Ralimetinib (LY2228820) dimesylate

Catalog No.S1494

For research use only.

Ralimetinib (LY2228820) dimesylate 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.

Ralimetinib (LY2228820) dimesylate Chemical Structure

CAS No. 862507-23-1

Selleck's Ralimetinib (LY2228820) dimesylate has been cited by 59 publications

Purity & Quality Control

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Biological Activity

Description Ralimetinib (LY2228820) dimesylate 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.
Targets
p38α [1]
(Cell-free assay)
7 nM
In vitro

LY2228820 inhibits p38α, as well as the level of phosphoMAPKAPK-2 (pMK2) in RAW 264.7 cells, with IC50 values of 7 nM and 34.3 nM, respectively. Furthermore, LY2228820 inhibits lipopolysaccharide (LPS)-induced TNFα formation in murine peritoneal macrophages, with IC50 of 5.2 nM. [1] In multiple myeloma (MM) cells, including INA6, RPMI-8226, U266, and RPMI-Dox40, LY2228820 (200 nM–800 nM) significantly blocks p38MAPK signaling, as revealed by its inhibition on phosphorylation of HSP27, a downstream target of p38MAPK, without affecting the expression level of HSP27. LY2228820 (200 nM–400 nM) enhances bortezomib-induced cytotoxicity and apoptosis, but LY2228820 alone doesn't inhibit the growth of MM.1S cells. LY2228820 (200 nM–800 nM) also inhibits secretion of IL-6 and MIP-1α in long-term BM stromal cells (LT-BMSCs), BM mononuclear cells (BMMNCs), peripheral blood (PB) CD138+, CD138 or PB CD14+ cells. LY2228820 (400 nM–800 nM) also blocks osteoclastogenesis from CD14+ cells. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RPMI-8226 NFnNc2pMcW6jc3WgZZN{[Xl? MonFglgxOCCwTR?= NH7TPGpFVVOR MXzpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? NWPjZlh5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizPVc{PDVpPkG4N|k4OzR3PD;hQi=>
U266 M1O3VmtqdmG|ZTDhd5NigQ>? Mo\HglgxOCCwTR?= NHOwcYdFVVOR MYTpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? NESxdnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO5O|M1PSd-MUizPVc{PDV:L3G+
MM.1S M13pZWtqdmG|ZTDhd5NigQ>? NH3E[WV,QDByIH7N M3TSZWROW09? NFTGNlNqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= NFrISHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO5O|M1PSd-MUizPVc{PDV:L3G+
RPMI-Dox40 MV7LbY5ie2ViYYPzZZk> NHLZZpR,QDByIH7N M4rUSmROW09? M1TDVYlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= MnfqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|OUezOFUoRjF6M{m3N|Q2RC:jPh?=
RPMI-LR5 NHrSfHBMcW6jc3WgZZN{[Xl? MVj+PFAxKG6P NFPTd2tFVVOR M{\LZYlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= NGPsWpE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO5O|M1PSd-MUizPVc{PDV:L3G+
INA-6 NX;hV|huU2mwYYPlJIF{e2G7 NHXqRlh,QDByIH7N MVXEUXNQ MU\pcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDN7N{O0OUc,OTh|OUezOFU9N2F-
RPMI-8226 MWDDfZRwgGmlaYT5JIF{e2G7 MnfPglExODBibl2= MYjEUXNQ MVHuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= M2XSWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{m3N|Q2Lz5zOEO5O|M1PTxxYU6=
U266 NVyzUIZQS3m2b4jpZ4l1gSCjc4PhfS=> MmWxglExODBibl2= M{LDSWROW09? MVLuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDN7N{O0OUc,OTh|OUezOFU9N2F-
MM.1S M2PuR2N6fG:6aXPpeJkh[XO|YYm= MYj+NVAxOCCwTR?= NXXY[I03TE2VTx?= NXzjdpZmdm9ic3nncolncWOjboSgZ5l1d3SxeHnjbZR6 M3XS[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{m3N|Q2Lz5zOEO5O|M1PTxxYU6=
RPMI-Dox40 MlXMR5l1d3irY3n0fUBie3OjeR?= M1zudp4yODByIH7N NYTvTXBwTE2VTx?= NGPHVVJvdyC|aXfubYZq[2GwdDDjfZRwfG:6aXPpeJk> Ml[1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|OUezOFUoRjF6M{m3N|Q2RC:jPh?=
RPMI-LR5 M{DiN2N6fG:6aXPpeJkh[XO|YYm= M2TtfJ4yODByIH7N MVzEUXNQ NXu1bHVmdm9ic3nncolncWOjboSgZ5l1d3SxeHnjbZR6 MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDN7N{O0OUc,OTh|OUezOFU9N2F-
INA-6 NV3Tcld6S3m2b4jpZ4l1gSCjc4PhfS=> MkHNglExODBibl2= M2DqcWROW09? M2njWY5wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> M{fKXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{m3N|Q2Lz5zOEO5O|M1PTxxYU6=
CD14+ NI\vXmRHfW6ldHnvckBie3OjeR?= MX;+PFAxKG6P NHHu[XZFVVOR MljibY5pcWKrdIOgc5N1\W:lbHHzeI9o\W6nc3nzJIZzd21iQ1SxOEBxd3OrdHn2[UBk\Wyucx?= NWTWfYdORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizPVc{PDVpPkG4N|k4OzR3PD;hQi=>
U-87-MG NUXMXodHTnWwY4Tpc44h[XO|YYm= MmTsNUDPxE1? Mm\WSG1UVw>? NFzHcFdz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> NIDuWlA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OzOVUxPid-MkOzN|U2ODZ:L3G+
MDA-MB-231 NFGzTI1HfW6ldHnvckBie3OjeR?= NVz5bolXOSEQvF2= NH[2XJVFVVOR NFfLVHBz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN|NUWwOkc,OjN|M{W1NFY9N2F-
A-2780 NXfMZplDTnWwY4Tpc44h[XO|YYm= NH3k[5gyKM7:TR?= NWXxU2VWTE2VTx?= M2q1d5Jm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u NWLlbIVWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzN|U2ODZpPkKzN|M2PTB4PD;hQi=>
SK-OV-3 M3fWemZ2dmO2aX;uJIF{e2G7 MkXNNUDPxE1? NUDE[IZQTE2VTx?= M1jkUJJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u M2TGPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{O1OVA3Lz5{M{OzOVUxPjxxYU6=
LXFA-629 MWTGeY5kfGmxbjDhd5NigQ>? Mom4NUDPxE1? NIDNXmhFVVOR NVLRXWJyemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN|NUWwOkc,OjN|M{W1NFY9N2F-
NCI-H1650 M4fuUGZ2dmO2aX;uJIF{e2G7 NHX3UJUyKM7:TR?= M1vhTGROW09? MkPodoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= NXfLfHpHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzN|U2ODZpPkKzN|M2PTB4PD;hQi=>
PC-3 NIDoSYZHfW6ldHnvckBie3OjeR?= MVmxJO69VQ>? MkDOSG1UVw>? NGjpd3Zz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> Mo\GQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|M{W1NFYoRjJ|M{O1OVA3RC:jPh?=
RAW264.7 M1q2Z2Z2dmO2aX;uJIF{e2G7 MWf+NlAh|ryP M4TUb2ROW09? MX3pcohq[mm2czDBcol{d227Y3nuMZN1cW23bHH0[YQhVUt{IIDoc5NxcG:{eXzheIlwdiC5aYToJGlEPTBib3[gN|UvOyCwTR?= MnL0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NU[4NVQoRjJ2M{W2PFE1RC:jPh?=
mouse peritoneal macrophages M4jNTmZ2dmO2aX;uJIF{e2G7 M3H4bp4zOCEQvF2= NFzLZYlFVVOR NFf2ZnFNWFNxSV\OMe6{6oDVc4TpcZVt[XSnZDDUUmYu|rFicILv[JVkfGmxbjD3bZRpKEmFNUCgc4YhPi5|IH7N M3TmZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2M{W2PFE1Lz5{NEO1OlgyPDxxYU6=
A549 M1qxOGZ2dmO2aX;uJIF{e2G7 MoTCglIxKM7:TR?= NHXPO5lFVVOR NYC3RWZxcW6qaXLpeJMhVFCVLXnu[JVk\WRiQ2jDUFgheHKxZIXjeIlwdiC5aYToJGlEPTBib3[gNVQ1Njlibl2= NFH2XXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO1OlgyPCd-MkSzOVY5OTR:L3G+
MDA-231 NILwNZRHfW6ldHnvckBie3OjeR?= M{\wXZ4yOCEQvF2= Mk\Hd5VxeHKnc4Pld{BFU0tvMTDlfJBz\XO|aX;u MkLOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ2MEe4OFMoRjJ4NEC3PFQ{RC:jPh?=
MCF-7 MoGxSpVv[3Srb36gZZN{[Xl? MXT+NVAh|ryP M1jS[5N2eHC{ZYPz[ZMhTEuNLUGg[ZhxemW|c3nvci=> M1[5UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NEC3PFQ{Lz5{NkSwO|g1OzxxYU6=
MDA-435 NXi1Rot5TnWwY4Tpc44h[XO|YYm= NIDwbG9,OTBizszN Mnnud5VxeHKnc4Pld{BFU0tvMTDlfJBz\XO|aX;u NGXjS2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkSwO|g1Oyd-Mk[0NFc5PDN:L3G+
PC3 MnrtSpVv[3Srb36gZZN{[Xl? MUD+NVAh|ryP MXvEUXNQ M3LmS5N2eHC{ZYPz[ZMhTEuNLUGg[ZhxemW|c3nvci=> NVrvdWd{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[5NVM3ODhpPkK2PVE{PjB6PD;hQi=>
TC32 M1XPbpFJXFNiYYPzZZk> M{\GTZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCWQ{OyJINmdGy| NGrpOW09[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
A673 MnHEdWhVWyCjc4PhfS=> MX\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? NHP6NpM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
DAOY MnHXdWhVWyCjc4PhfS=> NEToU5ZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiRFHPXUBk\Wyucx?= MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-37 NXTzOZBneUiWUzDhd5NigQ>? NELqNIpyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN|ch[2WubIO= MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
RD NHHJfGlyUFSVIHHzd4F6 NH;LfGZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN? M4S1bFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-12 MmXhdWhVWyCjc4PhfS=> NHTERYNyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStNVIh[2WubIO= MkfKQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB1643 M2LMVJFJXFNiYYPzZZk> NIq1cVZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz M{S3RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50 NWHOS45VeUiWUzDhd5NigQ>? NGP3SotyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz MlrqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh41 NXvaepRneUiWUzDhd5NigQ>? M{LDXpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaESxJINmdGy| M1LVe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh30 NGTJOZByUFSVIHHzd4F6 M3\HRpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEOwJINmdGy| M1;wNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Assay
Methods Test Index PMID
Western blot p-p38 / p38α / p38β / p-MK2 / MK2 / p-HSP27 / HSP27 ; p-S6K 23335506 26844273
In vivo In LPS-induced mice, LY2228820 effectively inhibits the formation of TNFα with a threshold minimum 50% effective dose (TMED50) less than 1 mg/kg. In a rat model of collagen-inducedarthritis (CIA), LY2228820 displays potent effects on paw swelling, bone erosion, and cartilage destruction, with a threshold minimum 50% effective dose (TMED50)of 1.5 mg/kg. [1]

Protocol (from reference)

Kinase Assay:[1]
  • Inhibition of p38α:

    Inhibition of p38α is determined using recombinant human p38α in a standard filter binding protocol using ATP[γ-33P] and EGFR 21-mer peptide as substrate. Functional inhibition of TNFα in murine peritoneal macrophages is determined using LPS stimulation in the presence of LY2228820. To assess p38α activity in cells more directly, RAW 264.7 cells are treated with LY2228820 and then stimulated with anisomycin. The level of p38α activity is detected using a phosphoMAPKAPK-2 (pMK2) (Thr 334) antibody which reacts with a residue specifically phosphorylated by p38α.

Cell Research:[2, 3]
  • Cell lines: MM cells, including INA6, RPMI-8226, U266, and RPMI-Dox40
  • Concentrations: 200 nM–800 nM
  • Incubation Time: 48 hours
  • Method: MTT assays and APO 2.7 staining are performed to assess cellular proliferation and induction of apoptosis, respectively. Viability is expressed as percent viable cells. Apoptosis in cells is evaluated by APO 2.7 staining. For detection of mitochondrial membrane protein 7A6 expressed in apoptotic cells, cells are incubated with APO 2.7 reagent for 20 min. Expression of APO 2.7 is determined using an EPICS XL flow cytometer.
  • (Only for Reference)
Animal Research:[1]
  • Animal Models: Lipopolysaccharide (LPS)-induced Balb/c mice
  • Dosages: 0–20 mg/kg
  • Administration: Oral bid dosing for 14 days
  • (Only for Reference)

Solubility (25°C)

In vitro

Water 100 mg/mL warmed
(163.2 mM)
DMSO 4 mg/mL warmed
(6.52 mM)
Ethanol '3 mg/mL

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
Saline
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

Molecular Weight 612.74
Formula

C24H29FN6.2CH4O3S

CAS No. 862507-23-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)(C)CN1C2=C(C=CC(=N2)C3=C(N=C(N3)C(C)(C)C)C4=CC=C(C=C4)F)N=C1N.CS(=O)(=O)O.CS(=O)(=O)O

In vivo Formulation Calculator (Clear solution)

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

mg/kg g μL

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

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02860780 Completed Drug: prexasertib|Drug: ralimetinib Advanced Cancer|Metastatic Cancer|Colorectal Cancer|Non-small Cell Lung Cancer Eli Lilly and Company August 10 2016 Phase 1
NCT02364206 Completed Drug: LY2228820|Drug: Temozolomide|Radiation: radiotherapy Adult Glioblastoma Centre Jean Perrin|National Cancer Institute France|ARC Foundation for Cancer Research June 8 2015 Phase 1|Phase 2
NCT02322853 Terminated Drug: Tamoxifen|Drug: Ralimetinib (LY2228820 dimesylate) Postmenopausal|Metastatic Breast Cancer Centre Francois Baclesse|National Cancer Institute France|ARC Foundation for Cancer Research January 2015 Phase 2
NCT01393990 Completed Drug: LY2228820|Drug: Midazolam|Drug: Tamoxifen Advanced Cancer Eli Lilly and Company September 4 2008 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

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