TDO-IN-1

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TDO-IN-1

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2490672-92-7

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

TDO-IN-1 是色氨酸 2,3-双加氧酶 (TDO) 的选择性抑制剂 (IC₅₀=0.62 μM)，具有口服活性，且对TDO的选择性高于吲哚胺-2,3-双加氧酶 (IDO,IC₅₀>100 μM)。TDO-IN-1 能够逆转肿瘤组织的局部免疫耐受来抑制体内肿瘤生长。

生物活性

TDO-IN-1 is an orally active and selective inhibitor oftryptophan 2,3-dioxygenase(TDO), shows excellent selectivity overindoleamine-2,3-dioxygenase(IDO), with anIC₅₀value of 0.62 μM (IDO). TDO-IN-1 reverse the local immune tolerance of tumor tissue to inhibit tumor growth in vivo^[1].

IC₅₀& Target

IC50: 0.62 μM (tryptophan 2,3-dioxygenase, TDO)^[1]

体外研究
(In Vitro)

TDO-IN-1 (HT-28) (0-100 μM; 24 h) shows significant tumoricidal effect on different tumor lines, with IC₅₀s of 0.54 μM (HepG2), 5.08 μM (Hepa1-6), 1.34 μM (H22), 37.39 μM (B16), 3.43 μM (MOLM-13), and 7.25 μM (Jurkat), respectively^[1].
TDO-IN-1 (0-100 μM; 24 h) exhibits few cytotoxic activity against normal cells (HEK 293 cells) below 10 μM^[1].

体内研究
(In Vivo)

TDO-IN-1 (HT-28) (25 mg/kg; p.o.; once daily; 9 d) improve the effect of tumor immunotherapy of CT26 tumor expressing TDO, substantially inhibits the proliferation of CT26 tumors in mice^[1].

Animal Model:	CT-26 allograft BALB/c mice (6-8 weeks old, female)^[1]
Dosage:	12.5, 25, and 50 mg/kg
Administration:	Oral gavage; once daily; 9 days
Result:	Resulted significant reduction in tumor weight and volume in mice, with the tumor volume inhibiton rate of 76.93%. Reduced the expression of Foxp3 and enhance the expression of CD8 and TNF-α in tumor tissue to increase the immune response of tumor-bearing mice.

分子量

350.30

Formula

C₁₆H₁₃F₃N₄O₂

CAS 号

2490672-92-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.