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Chemical Structure| 745833-23-2 Chemical Structure| 745833-23-2

Structure of VX-702
CAS No.: 745833-23-2

Chemical Structure| 745833-23-2

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VX-702 is a selective inhibitor of p38α MAPK, with selectivity 14 times that of p38β MAPK.

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Product Details of VX-702

CAS No. :745833-23-2
Formula : C19H12F4N4O2
M.W : 404.32
SMILES Code : O=C(C1=CC=C(N(C(N)=O)C2=C(F)C=CC=C2F)N=C1C3=CC=C(F)C=C3F)N
MDL No. :MFCD11616590
InChI Key :FYSRKRZDBHOFAY-UHFFFAOYSA-N
Pubchem ID :10341154

Safety of VX-702

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of VX-702

MAPK
TLR

Isoform Comparison

Biological Activity

Target
  • p38α

    p38α, IC50:4 nM-20 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
lung myofibroblasts 50 μM 96 hours VX-702 treatment significantly reduced αSMA and Col1A1 protein expression, promoted disassembly of αSMA stress fibers, and restored apoptosis sensitivity. PMC11093610
MCF7-TamR 0.5 μM 7 days VX-702 showed significant therapeutic effects on MCF7-TamR cells under estrogen-deprived conditions PMC8653766
T47D-TamR 0.5 μM 7 days VX-702 showed significant therapeutic effects on T47D-TamR cells under estrogen-deprived conditions PMC8653766
Calu-3 cells 5 μM 48 hours To evaluate the inhibitory effect of VX-702 on the inflaμMatory response after SARS-CoV-2 infection, results showed that VX-702 significantly reduced the expression of IL6 and CXCL8. PMC9677559
HCoEpiC cells 0.5 mg/ml VX-702 significantly suppressed the apoptosis rate induced by BBR in HCoEpiC cells and inhibited the expression of p38 MAPK and phosphorylated p38 MAPK PMC7176772
TCMK-1 cells 5 μM 24 hours VX-702 inhibited apoptosis and enhanced the viability of TCMK-1 cells. PMC11198005

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
mice bleomycin-induced pulmonary fibrosis model oral gavage 55 mg/kg daily for one week VX-702 significantly mitigated bleomycin-induced pulmonary fibrosis and restored spontaneous fibrosis resolution in MKP1-deficient mice. PMC11093610
Mice T47D-TamR tumor model Oral 3 mg/kg/day Once daily VX-702 in combination with mTOR inhibitor showed significant therapeutic effects in the T47D-TamR tumor model PMC8653766
Mice S-AKI model Oral 100 mg/kg 28 consecutive days VX-702 decreased the mortality of mice with S-AKI and reduced pathological changes and the number of apoptotic cells in kidney tissues. PMC11198005

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00205478 Rheumatoid Arthritis PHASE2 COMPLETED 2025-02-06 Medical University - Sofia, So... More >>fia, Bulgaria|Military Medical Academy - Sofia, Sofia, Bulgaria|Transport Hospital, Sofia, Bulgaria|MBAL "Stara Zagora" EAD, Stara Zagora, Bulgaria|Thalassotherapia, Opatija, Croatia|KBC Osijek Ambulanta za bol, Osijek, Croatia|University Hospital Centre Zagreb, Zagreb, Croatia|University Hospital U Sv.Anny, Brno, Czech Republic|University Hospital Kralovske Vinohrady, Praha 10, Czech Republic|SZZ-Jizni Mesto II, Praha 11, Czech Republic|Institute of Rheumatology, Praha 2, Czech Republic|Rheumatology Out-patient Department, Praha 6, Czech Republic|Institute of Rheumatology, Beograd, Former Serbia and Montenegro|Institute of Rheumatology - Niska Banja, Niska Banja, Former Serbia and Montenegro|Clinical Center Zemun, Zemun, Former Serbia and Montenegro|Szpital Specjalistyczny Nr 1, Bytom, Poland|Wojewodzki Szpital Zespolony, Elblag, Poland|Malopolskie Centrum Medyczne, Krakow, Poland|"Gabinety Profesorow" Prywatna Praktyka, Lublin, Poland|Instytut Medycyny Wsi im. Witolda Chodzki, Lublin, Poland|Wojewodzki Zespo?? Reumatologiczny im., Sopot, Poland|NZOZ "Nasz Lekarz" Praktyka Grupowa Lekarzy, Torun, Poland|Okregowy Szpital Kolejowy, Wroclaw, Poland|ZOZ Zyrardow, Zyrardow, Poland|Pirogov City Clinical Hospital #1, Moscow, Russian Federation|State Institute of Rheumatology of RAMS, Moscow, Russian Federation|State Clinical Immunology Research, Novosibirsk, Russian Federation|Ryazan Regional Clinical Cardiologic, Ryazan, Russian Federation|Saint Petersburg Clinical Hospital, Saint Petersburg, Russian Federation|Saint-Petersburg City Hospital, Saint-Petersburg, Russian Federation|Saint-Petersburg Medical Academy, Saint-Petersburg, Russian Federation|Saratov Regional Clinical Hospital, Saratov, Russian Federation|City Pokrovskaya Hospital, St. Petersburg, Russian Federation|EVIDENCE Clinical and Pharmaceutical Research, St. Petersburg, Russian Federation|Leningrad Regional Hospital, St. Petersburg, Russian Federation|National Institute of Rheumatic Diseases, Piestany, Slovakia|Clinical Center Ljubljana, Ljubljana, Slovenia|Dniepropetrovsk State Medical Academy, Dniepropetrovsk, Ukraine|Donetsk State Medical University, Donetsk, Ukraine|Institute of Cardiology of Ukranian AMS, Kiev, Ukraine|Institute of Gerontology of Ukrainian AMS, Kiev, Ukraine|SanaClis s.r.o., Kiev, Ukraine|Zaporizhya Medical Institute, Zaporizhya, Ukraine Less <<
NCT00395577 Rheumatoid Arthritis PHASE2 COMPLETED 2025-07-07 Call For Information, Dimitrov... More >>grad, Bulgaria|Call For Information, Pleven, Bulgaria|Call For Information, Sofia, Bulgaria|Call For Information, Veliko Tarnovo, Bulgaria|Call For Information, Osijek, Croatia|Call For Information, Zagreb, Croatia|Call For Information, Belgrade, Former Serbia and Montenegro|Call For Information, Niska Banja, Former Serbia and Montenegro|Call For Information, Zemun, Former Serbia and Montenegro|Call For Information, Bytom, Poland|Call For Information, Krakow, Poland|Call for Information, Torun, Poland|Call For Information, Zyrardow, Poland|Call For Information, Novosibirsk, Russian Federation|Call For Information, Saratov, Russian Federation|Call For Information, St. Petersburg, Russian Federation|Call For Information, Ljubljana, Slovenia Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.47mL

0.49mL

0.25mL

12.37mL

2.47mL

1.24mL

24.73mL

4.95mL

2.47mL

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

References

 

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