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Chemical Structure| 163239-22-3 Chemical Structure| 163239-22-3

Structure of 680C91
CAS No.: 163239-22-3

Chemical Structure| 163239-22-3

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680C91 is a selective TDO inhibitor that can regulate tryptophan metabolism, suitable for tumor immunity and Alzheimer's disease research.

4.5 *For Research Use Only! Not for Human Use. We Do Not Sell to Patients.

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Product Details of 680C91

CAS No. :163239-22-3
Formula : C15H11FN2
M.W : 238.26
SMILES Code : FC1=CC2=C(C=C1)C(/C=C/C3=CC=CN=C3)=CN2
English Name :(E)-6-Fluoro-3-(2-(pyridin-3-yl)vinyl)-1H-indole
MDL No. :MFCD20926361

Safety of 680C91

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Fibroid explants 50μM 48 hours To investigate the effect of 680C91 on mRNA expression in fibroid explants, results showed that 680C91 blocked tryptophan-induced expression of CYP1B1, TGF-β3, FN1, CDK2, E2F1, IL8, and SPARC mRNA. Fertil Steril. 2024 Apr;121(4):669-678.
HCT15 colon cancer cells 25 µM 3 days Reduction in cell number was caused by cell death or cell cycle arrest Genes Dev. 2019 Sep 1;33(17-18):1236-1251.
DLD1 colon cancer cells 25 µM 3 days Reduction in cell number was caused by cell death or cell cycle arrest Genes Dev. 2019 Sep 1;33(17-18):1236-1251.
SK-Mel-28 melanoma cells 40 μM 24 hours 680C91 significantly inhibited dexamethasone-induced migration and MMP2 activity in SK-Mel-28 cells. Pharmaceuticals (Basel). 2021 Mar 4;14(3):211.
SK-Mel-28 melanoma cells 40 μM 3 hours 680C91 partially but significantly inhibited dexamethasone-induced Akt phosphorylation. Pharmaceuticals (Basel). 2021 Mar 4;14(3):211.
SK-Mel-28 melanoma cells 40 μM 48 hours 680C91 significantly inhibited dexamethasone-induced proliferation of SK-Mel-28 cells by 41.2 ±7.1%, without affecting cell viability or FGF2-induced cell proliferation. Pharmaceuticals (Basel). 2021 Mar 4;14(3):211.
A172 cells 10 μM 24 hours 680C91 treatment resulted in decreased hpol κ expression. Chem Res Toxicol. 2016 Jan 19;29(1):101-8.
U-87-MG cells 10 μM 24 hours 680C91 treatment resulted in decreased hpol κ expression. Chem Res Toxicol. 2016 Jan 19;29(1):101-8.
T98G cells 10 μM or 100 μM 24 hours Inhibition of TDO activity led to reduced Kyn production and decreased hpol κ expression levels. Chem Res Toxicol. 2016 Jan 19;29(1):101-8.
ECFCs 40 µM 24 hours 680C91 significantly impaired ECFCs' tube formation ability Pharmaceuticals (Basel). 2024 Apr 27;17(5):558.
HUVECs 40 µM 48 hours 680C91 significantly inhibited HUVEC proliferation, with maximal effect at 40 µM inhibiting cell growth by 79.3 ± 28% Pharmaceuticals (Basel). 2024 Apr 27;17(5):558.
A375 cells 40 µM 24 hours 680C91 significantly abolished the dex-induced upregulation of stem cell markers Front Pharmacol. 2022 Jun 30;13:911019.
SK-Mel-28 cells 40 µM 24 hours 680C91 significantly abolished the dex-induced upregulation of stem cell markers Front Pharmacol. 2022 Jun 30;13:911019.
HepG2 cells 10, 20, 40, 80 µmol/L 72 hours To investigate the effect of 680C91 on TDO-mediated tryptophan degradation, results showed that 680C91 significantly inhibited tryptophan degradation and kynurenine accumulation J Clin Med. 2022 Aug 16;11(16):4794.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
SCID/Beige mice Human fibroid xenograft model Intraperitoneal injection 10 mg/kg Daily for two months To evaluate the therapeutic effects of 680C91 on fibroid xenografts, results showed a 30% reduction in fibroid weight after two months of treatment with 680C91, along with decreased levels of kynurenine and reduced mRNA and protein expression of multiple genes (CYP1B1, TGF-β3, FN1, CDK2, E2F1, IL-8, and SPARC) in the xenografts. Fertil Steril. 2024 Apr;121(4):669-678.

Protocol

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Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.20mL

0.84mL

0.42mL

20.99mL

4.20mL

2.10mL

41.97mL

8.39mL

4.20mL

 

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