C)* 体外 DMSO 69 mg/mL (198.93 mM)
Water 22 mg/mL (63.42 mM)
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 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.
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[1].
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[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 TF-1a and CMK11-5 cells
濃度 0, 10, 50 nM (TF-1a cells); 0, 20, 100 nM (CMK11-5 cells)
反応時間 24 and 48 h
実験の流れ

TF-1a and CMK11-5 cells are treated with the indicated concentration of T-3775440 for 24 or 48 hours. Treated cells are subsequently harvested and lysed to prepare total lysates. Immunoblotting analyses are performed to determine the expression levels of p27, cleaved PARP, and β-actin in the cell lysates.
動物実験 動物モデル Female C.B17/Icr-scid/scid Jcl mice subcutaneously (s.c.) inoculated in the flank with AML cells
投薬量 15-20 mg/kg
投与方法 oral

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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