VX-702 is a highly selective p38α MAPK inhibitor that acts 14 times more effectively on p38α than on p38β.

 

Brand: BCM

 

Target: p38 MAPK; Autophagy

 

Signaling Pathways: Autophagy; MAPK

 

In Vitro: Treatment with VX-702 (0.1 mg/kg) twice daily was similar to treatment with methotrexate (0.1 mg/kg). In addition, treatment with VX-702 twice daily (5 mg/kg) was similar to treatment with hydroprednisone once daily (10 mg/kg). The MI/AAR ratio was significantly lower in the 50 mg/kg treatment group compared to the control group and the treatment group treated with 5 mg/kg VX-702. VX-702 has a half-life of 16-20 h, a half-clearance dose of 3.75 L and a distribution volume of 73 L/kg. VX-702 has a selective inhibitory effect on p38 MAPK activity, but does not affect ERKs and JNKs.

 

In Vivo: VX-702 did not affect platelet aggregation induced by p38 MAPK stimulants. Treatment of platelets with VX-702 (1 μM) completely or partially inhibits p38 activity (IC50:4-20 nM) induced by platelet stimulants including thrombin,AYPGKF,SFLLRN,U46619, and collagen. The production of IL-6 (IC50:59 ng/ml), IL-1β (IC50:122 ng/ml) and TNF-α (IC50:99 ng/ml) was dose-dependently inhibited by VX-702.

 

Boiling Point: 555.2±60.0 °C(Predicted)

 

pKa: 10.65±0.50(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; insoluble in Ethanol.

 

GHS: GHS07

 

Isomeric SMILES: C1=CC(=C(C(=C1)F)N(C2=NC(=C(C=C2)C(=O)N)C3=C(C=C(C=C3)F)F)C(=O)N)F  

 

InChIKey: FYSRKRZDBHOFAY-UHFFFAOYSA-N  

 

InChI: InChI=1S/C19H12F4N4O2/c20-9-4-5-10(14(23)8-9)16-11(18(24)28)6-7-15(26-16)27(19(25)29)17-12(21)2-1-3-13(17)22/h1-8H,(H2,24,28)(H2,25,29) 

 

Attribute
[Chem Name]	6-(N-carbamoyl-2,6-difluoroanilino)-2-(2,4-difluorophenyl)pyridine-3-carboxamide
[Synonym]	VX-702
[CAS No.]	745833-23-2
[MDL No.]	MFCD11616590
[Formula]	C19H12F4N4O2
[Molecular]	404.32
[Form]	White solid powder
[Storage]	Keep in dark place. Inert atmosphere. Room temperature

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