VX-702

Item no.	S6005-10
Manufacturer	Selleckchem
CASRN	745833-23-2
Amount	10 mg
Quantity options	10 mg 100 mg 1 g 10 g 10 mM/1 mL 200 mg 25 mg 5 g
Category	Oncology Neuroscience Neuroinflammation Metabolism Diabetes Glucose Homeostasis Inhibitors & Compound Libraries Small Molecules By Organ Bone Cancer
Type	Inhibitors
Specific against	other
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
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	p38 MAPKalpha,p38 MAPK
Similar products	VX-702
Available
Storage Conditions	2 years -80 in solvent
Molecular Weight	404, 3
Administration	Administered via p.o.
Animal Models	Mouse with collagen-induced arthritis
Clinical Trials	VX-702 is currently in Phase II clinical trial in patients with rheumatoid arthritis.
Dosages	<=10 mg/kg
IC50	4 - 20 nM [1], 4 - 20 nM [1], 4 - 20 nM [1], 4 - 20 nM [1], 4 - 20 nM [1], 4 - 20 nM [1]
In vitro	Pre-incubation of platelets with VX-702 (1 uM) completely or partially inhibits p38 activation (IC50 4 to 20 nM) induced by platelet agonists including thrombin, SFLLRN, AYPGKF, U46619 and collagen. VX-702, shows no effect on platelet aggregation induced by any of the p38 MAPK agonists in the presence or absence of anti-platelet therapies. [1] VX-702 inhibits the production of IL-6, IL-1beta and TNFalpha (IC50 = 59, 122 and 99 ng/mL, respectively) in a dose-dependent manner. [2]
In vivo	The half-life of VX-702 is 16 to 20 hours, with a median clearance of 3.75 L/h and a volume of distribution of 73 L/kg. Both AUC and Cmax values are dose proportional for VX-702, which is predominantly cleared renally. [2] VX-702 (at a dose of 0.1 mg/kg twice daily) has an equivalent effect as that of methotrexate (0.1 mg/kg). In addition, VX-702 (5 mg/kg twice daily) also has an equivalent effect as prednisolone (10 mg/kg once daily), as measured by percentage inhibition of wrist joint erosion and inflammation score. [3] VX-702 selectively inhibits activation of p38 MAPK after ischemia with no effects on ERKs and JNKs. The MI/AAR ratio is significantly reduced in the 50 mg/kg group compared with the 5 mg/kg and vehicle groups.[4]
Solubility (25C)	DMSO 81 mg/mL, Water <1 mg/mL, Ethanol <1 mg/mL
Information	VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β.
Chemical Name	1-(5-carbamoyl-6-(2, 4-difluorophenyl)pyridin-2-yl)-1-(2, 6-difluorophenyl)urea
Features	VX-702 is a highly selective, orally active inhibitor of p38 MAPK

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