Ralimetinib (LY2228820) dimesylate

For research use only. Not for use in humans.

目录号:S1494

Ralimetinib (LY2228820) dimesylate Chemical Structure

CAS No. 862507-23-1

Ralimetinib (LY2228820) dimesylate 是一种新型有效的p38 MAPK抑制剂,无细胞试验中IC50为7 nM,不改变p38 MAPK的活化。Phase 1/2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2344.86 现货
RMB 1403.05 现货
RMB 7927.27 现货
有超大折扣

今日订购,明日送达,全国免运费!

全国免费电话:400-668-6834   |   Email:info@selleck.cn

客户使用Selleck生产的Ralimetinib (LY2228820) dimesylate发表文献59篇:

产品安全说明书

p38 MAPK抑制剂选择性比较

生物活性

产品描述 Ralimetinib (LY2228820) dimesylate 是一种新型有效的p38 MAPK抑制剂,无细胞试验中IC50为7 nM,不改变p38 MAPK的活化。Phase 1/2。
特性 LY2228820是新型有效的p38有丝分裂原活化蛋白激酶(MAPK)通路抑制剂。
靶点
p38α [1]
(Cell-free assay)
7 nM
体外研究

LY2228820作用于RAW 264.7细胞,抑制p38α,和磷酸MAPKAPK-2(pMK2)水平,IC50分别为7 nM 和 34.3 nM。而且, LY2228820作用于小鼠腹腔巨噬细胞,抑制脂多糖 (LPS)-诱导的TNFα形成, IC50为5.2 nM。[1] 200 nM-800 nM LY2228820作用于多发性骨髓瘤(MM)细胞, 包括INA6, RPMI-8226, U266, 和RPMI-Dox40,通过抑制HSP27磷酸化而显著抑制p38MAPK信号, HSP27是p38MAPK下游靶点,不影响 HSP27表达水平。200 nM-400 nM LY2228820增强Bortezomib诱导的细胞毒性和凋亡, 但是LY2228820 单独处理不会抑制MM.1S细胞生长。200 nM-800 nM LY2228820作用于长期骨髓基质干细胞(LT-BMSCs),骨髓单个核细胞(BMMNCs),外周血(PB)CD138+,CD138-或外周血(PB)CD14+细胞,也抑制IL-6和MIP-1α分泌。400 nM-800 nM LY2228820也抑制CD14+ 细胞形成破骨细胞。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RPMI-8226 NHG4XIJMcW6jc3WgZZN{[Xl? NInaN2N,QDByIH7N NFr2b|JFVVOR MkHUbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 M3TqTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{m3N|Q2Lz5zOEO5O|M1PTxxYU6=
U266 MWHLbY5ie2ViYYPzZZk> MXP+PFAxKG6P NGnCPWpFVVOR M3\LeIlvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= NXjGPGlDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizPVc{PDVpPkG4N|k4OzR3PD;hQi=>
MM.1S MV7LbY5ie2ViYYPzZZk> M2\4dp45ODBibl2= MVrEUXNQ M4nwOolvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= NVLpXnUxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizPVc{PDVpPkG4N|k4OzR3PD;hQi=>
RPMI-Dox40 MkDvT4lv[XOnIHHzd4F6 M1vsUZ45ODBibl2= MYLEUXNQ NGjTUm5qdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= NF;l[Gc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO5O|M1PSd-MUizPVc{PDV:L3G+
RPMI-LR5 NFX5NIpMcW6jc3WgZZN{[Xl? NIDmeXd,QDByIH7N NFjaUnhFVVOR MnrFbY5pcWKrdIOgdIhwe3Cqb4L5cIF1cW:wIH;mJGhUWDJ5 NYWwZ2FYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizPVc{PDVpPkG4N|k4OzR3PD;hQi=>
INA-6 NEjveYlMcW6jc3WgZZN{[Xl? MoSyglgxOCCwTR?= NUXCbY9FTE2VTx?= M3fnc4lvcGmkaYTzJJBpd3OyaH;yfYxifGmxbjDv[kBJW1B{Nx?= M4jWdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{m3N|Q2Lz5zOEO5O|M1PTxxYU6=
RPMI-8226 MlrER5l1d3irY3n0fUBie3OjeR?= M4PPXJ4yODByIH7N MmjoSG1UVw>? MYruc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= MmCyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|OUezOFUoRjF6M{m3N|Q2RC:jPh?=
U266 M336[mN6fG:6aXPpeJkh[XO|YYm= NVLKeodPhjFyMECgcm0> MWnEUXNQ M{HNVI5wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> MkD6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|OUezOFUoRjF6M{m3N|Q2RC:jPh?=
MM.1S M4HsVWN6fG:6aXPpeJkh[XO|YYm= NUPDPGllhjFyMECgcm0> MnTJSG1UVw>? M4LZ[45wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> NETuUGQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO5O|M1PSd-MUizPVc{PDV:L3G+
RPMI-Dox40 NYq0c|BRS3m2b4jpZ4l1gSCjc4PhfS=> M1P0W54yODByIH7N NHzqNXBFVVOR Mortco8he2mpbnnmbYNidnRiY4n0c5RwgGmlaYT5 Ml3PQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|OUezOFUoRjF6M{m3N|Q2RC:jPh?=
RPMI-LR5 NHnCfItEgXSxeHnjbZR6KGG|c3H5 M{HZdZ4yODByIH7N MkDWSG1UVw>? MYjuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= M{e1b|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{m3N|Q2Lz5zOEO5O|M1PTxxYU6=
INA-6 MmP4R5l1d3irY3n0fUBie3OjeR?= NIm3blZ,OTByMDDuUS=> NEDW[ZBFVVOR NFnXUYFvdyC|aXfubYZq[2GwdDDjfZRwfG:6aXPpeJk> MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDN7N{O0OUc,OTh|OUezOFU9N2F-
CD14+ M1roSmZ2dmO2aX;uJIF{e2G7 NUHJdpBRhjhyMDDuUS=> NU\VWXZ1TE2VTx?= MXnpcohq[mm2czDvd5Rmd2OuYYP0c4dmdmW|aYOg[pJwdSCFREG0JJBwe2m2aY\lJINmdGy| NHvhSGo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO5O|M1PSd-MUizPVc{PDV:L3G+
U-87-MG M1jlN2Z2dmO2aX;uJIF{e2G7 MYqxJO69VQ>? NGK2XZRFVVOR NWLXc3AyemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN|NUWwOkc,OjN|M{W1NFY9N2F-
MDA-MB-231 NID2PY9HfW6ldHnvckBie3OjeR?= Mme3NUDPxE1? NHLCUFhFVVOR NHLsWVlz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> M4nEe|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{O1OVA3Lz5{M{OzOVUxPjxxYU6=
A-2780 MWXGeY5kfGmxbjDhd5NigQ>? MnmyNUDPxE1? MWTEUXNQ MUny[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= NGG2PGI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OzOVUxPid-MkOzN|U2ODZ:L3G+
SK-OV-3 NHTqVW1HfW6ldHnvckBie3OjeR?= MYCxJO69VQ>? NXTMcow2TE2VTx?= MmfPdoVlfWOnczD0eY1wei2mcnn2[Y4h[2:{ZDDmc5Ju[XSrb36= NIPBO3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OzOVUxPid-MkOzN|U2ODZ:L3G+
LXFA-629 MlixSpVv[3Srb36gZZN{[Xl? NEOwZ48yKM7:TR?= NInvRZlFVVOR NFPpRmhz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN|NUWwOkc,OjN|M{W1NFY9N2F-
NCI-H1650 MVzGeY5kfGmxbjDhd5NigQ>? MknENUDPxE1? NYLWXnRyTE2VTx?= NHnGUFBz\WS3Y3XzJJR2dW:{LXTybZZmdiClb4LkJIZwem2jdHnvci=> MmDlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|M{W1NFYoRjJ|M{O1OVA3RC:jPh?=
PC-3 Ml3sSpVv[3Srb36gZZN{[Xl? M33kdVEh|ryP NIr6fHRFVVOR MXny[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN|NUWwOkc,OjN|M{W1NFY9N2F-
RAW264.7 M4fPcGZ2dmO2aX;uJIF{e2G7 M3ntPZ4zOCEQvF2= NHPNe|ZFVVOR NIjm[W9qdmirYnn0d{BCdmm|b335Z4lvNXO2aX31cIF1\WRiTVuyJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOzVwMzDuUS=> NGTWXJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEO1OlgyPCd-MkSzOVY5OTR:L3G+
mouse peritoneal macrophages MX;GeY5kfGmxbjDhd5NigQ>? MYT+NlAh|ryP M4juT2ROW09? NHi4UXBNWFNxSV\OMe6{6oDVc4TpcZVt[XSnZDDUUmYu|rFicILv[JVkfGmxbjD3bZRpKEmFNUCgc4YhPi5|IH7N MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN3NkixOEc,OjR|NU[4NVQ9N2F-
A549 MonzSpVv[3Srb36gZZN{[Xl? NIP0VWJ,OjBizszN MUXEUXNQ MmrUbY5pcWKrdIOgUHBUNWmwZIXj[YQhS1iFTEigdJJw\HWldHnvckB4cXSqIFnDOVAhd2ZiMUS0Mlkhdk1? MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN3NkixOEc,OjR|NU[4NVQ9N2F-
MDA-231 M1y2Z2Z2dmO2aX;uJIF{e2G7 MYP+NVAh|ryP M3vNfJN2eHC{ZYPz[ZMhTEuNLUGg[ZhxemW|c3nvci=> NUXO[2Y5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0NFc5PDNpPkK2OFA4QDR|PD;hQi=>
MCF-7 MoP6SpVv[3Srb36gZZN{[Xl? NUDP[5JGhjFyIN88US=> MYHzeZBxemW|c3XzJGRMUy1zIHX4dJJme3Orb36= NW\XV5VpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[0NFc5PDNpPkK2OFA4QDR|PD;hQi=>
MDA-435 M3Hje2Z2dmO2aX;uJIF{e2G7 NEfTfYJ,OTBizszN NGW5[pF{fXCycnXzd4V{KESNSz2xJIV5eHKnc4Ppc44> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjRyN{i0N{c,OjZ2MEe4OFM9N2F-
PC3 MljqSpVv[3Srb36gZZN{[Xl? MXL+NVAh|ryP MYrEUXNQ NFGzdZh{fXCycnXzd4V{KESNSz2xJIV5eHKnc4Ppc44> MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjlzM{[wPEc,OjZ7MUO2NFg9N2F-
TC32 MnLwdWhVWyCjc4PhfS=> M33EW5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCWQ{OyJINmdGy| M4rRTVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A673 NW\Q[mF6eUiWUzDhd5NigQ>? NYnxflJweUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
DAOY M1rHZ5FJXFNiYYPzZZk> MoDqdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKESDT2mgZ4VtdHN? NVTPWZRFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37 MkHrdWhVWyCjc4PhfS=> MWnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvM{egZ4VtdHN? MlvWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
RD M3HGd5FJXFNiYYPzZZk> MlnSdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{ MljiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-12 M{nHTZFJXFNiYYPzZZk> Ml7DdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB1643 NHuxcVRyUFSVIHHzd4F6 MljGdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= MnzvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 MY\xTHRUKGG|c3H5 NI\RUVRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh41 M3vkOpFJXFNiYYPzZZk> MYLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>? MlTxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh30 M3rZT5FJXFNiYYPzZZk> MmPCdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqM{CgZ4VtdHN? M1PH[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-p38 / p38α / p38β / p-MK2 / MK2 / p-HSP27 / HSP27; 

PubMed: 23335506     


whole cell protein extracts were isolated from ECFCs or ADSCs following pretreatment with DMSO (−) or 1 μm LY2228820 dimesylate (+) for 30 min prior to the addition of 10 ng/ml VEGF, bFGF, EGF, or 100 ng/ml IL-6, and then the extracts were subjected to Western blot analysis using antisera directed against p-p38, p38α, p38β, p-MK2, total MK2, p-HSP27, total HSP27, and β-actin as a loading control.

p-S6K ; 

PubMed: 26844273     


CRC cells were treated with 4 μM LY2228820, 10 μM BIRB796 or 10 μM SB202190 for 2 h and p38 and mTORC1 signaling was analyzed by immunoblot.

23335506 26844273
体内研究 LY2228820 作用于LPS诱导的小鼠,有效抑制TNFα 形成,半数有效剂量最小阈值 (TMED 50)小于1 mg/kg。LY2228820 作用于患胶原性关节炎(CIA)大鼠模型,有效作用于足肿胀, 骨质糜烂, 和软骨破坏, 半数有效剂量最小阈值(TMED50)为 1.5 mg/kg。[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

激酶实验:[1]
- 合并

抑制p38α实验:

使用重组人p38α 在标准过滤器中使用ATP[γ-33P] 和EGFR 21肽底物测定抑制p38α的效果。在LY2228820存在时,使用LPS刺激,在小鼠腹腔巨噬细胞测定抑制TNFα效果。在使用LY2228820处理,然后用Anisomycin刺激的RAW 264.7细胞中测定p38α活性。使用磷酸MAPKAPK-2(pMK2)(Thr 334)抗体测定p38α活性水平。
细胞实验: [2]
- 合并
  • Cell lines: MM细胞,包括 INA6, RPMI-8226, U266,和RPMI-Dox40
  • Concentrations: 200 nM-800 nM
  • Incubation Time: 48小时
  • Method: 进行MTT实验和APO 2.7 染色分别测定细胞增殖和凋亡诱导。测定活细胞百分数作为可活力。通过APO 2.7染色测定凋亡。为了测定凋亡细胞中线粒体膜蛋白7A6的表达,用APO 2.7试剂处理细胞20分钟。使用EPICS XL流式细胞仪测定APO 2.7的表达。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 脂多糖(LPS)-诱导的Balb/c小鼠
  • Dosages: 0-20 mg/kg
  • Administration: 口服处理,每天两次,持续14天
    (Only for Reference)

溶解度 (25°C)

体外 Water 100 mg/mL warmed (163.2 mM)
DMSO 4 mg/mL warmed (6.52 mM)
Ethanol '3 mg/mL
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
Saline
30 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 612.74
化学式

C24H29FN6.2CH4O3S

CAS号 862507-23-1
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

p38 MAPK Signaling Pathway Map

p38 MAPK Inhibitors with Unique Features

相关p38 MAPK产品

Tags: 购买Ralimetinib (LY2228820) dimesylate | Ralimetinib (LY2228820) dimesylate供应商 | 采购Ralimetinib (LY2228820) dimesylate | Ralimetinib (LY2228820) dimesylate价格 | Ralimetinib (LY2228820) dimesylate生产 | 订购Ralimetinib (LY2228820) dimesylate | Ralimetinib (LY2228820) dimesylate代理商
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID