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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
Size Price / USD Stock Quantity
2MG 178 Get Quote
5MG 275 Get Quote
10MG 432 Get Quote
25MG 821 Get Quote
50MG 1334 Get Quote
100MG 1773 Get Quote
500MG Get Quote Get Quote
1G Get Quote Get Quote

Biological Information

  • Product Name
    TDO-IN-1
  • Note
    Research use only, not for human use.
  • Brief Description
    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.
  • Description
    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.
  • 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.TDO-IN-1 (0-100 μM; 24 h) exhibits few cytotoxic activity against normal cells (HEK 293 cells) below 10 μM.
  • 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.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.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Others
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2490672-92-7
  • Formula Weight
    350.3
  • Molecular Formula
    C16H13F3N4O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (285.47 mM; Ultrasonic )
  • SMILES
    N(CC1=C(N(=O)=O)C=C(C)C=C1)C2=C3C(=CC(C(F)(F)F)=C2)NN=C3
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • 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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