
TDO-IN-1
CAS No. 2490672-92-7
TDO-IN-1( —— )
Catalog No. M35528 CAS No. 2490672-92-7
TDO-IN-1 is an orally active, potent, and selective inhibitor of tryptophan 2,3-dioxygenase (TDO), inhibiting indoleamine-2,3-dioxygenase, with antitumor activity that reverses local immune tolerance in tumor tissues.
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
2MG | 178 | Get Quote |
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5MG | 275 | Get Quote |
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10MG | 432 | Get Quote |
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25MG | 821 | Get Quote |
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50MG | 1334 | Get Quote |
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100MG | 1773 | Get Quote |
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500MG | Get Quote | Get Quote |
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1G | Get Quote | Get Quote |
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Biological Information
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Product NameTDO-IN-1
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NoteResearch use only, not for human use.
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Brief DescriptionTDO-IN-1 is an orally active, potent, and selective inhibitor of tryptophan 2,3-dioxygenase (TDO), inhibiting indoleamine-2,3-dioxygenase, with antitumor activity that reverses local immune tolerance in tumor tissues.
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DescriptionTDO-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.
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In VitroTDO-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.
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In VivoTDO-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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Synonyms——
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PathwayOthers
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TargetOther Targets
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RecptorOthers
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Research Area——
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Indication——
Chemical Information
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CAS Number2490672-92-7
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Formula Weight350.3
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Molecular FormulaC16H13F3N4O2
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 100 mg/mL (285.47 mM; Ultrasonic )
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SMILESN(CC1=C(N(=O)=O)C=C(C)C=C1)C2=C3C(=CC(C(F)(F)F)=C2)NN=C3
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Huo C, et al. 4,6-Disubstituted-1H-Indazole-4-Amine derivatives with immune-chemotherapy effect and in vivo antitumor activity. Eur J Med Chem. 2022 Nov 5;241:114625.? ?
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