VX-702

Catalog No.S6005

Molecular Weight(MW): 404.3

VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2.

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J Invest Dermatol, 2018, 138(6):1380-1390. VX-702 purchased from Selleck.

Reduction of IL-10 expression due to p38 inhibition is observed also in CpG-stimulated B cells and using VX-702. B cells were pre-treated with 10 uM of VX-702 for 1 h and stimulated with LPS or CpG for 24 or 48 h. Bar graphs indicate mean (±SEM) IL-10 concentrations at 48 h from n = 4 (LPS) and n = 3 (CpG) experiments. Significant differences against the no inhibitor condition were calculated using a paired Student's t-test and indicated as follows: *p < 0.05, ***p < 0.001.

Mol Immunol 2014 62(2), 266-76. VX-702 purchased from Selleck.
Bone marrow derived macrophages were pre-treated with the indicated concentrations of VX702 for 1h prior to LPS treatment (100 ng/ml). TNF-a production was analyzed 24h later.

Lee lay hoon from National University of Singapore. VX-702 purchased from Selleck.

Purity & Quality Control

Choose Selective p38 MAPK Inhibitors

Biological Activity

Description

VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2.

Features

Highly selective, orally active inhibitor of p38 MAPK.

Targets

p38α ^[1]
(Cell-free assay)

4 nM-20 nM

In vitro

Pre-incubation of platelets with VX-702 (1 μM) 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-1β and TNFα (IC50 = 59, 122 and 99 ng/mL, respectively) in a dose-dependent manner. ^[2]

Cell Data

Cell Lines	Assay Type	Activity Description	PMID
HOP-62 cell	MVXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MYrJcohq[mm2aX;uJI9nKGi3bXHuJGhQWC14MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuNFE2PDNizszN	NWnrSY9ZW0GQR1XS
human NCI-H720 cell	NYDEVlI2T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MVXJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KN{KwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4xOTZ6MjFOwG0>	MUXTRW5ITVJ?
JVM-2 cell	M4PmUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	M3jGVGlvcGmkaYTpc44hd2ZiaIXtZY4hUl[PLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlA5OyEQvF2=	MVTTRW5ITVJ?
human NCI-H69 cell	NXrMfGlTT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NIm0UnBKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IOlkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjB7OUSxJO69VQ>?	MUPTRW5ITVJ?
human BV-173 cell	M2fweWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NGDxbnBKdmirYnn0bY9vKG:oIHj1cYFvKEKYLUG3N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTF\|OE[g{txO	MX;TRW5ITVJ?
human KU812 cell	NVvu[HRXT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NXTNfnB[UW6qaXLpeIlwdiCxZjDoeY1idiCNVUixNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTJ2OEig{txO	NEPKfIVUSU6JRWK=
human DU-145 cell	MoL3S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NGrCRWVKdmirYnn0bY9vKG:oIHj1cYFvKESXLUG0OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTR3NUSg{txO	NWnLS4RoW0GQR1XS
KARPAS-45 cell	MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MnjpTY5pcWKrdHnvckBw\iCqdX3hckBMSVKSQWOtOFUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjF2OEK2JO69VQ>?	M2TyNHNCVkeHUh?=
human AGS cell	Mm\hS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MnvVTY5pcWKrdHnvckBw\iCqdX3hckBCT1NiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkG1NlUyKM7:TR?=	M371WHNCVkeHUh?=
human MOLT-13 cell	NYDVSZFvT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MnHnTY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yPTl6MTFOwG0>	NEPtfIVUSU6JRWK=
human NCI-H209 cell	Ml2wS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MmnPTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKwPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTd3ODFOwG0>	MUfTRW5ITVJ?
human CTV-1 cell	NHu4TpZIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NXHWdncyUW6qaXLpeIlwdiCxZjDoeY1idiCFVG[tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTh\|OEmg{txO	NU\KW2hsW0GQR1XS
LU-139 cell	NH2yN4dIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NHLr[\|dKdmirYnn0bY9vKG:oIHj1cYFvKEyXLUGzPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOTl2M{Wg{txO	Mn2yV2FPT0WU
ML-2 cell	MnTHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NHXidJJKdmirYnn0bY9vKG:oIHj1cYFvKE2OLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIzPjZzIN88US=>	MmXNV2FPT0WU
human K5 cell	NWjxWHhPT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NIflUIlKdmirYnn0bY9vKG:oIHj1cYFvKEt3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD6yNlkyPyEQvF2=	M4rKbnNCVkeHUh?=
human SBC-1 cell	M1j2[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	MYDJcohq[mm2aX;uJI9nKGi3bXHuJHNDSy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD6yN\|YzKM7:TR?=	M2HmWHNCVkeHUh?=
human COR-L88 cell	NGPaSGtIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MVPJcohq[mm2aX;uJI9nKGi3bXHuJGNQWi2OOEigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM{PDhizszN	MXzTRW5ITVJ?
human KY821 cell	MmrOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M1LSVmlvcGmkaYTpc44hd2ZiaIXtZY4hU1l6MkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlM6PjB\|IN88US=>	MUTTRW5ITVJ?
human HCC2218 cell	NV3wNldNT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NYj0RXc3UW6qaXLpeIlwdiCxZjDoeY1idiCKQ1OyNlE5KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OC52OUeyPEDPxE1?	MU\TRW5ITVJ?
human ECC10 cell	NWW4T\|VRT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M{m3WmlvcGmkaYTpc44hd2ZiaIXtZY4hTUOFMUCgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlY2Ozh7IN88US=>	M2LDWHNCVkeHUh?=
human EW-3 cell	MmjPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M33HUWlvcGmkaYTpc44hd2ZiaIXtZY4hTVdvMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUCuOlY3OTFizszN	MnTzV2FPT0WU
human EW-18 cell	NWLuO2psT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NYPNdJM6UW6qaXLpeIlwdiCxZjDoeY1idiCHVz2xPEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvPzR4N{mg{txO	NGT5NpNUSU6JRWK=
human UACC-257 cell	MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NYftSIlDUW6qaXLpeIlwdiCxZjDoeY1idiCXQVPDMVI2PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTFwMkCzNlYh\|ryP	MkjkV2FPT0WU
human G-361 cell	MnK5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MnHPTY5pcWKrdHnvckBw\iCqdX3hckBINTN4MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUGuOFk2OTlizszN	NVLleIp4W0GQR1XS
human HMV-II cell	NYLyNWRYT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	Mo\VTY5pcWKrdHnvckBw\iCqdX3hckBJVVZvSVmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlc4OTh2IN88US=>	NELZSnJUSU6JRWK=
human DEL cell	NWT6R\|VqT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NY\2bGx4UW6qaXLpeIlwdiCxZjDoeY1idiCGRVygZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlIxPzB2IN88US=>	NVHucXg5W0GQR1XS
human IGROV-1 cell	NYm0cZdpT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M3XHOGlvcGmkaYTpc44hd2ZiaIXtZY4hUUeUT2[tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvPDNzOEig{txO	NY\5Oo5LW0GQR1XS
human SK-OV-3 cell	MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MXLJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU:YLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlYyPjl5IN88US=>	MYPTRW5ITVJ?
human LAMA-84 cell	NIT3T4hIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MkfQTY5pcWKrdHnvckBw\iCqdX3hckBNSU2DLUi0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk44OTJ6NDFOwG0>	Ml72V2FPT0WU
human NCI-H510A cell	M{LVUWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NUjoZpZ3UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFUyOEFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{LkmyOVI3KM7:TR?=	MmLSV2FPT0WU
human CP66-MEL cell	NVz3S4V6T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M3LUXGlvcGmkaYTpc44hd2ZiaIXtZY4hS1B4Nj3NSWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjl\|NUW5JO69VQ>?	MUnTRW5ITVJ?
human HAL-01 cell	Mo\yS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NXLCSI5nUW6qaXLpeIlwdiCxZjDoeY1idiCKQVytNFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjJ5OUG4JO69VQ>?	NX:3eGJDW0GQR1XS
human RS4-11 cell	MlHkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NHTkfIpKdmirYnn0bY9vKG:oIHj1cYFvKFKVND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMvPzB3N{Og{txO	MXrTRW5ITVJ?
human RPMI-8226 cell	M3\wSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	M1fuXmlvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST24NlI3KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oy56MkO3OkDPxE1?	MnTXV2FPT0WU
human NCI-H82 cell	M4q3VWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NFjONmFKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3IPFIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{Njh7M{C1JO69VQ>?	NH3lRWhUSU6JRWK=
human NY cells	M3zEO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7	MX;Jcohq[mm2aX;uJI9nKGi3bXHuJG5[KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PC5{N{[zO{DPxE1?	MUfTRW5ITVJ?
human MDA-MB-361 cell	MnPOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M{fXe2lvcGmkaYTpc44hd2ZiaIXtZY4hVUSDLV3CMVM3OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTRwNEOxOVgh\|ryP	NWnJNI9pW0GQR1XS
human MOLT-4 cell	M1vPO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NGm0eVZKdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStOEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQvQTlzOUOg{txO	NG\scndUSU6JRWK=
human DU-4475 cell	NVr0N5NpT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M2[5UGlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvNES3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvODV3NkWg{txO	M33ZWXNCVkeHUh?=
human ESS-1 cell	NXT1[\|A3T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NE\CVnZKdmirYnn0bY9vKG:oIHj1cYFvKEWVUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4zQTF5OTFOwG0>	MUHTRW5ITVJ?
human NCI-H1299 cell	M{fNN2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7	MUPJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUK5PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvPTNyM{Og{txO	M4S0WnNCVkeHUh?=
human COLO-684 cell	NIPxdo9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MVHJcohq[mm2aX;uJI9nKGi3bXHuJGNQVE9vNki0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU42QDF4NTFOwG0>	MV\TRW5ITVJ?
human MV-4-11 cell	NGPoelRIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MXLJcohq[mm2aX;uJI9nKGi3bXHuJG1XNTRvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlcyOTl7IN88US=>	M3\TO3NCVkeHUh?=
human D-542MG cell	MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M1rJbmlvcGmkaYTpc44hd2ZiaIXtZY4hTC13NELNS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVYvOzl{N{Kg{txO	MknBV2FPT0WU
human A4-Fuk cell	Mn7mS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MYHJcohq[mm2aX;uJI9nKGi3bXHuJGE1NU[3azDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPU[uOFM3PjJizszN	M2jhVXNCVkeHUh?=
human HL-60 cell	MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MkC2TY5pcWKrdHnvckBw\iCqdX3hckBJVC14MDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUeuOVIzOTJizszN	Mof3V2FPT0WU
human NCI-H526 cell	MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NVzyV2N5UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFUzPiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTdwNUm4NFEh\|ryP	M1e0UHNCVkeHUh?=
human L-363 cell	NUPK[HZNT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NXvPO\|NoUW6qaXLpeIlwdiCxZjDoeY1idiCOLUO2N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcvPzl{NUKg{txO	NUW3VGljW0GQR1XS
human A388 cell	NWe3WGZ7T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NVjQVFExUW6qaXLpeIlwdiCxZjDoeY1idiCDM{i4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O{45ODN6NDFOwG0>	MnnoV2FPT0WU
human MS-1	NIH2OnZIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	Mo\MTY5pcWKrdHnvckBw\iCqdX3hckBOWy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;Nz64N\|Q3PSEQvF2=	MYrTRW5ITVJ?
human JAR cell	NVLRVnlWT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MVfJcohq[mm2aX;uJI9nKGi3bXHuJGpCWiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTdwOES5NlMh\|ryP	NXH3dldRW0GQR1XS
human TI-73 cell	NF:zOI9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=	M4XZRWlvcGmkaYTpc44hd2ZiaIXtZY4hXElvN{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24MlA3OjJizszN	NH7tZ2pUSU6JRWK=
human CTB-1 cell	MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M3rYRmlvcGmkaYTpc44hd2ZiaIXtZY4hS1SELUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24MlE4QDJ3IN88US=>	MojJV2FPT0WU
human SK-NEP-1 cell	MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MlTNTY5pcWKrdHnvckBw\iCqdX3hckBUUy2QRWCtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjNyM{ig{txO	MkDZV2FPT0WU
human HT-29 cell	NVnrZpVJT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGhVNTJ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MUOuPVEyOSEQvF2=	MX3TRW5ITVJ?
human NCI-H1092 cell	NXzaNIh5T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MlTiTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEGwPVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPC5\|MUig{txO	M1fxNnNCVkeHUh?=
human KMOE-2 cell	MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MkDpTY5pcWKrdHnvckBw\iCqdX3hckBMVU:HLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOE43OTd6IN88US=>	NFHpZ5pUSU6JRWK=
human EM-2 cell	NI[3[FJIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MWfJcohq[mm2aX;uJI9nKGi3bXHuJGVONTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zNT6yPFQyKM7:TR?=	MlLwV2FPT0WU
human RT-112 cell	MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NYjONGVxUW6qaXLpeIlwdiCxZjDoeY1idiCUVD2xNVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPS5\|OUi0JO69VQ>?	NYO3U5FKW0GQR1XS
human DB cell	MlPpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NWGxbnoxUW6qaXLpeIlwdiCxZjDoeY1idiCGQjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUG1Mlg2OTNizszN	M3L6enNCVkeHUh?=
human NCI-H1770 cell	M3jLXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NH65VGRKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVc4OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7	M{\ESHNCVkeHUh?=
human CAL-54 cell	M4XvSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	MknETY5pcWKrdHnvckBw\iCqdX3hckBESUxvNUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOk44OyEQvF2=	M3PsR3NCVkeHUh?=
human NB14 cell	NWrpXVZUT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NYmxTmpDUW6qaXLpeIlwdiCxZjDoeY1idiCQQkG0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVcvPjN7NTFOwG0>	NVL2bWhlW0GQR1XS
human RPMI-7951 cell	Ml7qS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MnLrTY5pcWKrdHnvckBw\iCqdX3hckBTWE2LLUe5OVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yQS5zN{izJO69VQ>?	MkL0V2FPT0WU
human T47D cell	NETHXXFIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NWjSXZR{UW6qaXLpeIlwdiCxZjDoeY1idiCWNEfEJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlEvOjJ2MzFOwG0>	M2XHc3NCVkeHUh?=
human A549 cell	M3zSVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	M{HOPGlvcGmkaYTpc44hd2ZiaIXtZY4hSTV2OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUKxMlI5OTFizszN	NG\IT3BUSU6JRWK=
human A2780 cell	M{HLdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NIjI[JhKdmirYnn0bY9vKG:oIHj1cYFvKEF{N{iwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlEvQDJ{NTFOwG0>	M2LGSHNCVkeHUh?=
human SK-MEL-24 cell	NH;qbJFIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	M{jXfmlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVI1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzNwMEOxNUDPxE1?	MWXTRW5ITVJ?

... Click to View More Cell Line Experimental Data

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 C_max 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]

Protocol

References

[4] Bhattacharya K, et al. Circulation, 2003, 108(17), 882.

+ Expand

Solubility (25°C)

In vitro	DMSO	81 mg/mL (200.34 mM)
	Water	Insoluble
	Ethanol	Insoluble
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 30% PEG400+0.5% Tween80+5% propylene glycol For best results, use promptly after mixing.	30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download VX-702 SDF

Molecular Weight	404.3
Formula	C₁₉H₁₂F₄N₄O₂
CAS No.	745833-23-2
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	N/A

Bio Calculators

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration _(start) x Volume _(start) = Concentration _(final) x Volume _(final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

Serial Dilutions
Concertration (start):
Dilution-folds:

Computed Result

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2018-10-19)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00395577	Completed	Rheumatoid Arthritis	Vertex Pharmaceuticals Incorporated	November 2006	Phase 2
NCT00205478	Completed	Rheumatoid Arthritis	Vertex Pharmaceuticals Incorporated	June 2005	Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

p38 MAPK Signaling Pathway Map

p38 MAPK Inhibitors with Unique Features

Pan p38 MAPK Inhibitor

SB202190 (FHPI) : Pan-p38α/β inhibitor, IC50=50 nM/100 nM.
Most Potent p38 MAPK Inhibitor

Skepinone-L ^New : p38α-MAPK, IC50=5 nM.
p38 MAPK Inhibitor in Clinical Trial

PH-797804 : Phase II for Chronic Obstructive Pulmonary Disease (COPD).
Newest p38 MAPK Inhibitor

Skepinone-L ^New : Selective p38α-MAPK inhibitor with IC50 of 5 nM.

Related p38 MAPK Products

Pexmetinib (ARRY-614) ^New

Pexmetinib (ARRY-614) is a potent, orally bioavailable, dual p38 MAPK/Tie-2 inhibitor with IC50 of 4 nM/18 nM in a HEK-293 cell line. Phase 1.
SB239063 ^New

SB239063 is a potent and selective p38 MAPKα/β inhibitor with IC50 of 44 nM, showing no activity against the γ- and δ-kinase isoforms.
GDC-0994 ^New

GDC-0994 is a potent, orally available and highly selective ERK1/2 inhibitor with IC50 of 1.1 nM and 0.3 nM, respectively. Phase 1.
SB203580

SB203580 is a p38 MAPK inhibitor with IC50 of 0.3-0.5 μM in THP-1 cells, 10-fold less sensitive to SAPK3(106T) and SAPK4(106T) and blocks PKB phosphorylation with IC50 of 3-5 μM.

Features:First reported p38 inhibitor.
Doramapimod (BIRB 796)

Doramapimod (BIRB 796) is a pan-p38 MAPK inhibitor with IC50 of 38 nM, 65 nM, 200 nM and 520 nM for p38α/β/γ/δ in cell-free assays, and binds p38α with K_d of 0.1 nM in THP-1 cells, 330-fold greater selectivity versus JNK2, weak inhibition for c-RAF, Fyn and Lck, insignificant inhibition of ERK-1, SYK, IKK2.

Features:The first p38 MAPK inhibitor to be tested in a phase III clinical trial.
SB202190 (FHPI)

SB202190 (FHPI) is a potent p38 MAPK inhibitor targeting p38α/β with IC50 of 50 nM/100 nM in cell-free assays, sometimes used instead of SB 203580 to investigate potential roles for SAPK2a/p38 in vivo.
Ralimetinib (LY2228820)

Ralimetinib (LY2228820) is a novel and potent inhibitor of p38 MAPK with IC50 of 7 nM in a cell-free assay, does not alter p38 MAPK activation. Phase 1/2.
Losmapimod (GW856553X)

Losmapimod (GW856553X) is a selective, potent, and orally active p38 MAPK inhibitor with pK_i of 8.1 and 7.6 for p38α and p38β, respectively. Phase 3.
PH-797804

PH-797804 is a novel pyridinone inhibitor of p38α with IC50 of 26 nM in a cell-free assay; 4-fold more selective versus p38β and does not inhibit JNK2. Phase 2.
TAK-715

TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1. Phase 2.

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VX-702