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。

TDO-IN-1 is an orally active and selective inhibitor of tryptophan 2,3-dioxygenase ( TDO ), shows excellent selectivity over indoleamine-2,3-dioxygenase ( IDO ), with an IC 50 value of 0.62 μM ( IDO ). TDO-IN-1 reverse the local immune tolerance of tumor tissue to inhibit tumor growth in vivo [1].

TDO-IN-1 (HT-28) (0-100 μM; 24 h) shows significant tumoricidal effect on different tumor lines, with IC 50 s 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].

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.

2490672-92-7

C16H13F3N4O2

350.3

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years