Name: Doramapimod (BIRB 796)
Brand: Selleck Chemicals
SKU: S1574
Rating: 5 (93 reviews)

Doramapimod (BIRB 796) Chemical Structure

CAS No. 285983-48-4

Selleck's Doramapimod (BIRB 796) has been cited by 93 publications

Purity & Quality Control

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p38 MAPK Signaling Pathway Map

Biological Activity

Description

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.

Targets

JNK2 ^[1] ()	c-RAF ^[1] ()	Fyn ^[1] ()	p38α ^[1] (Cell-free assay)	p38α ^[7] ()
			0.1 nM(Kd)	38 nM

In vitro

BIRB 796 shows no significant inhibition to ERK-1, SYK, IKK2β, ZAP-70, EGF receptor kinase, HER2, protein kinase A (PKA), PKC, PKC-α, PKC-β (I and II) and PKC-γ. BIRB 796 greatly improves binding affinity by forming a hydrogen bond between the morpholine oxygen and the ATP-binding domain of p38α. BIRB 796 represents one of the most potent and slowest dissociating inhibitors against human p38 MAP kinase now known. ^[1] BIRB 796 potently inhibits c-Raf-1 and Jnk2α2 with IC50 of 1.4 and 0.1 nM, respectively. ^[2] BIRB796 also inhibits the activity and the activation of SAPK3/p38γ at a higher concentration than it does in p38α. BIRB796 blocks the stress-induced phosphorylation of the scaffold protein SAP97, which is a physiological substrate of SAPK3/p38γ. BIRB796 blocks JNK1/2 activation and activity in HEK293 cells, while not inhibits the activation and activity of ERK1/ERK2 in Hela cells. Moreover, the binding of BIRB796 to the p38 MAPKs or JNK1/2 is impairing their phosphorylation by the upstream kinase MKK6 or MKK4 rather than enhancing their dephosphorylation. ^[3] BIRB 796 blocks baseline and bortezomib-triggered upregulation of p38 MAPK and Hsp27 phosphorylation, thereby enhancing cytotoxicity and caspase activation. BIRB 796 downregulates IL-6 and VEGF secretion in BMSCs triggered by TNF-α and TGF-β1. ^[4] BIRB-796 has a pyrazole scaffold that places a lipophilic t-butyl group into the lower selectivity site and a tolyl ring into the upper selectivity site. BIRB-796 also inhibits B-Raf and Abl with IC50 of 83 nM and 14.6 μM, respectively. ^[5]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

HOP-92	NH7TbXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NYPwWFhFUUN3ME2yOE4{QDN6IN88US=>	M1K4bFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExOzZ4Nz:nQnNCVkeHUkyvZV4>
NCI-H2228	MkCxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NHzBOZVKSzVyPUKzMlY3PjhizszN	MmDtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA{PjZ5Lze+V2FPT0WUPD;hQi=>
CAPAN-1	MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MoG3TWM2OD1{Mj6xPFg1KM7:TR?=	M3XJSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExOzZ4Nz:nQnNCVkeHUkyvZV4>
SK-MEL-1	NYj6[lhUT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NHvpRotKSzVyPUKwMlM3QDNizszN	MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
DB	NWnYSHVlT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MnvtTWM2OD1zOD63PVI{KM7:TR?=	MoH1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA{PjZ5Lze+V2FPT0WUPD;hQi=>
AN3-CA	MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NVXUd\|M2UUN3ME2xPE4yKM7:TR?=	NIj6Um89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODN4NkevK\|5USU6JRWK8M4E,
EW-13	Mn3rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MWLJR\|UxRTF5Lkm1NVYh\|ryP	NVrNUXZURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB\|Nk[3M{c,W0GQR1XSQE9iRg>?
LC-2-ad	MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MXTJR\|UxRTF5LkSzOlYh\|ryP	NWfDfI9iRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB\|Nk[3M{c,W0GQR1XSQE9iRg>?
ES8	NG[zVXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NVXjcXczUUN3ME2xO{4yPjdizszN	MmDKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA{PjZ5Lze+V2FPT0WUPD;hQi=>
NCI-H1581	M2L6VGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MlHKTWM2OD1zNz6wOFQ4KM7:TR?=	NEjndoU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODN4NkevK\|5USU6JRWK8M4E,
HMV-II	M4foZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MnfFTWM2OD1zND6yN\|A6KM7:TR?=	M3Xl[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExOzZ4Nz:nQnNCVkeHUkyvZV4>
BEN	M3zPcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NYXZbmZFUUN3ME2xN{4yOjZ2IN88US=>	NXHRUWtwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB\|Nk[3M{c,W0GQR1XSQE9iRg>?
NBsusSR	NYX5fZJTT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NYnLfHlkUUN3ME2xNE45OjN3IN88US=>	MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
MS-1	MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MlzLTWM2OD1zMD64NlM2KM7:TR?=	NInwWJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODN4NkevK\|5USU6JRWK8M4E,
BFTC-905	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M13lNWlEPTB;MUCuNVI{OyEQvF2=	NYrkVpk1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB\|Nk[3M{c,W0GQR1XSQE9iRg>?
NCI-SNU-1	NEHBXI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NVzL[mcxUUN3ME25MlA3PzN7IN88US=>	NGXKcXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODN4NkevK\|5USU6JRWK8M4E,
MPP-89	MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NGXjPIFKSzVyPUiuOFYzPTFizszN	NWrXVGl2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB\|Nk[3M{c,W0GQR1XSQE9iRg>?
T-24	MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NG\MRpJKSzVyPUiuOFA3PzNizszN	NVS1PIlNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB\|Nk[3M{c,W0GQR1XSQE9iRg>?
KP-N-YN	M17Ke2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		MVzJR\|UxRThwMkCxPUDPxE1?	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
IST-MES1	NWDsVHNQT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		MUHJR\|UxRTdwOUW2N\|ch\|ryP	NUHpboEzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB\|Nk[3M{c,W0GQR1XSQE9iRg>?
NCI-H358	MoDGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NVKw[ot[UUN3ME23MlU{QCEQvF2=	NVzHc5puRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB\|Nk[3M{c,W0GQR1XSQE9iRg>?
GOTO	NV2xbFE5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NWXnSoNxUUN3ME22MlM6OTZzIN88US=>	NV\MO2xIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB\|Nk[3M{c,W0GQR1XSQE9iRg>?
DU-145	Mn;6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MWTJR\|UxRTNwOUO4NVEh\|ryP	NGTWPVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODN4NkevK\|5USU6JRWK8M4E,
EoL-1-cell	MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NYHNeVNIUUN3ME2wMlM1PzZ\|IN88US=>	MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
KYSE-270	MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MnnwTWM2OD1{ND61OVc{KM7:TR?=	MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
HCC1806	Mn;5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MX;JR\|UxRTJ2Lke3PVkh\|ryP	M2rjTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExOzZ4Nz:nQnNCVkeHUkyvZV4>
HuO-3N1	Ml3US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NH3Lem1KSzVyPUK1MlgyQDVizszN	NFTuVIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODN4NkevK\|5USU6JRWK8M4E,
HOS	NXzXXZpbT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NVrwTnNwUUN3ME2yOU46Ojl{IN88US=>	NUizWJFLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB\|Nk[3M{c,W0GQR1XSQE9iRg>?
KYSE-510	NIjXe4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M{\sO2lEPTB;Mk[uNVYyOiEQvF2=	MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
COLO-741	MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		NV;2bldlUUN3ME2yOk4{OzJ7IN88US=>	M4jON\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExOzZ4Nz:nQnNCVkeHUkyvZV4>
H-EMC-SS	NVTXSZVLT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NVq1cVVDUUN3ME2yOk46OjR3IN88US=>	NF3leFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODN4NkevK\|5USU6JRWK8M4E,
HCC1937	NVXnRZVYT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		Ml\JTWM2OD1{Nz6yNlM5KM7:TR?=	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
NCI-H2126	MoryS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		NEjhXphKSzVyPUK3MlM6PzVizszN	M{[3ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExOzZ4Nz:nQnNCVkeHUkyvZV4>
NCI-H1703	MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		M3PKXGlEPTB;MkiuNFQyOyEQvF2=	MlXVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA{PjZ5Lze+V2FPT0WUPD;hQi=>
U-2-OS	MkLkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MkTVTWM2OD1{OD61OVE2KM7:TR?=	NFrEOWg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODN4NkevK\|5USU6JRWK8M4E,
DBTRG-05MG	M{\2T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7		NW\YZow4UUN3ME2yPE42PjVzIN88US=>	MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
MHH-ES-1	Ml7RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?		MYnJR\|UxRTNzLkm0NUDPxE1?	NVLBbJJiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB\|Nk[3M{c,W0GQR1XSQE9iRg>?
HCC1419	NWDCeYZiT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=		NX7vVYduUUN3ME2zNk4yOTF7IN88US=>	M2PPWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExOzZ4Nz:nQnNCVkeHUkyvZV4>
HOP-62	MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?		MWHJR\|UxRTN{LkK3NFEh\|ryP	MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFM3PjdxJ{7TRW5ITVJ:L3G+
AM-38	NH;qO4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		MX3JR\|UxRTN{Lkm5N\|Eh\|ryP	NU\sRlJ2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB\|Nk[3M{c,W0GQR1XSQE9iRg>?
NCI-H2009	NELEbmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		NXi3e\|VwUUN3ME2zN{41ODB5IN88US=>	NX70PYdbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB\|Nk[3M{c,W0GQR1XSQE9iRg>?
EM-2	NH3ydWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=		M2TsXmlEPTB;M{OuOVUyOSEQvF2=	Mny0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA{PjZ5Lze+V2FPT0WUPD;hQi=>
SW1116	M1LXRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7		Mm\rTWM2OD1\|ND60PFM5KM7:TR?=	M4\ndlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExOzZ4Nz:nQnNCVkeHUkyvZV4>
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Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Western blot

p-p38 / p38 ; mTOR / p-S6K / S6K / p-MK2 / MK2 / p-Hsp27 / Hsp27 ; p-p38 / γ-H2AX

23349819 26844273 27082306

In vivo

BIRB 796 (30 mg/kg) inhibits 84% of TNF-α in LPS-stimulated mice and demonstrates efficacy in a mouse model of established collagen-induced arthritis. ^[1] BIRB 796 has good pharmacokinetic performance even after oral administration in mice. ^[2]

Protocol (from reference)

Animal Research: ^[2]	Animal Models: Collagen-induced arthritis in female Balb/c mice Dosages: 1 mg/kg (intravenous) or 10 mg/kg (oral) Administration: Intravenous injection or by oral (Only for Reference)

References

+ Expand

Solubility (25°C)

In vitro	DMSO	100 mg/mL (189.51 mM)
	Ethanol	100 mg/mL (189.51 mM)
	Water	Insoluble
In vivo	Add solvents to the product individually and in order (Data is from Selleck tests instead of citations): 5% DMSO+40%PEG300+5%Tween80 +50%H2O For best results, use promptly after mixing. Click to purchase: PEG300 Tween 80	5mg/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

Molecular Weight	527.66
Formula	C₃₁H₃₇N₅O₃
CAS No.	285983-48-4
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC1=CC=C(C=C1)N2C(=CC(=N2)C(C)(C)C)NC(=O)NC3=CC=C(C4=CC=CC=C43)OCCN5CCOCC5

Download Doramapimod (BIRB 796) SDF

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02211885	Completed	Drug: 14C-BIRB 796 BS	Healthy	Boehringer Ingelheim	October 2002	Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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
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