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CAS No.: 1316695-35-8

LM10 Catalog No. CSN13821

Synonyms: LM10

LM10 is a selective tryptophan 2,3-dioxygenase (TDO) inhibitor with IC50 values of 0.62 and 2 μM for human and mouse TDO, respectively.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Tryptophan-2,3-dioxygenase (TDO) and indoleamine 2,3-dioxygenase (IDO) are the enzymes controlling the rate-limiting step of the catabolism of tryptophan to immunosuppressive and neuroactive kynurenines, a key metabolic pathway regulating immune responses and neurotoxicity . LM10 can selective inhibit human and mouse TDO with IC50 values of 0.62 and 2 μM, respectively, which display good TDO inhibition with Ki of 5.5 μM. LM10 with a concentration of 1 mg/mL dissolved was given ad libitum to DBA/2 mice in the drinking water of 4 mL/mice/day, plasma concentration was detected from 60-136μM, suggesting a higher oral bioavailability. LM10 was also proved to be highly selective for TDO as, at 10 μM, none of the investigated systems are significantly inhibited. Furthermore, LM10 does not display any inhibitory potency on IDO at all. In an In vivo efficacy study, treatment of immunized mice with LM10 at 160 (mg/kg)/day prevented the growth of TDO-expressing P815 tumor cells . LM10 also showed no obvious signs of toxicity after more than 100 days of systemic administration of LM10 and no significant difference between treated and untreated mice for their plasma level of ALAP, γ-GT, ALAT and ASAT, all of which remained within the normal range. To determine whether the antitumor effects of LM10 resulted only from promoting tumor rejection or whether LM10 also had a direct effect on tumor cells, immunodeficient RAG2 knockout mice with TDO-expressing P815 cells was treated with LM10, while tumor growth was not affected by LM10 treatment indicating that the effect of LM10 was dependent on the immune system in this model.
动物研究
剂量
Mice: 160 mg/kg^[1] (p.o.)

给药途径
p.o.
临床研究

动物研究
剂量	Mice: 160 mg/kg^[1] (p.o.)
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02315183	-	-	Completed	-	United Kingdom ... more >> Department of Cardiovascular Sciences. Leicester, Leicestershire, United Kingdom, LE3 9QP Collapse <<

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.3628 mL
- 21.8138 mL
- 43.6275 mL
- 5 mM
- 0.8726 mL
- 4.3628 mL
- 8.7255 mL
- 10 mM
- 0.4363 mL
- 2.1814 mL
- 4.3628 mL

技术信息

CAS号

1316695-35-8

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C11H8FN5

运输

蓝冰

分子量

229.21

别名

LM10

溶解度

DMSO	450.0 mg/mL (1963.2 mM) warming
Water	insoluble

动物实验配方

IP	2% DMSO+2% Tween80+40% PEG300+water	9 mg/mL	clear
PO	0.5% CMC-Na	42 mg/mL	suspension

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