Ralimetinib (LY2228820) dimesylate

目录号:S1494

仅限科研使用

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。

Ralimetinib (LY2228820) dimesylate Chemical Structure

CAS: 862507-23-1

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
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客户使用Selleck生产的Ralimetinib (LY2228820) dimesylate发表文献60篇:

产品安全说明书

p38 MAPK抑制剂选择性比较

相关p38 MAPK产品

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 NWPMdJQ2U2mwYYPlJIF{e2G7 NHrTZZd,QDByIH7N NV;ufHlITE2VTx?= NFvMNJdqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= NVPHUVdqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizPVc{PDVpPkG4N|k4OzR3PD;hQi=>
U266 NHrobpRMcW6jc3WgZZN{[Xl? M{DkRZ45ODBibl2= MUPEUXNQ MXrpcohq[mm2czDwbI9{eGixconsZZRqd25ib3[gTHNROjd? MlLRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|OUezOFUoRjF6M{m3N|Q2RC:jPh?=
MM.1S NXTnNmNZU2mwYYPlJIF{e2G7 MmC5glgxOCCwTR?= NXSw[W0zTE2VTx?= NET3W4FqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= NXfBbY5[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizPVc{PDVpPkG4N|k4OzR3PD;hQi=>
RPMI-Dox40 NXLWcoptU2mwYYPlJIF{e2G7 MmfmglgxOCCwTR?= NE[3[41FVVOR NGfqNVlqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDN7N{O0OUc,OTh|OUezOFU9N2F-
RPMI-LR5 NFjTNWhMcW6jc3WgZZN{[Xl? MWT+PFAxKG6P MX;EUXNQ NHrC[FNqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDN7N{O0OUc,OTh|OUezOFU9N2F-
INA-6 NHvKb4RMcW6jc3WgZZN{[Xl? Mn\1glgxOCCwTR?= MW\EUXNQ NE\FSpFqdmirYnn0d{BxcG:|cHjvdplt[XSrb36gc4YhUFOSMke= NI\HW3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO5O|M1PSd-MUizPVc{PDV:L3G+
RPMI-8226 NWfHbm1TS3m2b4jpZ4l1gSCjc4PhfS=> MVj+NVAxOCCwTR?= MkDTSG1UVw>? M1vwNI5wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> MnvYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|OUezOFUoRjF6M{m3N|Q2RC:jPh?=
U266 MX7DfZRwgGmlaYT5JIF{e2G7 MnXsglExODBibl2= NWXIc5BiTE2VTx?= NYLSZ3BOdm9ic3nncolncWOjboSgZ5l1d3SxeHnjbZR6 MlLDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh|OUezOFUoRjF6M{m3N|Q2RC:jPh?=
MM.1S NXn4c5pqS3m2b4jpZ4l1gSCjc4PhfS=> MYT+NVAxOCCwTR?= NYPCNXZSTE2VTx?= MYLuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= NGH5V|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO5O|M1PSd-MUizPVc{PDV:L3G+
RPMI-Dox40 NHfEfHJEgXSxeHnjbZR6KGG|c3H5 MlviglExODBibl2= MV3EUXNQ MVnuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= NIDBN209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEO5O|M1PSd-MUizPVc{PDV:L3G+
RPMI-LR5 M3;iZ2N6fG:6aXPpeJkh[XO|YYm= M1zlep4yODByIH7N MUfEUXNQ MXLuc{B{cWewaX\pZ4FvfCCleYTveI95cWOrdIm= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDN7N{O0OUc,OTh|OUezOFU9N2F-
INA-6 MoLjR5l1d3irY3n0fUBie3OjeR?= NVjYWYZ2hjFyMECgcm0> M37wcGROW09? M33Nfo5wKHOrZ37p[olk[W62IHP5eI91d3irY3n0fS=> NWPZWJJXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizPVc{PDVpPkG4N|k4OzR3PD;hQi=>
CD14+ NFq4[VdHfW6ldHnvckBie3OjeR?= MYX+PFAxKG6P NVjvblJ1TE2VTx?= MXXpcohq[mm2czDvd5Rmd2OuYYP0c4dmdmW|aYOg[pJwdSCFREG0JJBwe2m2aY\lJINmdGy| NUnHXW9TRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizPVc{PDVpPkG4N|k4OzR3PD;hQi=>
U-87-MG NVT3UnBJTnWwY4Tpc44h[XO|YYm= NUTHN4JwOSEQvF2= Mnq2SG1UVw>? NXG1b4FIemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> NEfqW4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{OzOVUxPid-MkOzN|U2ODZ:L3G+
MDA-MB-231 NILzN3NHfW6ldHnvckBie3OjeR?= NH;1cIQyKM7:TR?= MVfEUXNQ M4XFOpJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u MmHEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN|M{W1NFYoRjJ|M{O1OVA3RC:jPh?=
A-2780 NYnIT4ZtTnWwY4Tpc44h[XO|YYm= NWmwPHduOSEQvF2= M134b2ROW09? NVnHXFZxemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> MV[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN|NUWwOkc,OjN|M{W1NFY9N2F-
SK-OV-3 NEHoPGdHfW6ldHnvckBie3OjeR?= MXuxJO69VQ>? M3zRfWROW09? NWDpRYRYemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN|NUWwOkc,OjN|M{W1NFY9N2F-
LXFA-629 NUD6emt{TnWwY4Tpc44h[XO|YYm= MkPINUDPxE1? NV;MelJFTE2VTx?= NUfJVIVGemWmdXPld{B1fW2xcj3kdol3\W5iY3;y[EBnd3KvYYTpc44> MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzN|NUWwOkc,OjN|M{W1NFY9N2F-
NCI-H1650 NGfjNXlHfW6ldHnvckBie3OjeR?= M3\KOVEh|ryP MkXSSG1UVw>? MXny[YR2[2W|IIT1cY9zNWS{aY\lckBkd3KmIH\vdo1ifGmxbh?= NWTRbWJkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzN|U2ODZpPkKzN|M2PTB4PD;hQi=>
PC-3 NEnzOopHfW6ldHnvckBie3OjeR?= MmqzNUDPxE1? NI\ZfJNFVVOR M{\0[JJm\HWlZYOgeJVud3JvZILpeoVvKGOxcnSg[o9zdWG2aX;u NWm0cot3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOzN|U2ODZpPkKzN|M2PTB4PD;hQi=>
RAW264.7 M1HoPWZ2dmO2aX;uJIF{e2G7 NWHoUFY1hjJyIN88US=> M3PDbWROW09? NGnZUpdqdmirYnn0d{BCdmm|b335Z4lvNXO2aX31cIF1\WRiTVuyJJBpd3OyaH;yfYxifGmxbjD3bZRpKEmFNUCgc4YhOzVwMzDuUS=> MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN3NkixOEc,OjR|NU[4NVQ9N2F-
mouse peritoneal macrophages NGPYcYRHfW6ldHnvckBie3OjeR?= NFzrSXp,OjBizszN MkTvSG1UVw>? NHHsUYlNWFNxSV\OMe6{6oDVc4TpcZVt[XSnZDDUUmYu|rFicILv[JVkfGmxbjD3bZRpKEmFNUCgc4YhPi5|IH7N MoH0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR|NU[4NVQoRjJ2M{W2PFE1RC:jPh?=
A549 M3y0VWZ2dmO2aX;uJIF{e2G7 NETPVox,OjBizszN MnnRSG1UVw>? MWjpcohq[mm2czDMVHMucW6mdXPl[EBEYEOOODDwdo9lfWO2aX;uJJdqfGhiSVO1NEBw\iBzNESuPUBvVQ>? MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDN3NkixOEc,OjR|NU[4NVQ9N2F-
MDA-231 MUXGeY5kfGmxbjDhd5NigQ>? MkP4glExKM7:TR?= NUnXS5Zne3WycILld5NmeyCGS1utNUBmgHC{ZYPzbY9v NETuWYo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkSwO|g1Oyd-Mk[0NFc5PDN:L3G+
MCF-7 NYfGfZVjTnWwY4Tpc44h[XO|YYm= NGD5Xm5,OTBizszN M37YbJN2eHC{ZYPz[ZMhTEuNLUGg[ZhxemW|c3nvci=> M3\CW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4NEC3PFQ{Lz5{NkSwO|g1OzxxYU6=
MDA-435 MWPGeY5kfGmxbjDhd5NigQ>? NF3COFB,OTBizszN MYLzeZBxemW|c3XzJGRMUy1zIHX4dJJme3Orb36= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjRyN{i0N{c,OjZ2MEe4OFM9N2F-
PC3 NFWwUmVHfW6ldHnvckBie3OjeR?= MXT+NVAh|ryP NF\yeGRFVVOR M2LKPJN2eHC{ZYPz[ZMhTEuNLUGg[ZhxemW|c3nvci=> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjlzM{[wPEc,OjZ7MUO2NFg9N2F-
TC32 NFr6RVhyUFSVIHHzd4F6 M1i3S5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCWQ{OyJINmdGy| MoXEQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
A673 MWPxTHRUKGG|c3H5 NGr2eIdyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= M4LLclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
DAOY M1XyVJFJXFNiYYPzZZk> NIewN4ZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiRFHPXUBk\Wyucx?= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-37 NEPE[XJyUFSVIHHzd4F6 M4HpbJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?= NEjlVpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
RD NV7lWFF7eUiWUzDhd5NigQ>? NH;tfIRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN? MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-12 M{fBU5FJXFNiYYPzZZk> Mn\QdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| MnPHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB1643 NUL1T4s3eUiWUzDhd5NigQ>? NF7lOJZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz M4TIWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50 NYD5cGdDeUiWUzDhd5NigQ>? NGftXGFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiT1jTMVUxKGOnbHzz NXG2TVNiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh41 NXi4UoFPeUiWUzDhd5NigQ>? M4j3O5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaESxJINmdGy| MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh30 NUDOcHdCeUiWUzDhd5NigQ>? MorldWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqM{CgZ4VtdHN? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Assay
Methods Test Index PMID
Western blot p-p38 / p38α / p38β / p-MK2 / MK2 / p-HSP27 / HSP27 p-S6K 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]
  • 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]
  • 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。
动物实验:[1]
  • 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

溶解度(25°C)

体外

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 3年 -20°C 粉状
2年 -80°C 溶于溶剂

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)

mg/kg g μL

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
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

摩尔浓度计算器

质量 浓度 体积 分子量

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

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

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