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Chemical Structure| 198474-05-4 Chemical Structure| 198474-05-4

Structure of PF-06840003
CAS No.: 198474-05-4

Chemical Structure| 198474-05-4

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PF-06840003 is a highly selective orally bioavailable IDO-1 inhibitor with IC50 of 0.41 μM.

Synonyms: EOS200271

4.5 *For Research Use Only !

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Product Details of PF-06840003

CAS No. :198474-05-4
Formula : C12H9FN2O2
M.W : 232.21
SMILES Code : O=C(C(C1=CNC2=C1C=C(F)C=C2)C3)NC3=O
Synonyms :
EOS200271
MDL No. :MFCD25121820
InChI Key :MXKLDYKORJEOPR-UHFFFAOYSA-N
Pubchem ID :23063810

Safety of PF-06840003

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human periodontal ligament cells (hPDLCs) 50 µM 5 days To inhibit IDO-1 activity and investigate its effect on CD4+ T lymphocyte proliferation and cytokine production. Results showed that IDO-1 inhibition significantly reversed the suppressive effect of hPDLCs on CD4+ T lymphocyte proliferation and reduced the production of IL-10, IL-17A, and IL-6. J Clin Periodontol. 2020 Jun;47(6):689-701.
Hepa1–6 2 μM 48 hours Inhibited IDO1 activity, reversed ZNF207-mediated CD8+ T cell exhaustion J Immunother Cancer. 2022 Mar;10(3):e004414.
Human periodontal ligament stem cells (hPDLSCs) 50 µM 48 hours Inhibition of IDO-1 enzymatic activity to evaluate its impact on the immunomodulatory function of hPDLSCs. Results showed that PF-06840003 significantly inhibited IDO-1 enzymatic activity. Cells. 2020 May 14;9(5):1222.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Hepa1–6 subcutaneous xenograft tumor model 2 μM PF-06840003 treatment reversed the tumor growth-promoting effect of ZNF207-OE J Immunother Cancer. 2022 Mar;10(3):e004414.

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT02764151 Oligodendroglioma|Astrocytoma|... More >>Malignant Glioma Less << PHASE1 TERMINATED 2018-12-26 Ronald Reagan UCLA Medical Cen... More >>ter, Los Angeles, California, 90095-6894, United States|UCLA Clinical & Translational Research Center, Los Angeles, California, 90095, United States|UCLA Oncology Center, Los Angeles, California, 90095, United States|UCLA School of Medicine, Los Angeles, California, 90095, United States|Massachusetts General Hospital, Boston, Massachusetts, 02114, United States|Brigham & Women's Hospital, Boston, Massachusetts, 02115, United States|Dana-Farber Cancer Institute, Boston, Massachusetts, 02215, United States|University of New Mexico Comprehensive Cancer Center, Albuquerque, New Mexico, 87102, United States|Columbia University Medical Center, New York, New York, 10019, United States|Columbia University Medical Center, New York, New York, 10032, United States|CUMC Research Pharmacy, New York, New York, 10032, United States|Columbia Doctors Tarrytown, Tarrytown, New York, 10591, United States|Duke Cancer Center, Durham, North Carolina, 27710, United States|Duke University Medical Center, Duke Cancer Center, Durham, North Carolina, 27710, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.31mL

0.86mL

0.43mL

21.53mL

4.31mL

2.15mL

43.06mL

8.61mL

4.31mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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