TDO-IN-1

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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 IC50 value of 0.62 μM (IDO). TDO-IN-1 reverse the local immune tolerance of tumor tissue to inhibit tumor growth in vivo.

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.TDO-IN-1 (0-100 μM; 24 h) exhibits few cytotoxic activity against normal cells (HEK 293 cells) below 10 μM.

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.Animal Model:CT-26 allograft BALB/c mice (6-8 weeks old, female)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.

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2490672-92-7

350.3

C16H13F3N4O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 100 mg/mL (285.47 mM; 超声助溶 )

N(CC1=C(N(=O)=O)C=C(C)C=C1)C2=C3C(=CC(C(F)(F)F)=C2)NN=C3

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(-20℃)

With Ice Pack

≥ 2 years