RAF265 (CHIR-265)

For research use only. Not for use in humans.

目录号:S2161

RAF265 (CHIR-265) Chemical Structure

CAS No. 927880-90-8

RAF265 (CHIR-265)是一种有效的选择性C-Raf/B-Raf/B-Raf V600E抑制剂,IC50为3-60 nM,对VEGFR2磷酸化表现出有效的抑制作用,无细胞试验中EC50为30 nM。RAF265 (CHIR-265)可诱导细胞周期阻滞和凋亡。Phase 2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1956.12 现货
RMB 1415.74 现货
RMB 2629.71 现货
RMB 4561.83 现货
RMB 13677.3 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RAF265 (CHIR-265)发表文献18篇:

客户使用该产品的4个实验数据:

  • Immunoblots showing levels of phospho-MEK (p-MEK), total MEK (t-MEK), phospho-ERK1/2 (p-ERK1/2) and total ERK1/2 (t-ERK1/2) in A375 cells transduced with a retrovirus expressing BRAFV600E, BRAFV600E/L505H, BRAFV600E/F516G or BRAFV600E/T529N and treated with increasing doses of RAF265. α-tubulin (TUBA) was monitored as a loading control.

    Pigment Cell Melanoma Res 2014 27(1), 124-33. RAF265 (CHIR-265) purchased from Selleck.

  • Raf265 inhibited the kinase activity of B-Raf but not of Raf-1 in Pkd2cKO cholangiocytes. Cells were treated for 30 min with different concentrations of Raf265. B-Raf and Raf-1 were immunoprecipated as described in the methods section and a kinase assay in vitro was performed using MEK as a substrate. The kinase activity of Raf was assessed by immunoblot analysis and quantified as optical density of pMEK with respect to untreated cells. In WT cholangiocytes (A) Raf265 inhibited both B-Raf and Raf-1 kinase activity. In Pkd2cKO cholangiocytes (B), Raf265 inhibited only B-Raf while a biphasic effect was found in Raf-1 with a significant increase at doses from 0.001 to 1 uM and a significant inhibition at 10 uM. Blots are representative of four different experiments. (*p<0.05 vs controls; **p<0.001 vs controls).

    Hepatology 2012 56(6), 2363-74. RAF265 (CHIR-265) purchased from Selleck.

  • LS513 cells were treated with increasing concentrations of selumetinib or selumetinib combined with different concentration of RAF265 for 48 hr. Lysates were subjected to western blot analyses, and membranes were probed with the indicated antibodies. Vinculin was included as a loading control.

    Cell Rep, 2014, 8(5):1475-83. RAF265 (CHIR-265) purchased from Selleck.

  • Wild-type fetal liver-derived cells were differentiated for 2 days in culture. Kinase inhibitors (A-674563 and RAF265; concentrations are listed in Materials and Methods) were added during the final 14 h of culture.

    Mol Cell Biol, 2016, 37(1). RAF265 (CHIR-265) purchased from Selleck.

产品安全说明书

Raf抑制剂选择性比较

生物活性

产品描述 RAF265 (CHIR-265)是一种有效的选择性C-Raf/B-Raf/B-Raf V600E抑制剂,IC50为3-60 nM,对VEGFR2磷酸化表现出有效的抑制作用,无细胞试验中EC50为30 nM。RAF265 (CHIR-265)可诱导细胞周期阻滞和凋亡。Phase 2。
特性 CHIR-265是有效的c-Raf/B-Raf/mutB-Raf选择性抑制剂,有效抑制含Ras/Raf 通路突变的肿瘤细胞增殖和存活,作用于一大批临床前期模型具有高效性。
靶点
VEGFR2 [1]
(Cell-free assay)
B-Raf [1]
(Cell-free assay)
30 nM(EC50) 3 nM-60 nM
体外研究

RAF265 是有效的新型BRAF/VEGFR-2抑制剂, 作用于A375M(V600EBRAF)人黑色素瘤细胞系,降低肿瘤糖代谢和FDG累积。RAF265抑制2-脱氧-2-[18F]氟代-D-葡萄糖(FDG)累积,这种作用存在剂量依赖性。 RAF265 显著调节糖代谢, 嘧啶代谢,和凋亡通路。RAF265抑制VEGF诱导的血管生成和突变BRAF, 血管生成通路和新的用于血管生成成像的新兴示踪剂将被用于评估双重作用机制的相对优势。[1]RAF265作用于HT29和 MDAMB231 细胞中的BRAF,具有显著活性,IC20为1到3 μM,IC50为5 到10 μM。使用浓度为1到10 μM RAF265 处理BRAF突变的细胞系,降低MEK磷酸化。 1 μM RAF265处理非 BRAF突变的细胞系,却提高MEK磷酸化, RAF265浓度达到 5 μM时可逆转这种变化。加入RAD001,增强RAF265作用于 HCT116细胞系的毒性。[2] RAF265处理,降低 pERK水平,这种作用存在剂量依赖性,0.5 mM RAF265 处理2小时后,完全阻断 G2-M期进展, 导致G2-M期细胞为0%。[3] RAF265抑制表达V600EBRAF的细胞生长,比作用于WTBRAF细胞选择性高14倍,比作用于对选择性 BRAF抑制剂不敏感的守卫-突变T529N, V600EBRAF细胞高7倍, 说明RAF265的细胞内靶点是BRAF。[4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SK-MEL-28 NUK2Wnc1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1rwOGdzd3e2aDDpcohq[mm2aX;uJI9nKFONLV3FUE0zQCClZXzsd{whUUN3ME2wMlE1|ryPLh?= M1eyWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzNUe2NFI{Lz5{MUW3OlAzOzxxYU6=
MALME-3M NGrLUXFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmDBS5Jwf3SqIHnubIljcXSrb36gc4YhVUGOTVWtN20h[2WubIOsJGlEPTB;MD6xOO69VS5? NHT2SFQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUW3OlAzOyd-MkG1O|YxOjN:L3G+
A375M MlH2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYfHdo94fGhiaX7obYJqfGmxbjDv[kBCOzd3TTDj[YxteyxiSVO1NF0xNjF2zszNMi=> MkDiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF3N{[wNlMoRjJzNUe2NFI{RC:jPh?=
A375 M1LXT2Z2dmO2aX;uJIF{e2G7 MYXJcohq[mm2aX;uJI9nKEJvUlHGJHY3ODCHIH31eIFvfCCrbjDoeY1idiCDM{e1JINmdGy|IHHzd4V{e2WmIHHzJJBpd3OyaH;yfYxifGmxbjDv[kBGWktuIFnDOVA:OC5yNN88UU4> M4LwVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{m2OlgyLz5{NkO5OlY5OTxxYU6=
Malme-3M MkDRSpVv[3Srb36gZZN{[Xl? M1XqS2lvcGmkaYTpc44hd2ZiQj3SRWYhXjZyMFWgcZV1[W62IHnuJIh2dWGwIF3hcI1mNTOPIHPlcIx{KGG|c3Xzd4VlKGG|IIDoc5NxcG:{eXzheIlwdiCxZjDFVmstKEmFNUC9NE4xPM7:TT6= NGDaPGs9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO5OlY5OSd-Mk[zPVY3QDF:L3G+
WM-1799 M131V2Z2dmO2aX;uJIF{e2G7 NEHidGNKdmirYnn0bY9vKG:oIFKtVmFHKFZ4MEDFJI12fGGwdDDpckBpfW2jbjDXUU0yPzl7IHPlcIx{KGG|c3Xzd4VlKGG|IIDoc5NxcG:{eXzheIlwdiCxZjDFVmstKEmFNUC9NE4xPM7:TT6= NFzU[HA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO5OlY5OSd-Mk[zPVY3QDF:L3G+
MALME-3M NWjPZ|YzSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MXTBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2DTF3FMVNOKGOnbHzzJIhiemKxcnnu[{BDNVKDRjDWOlAxTSCvdYThcpQtKEmFNUC9NE4xPM7:TT6= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN7Nk[4NUc,OjZ|OU[2PFE9N2F-
A375 MUXBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NXnlcZZISW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBN|c2KGOnbHzzJIhiemKxcnnu[{BDNVKDRjDWOlAxTSCvdYThcpQtKEmFNUC9NE4xPM7:TT6= NFeySlc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO5OlY5OSd-Mk[zPVY3QDF:L3G+
WM1799 M2nlcGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MmDkRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCZTUG3PVkh[2WubIOgbIFz[m:{aX7nJGIuWkGIIG[2NFBGKG23dHHueEwhUUN3ME2wMlA1|ryPLh?= MorrQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|OU[2PFEoRjJ4M{m2OlgyRC:jPh?=
SK-MEL-28 NFPh[|NHfW6ldHnvckBie3OjeR?= NIP1N45KdmirYnn0bY9vKG:oIFKtVmFHKFZ4MEDFJI12fGGwdDDpckBpfW2jbjDTT{1OTUxvMkigZ4VtdHNiYYPz[ZN{\WRiYYOgdIhwe3Cqb4L5cIF1cW:wIH;mJGVTUyxiSVO1NF0xNjF2zszNMi=> MmO4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|OU[2PFEoRjJ4M{m2OlgyRC:jPh?=
SK-MEL-28 NYHVVotKSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= M3z6TWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU1utUWVNNTJ6IHPlcIx{KGijcnLvdolv\yCELWLBSkBXPjByRTDteZRidnRuIFnDOVA:OC5zNt88UU4> NIOzWI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO5OlY5OSd-Mk[zPVY3QDF:L3G+
A375M MkjPSpVv[3Srb36gZZN{[Xl? NVL0enBIOTByIH3nM4to MV;mR41qdiCrbjDtc5V{\SC6ZX7v[5Ji\nSnZDD3bZRpKGi3bXHuJGE{PzWPIHPlcIx{KGG2IEGwNEBu\y:tZzygdI8heTKmLDDmR41qdj1yLkZOwG0v NEPPe4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO5OlY5OSd-Mk[zPVY3QDF:L3G+
A375M NWO3doQ3TnWwY4Tpc44h[XO|YYm= Mo[1NVAxKG2pL3vn NX\5[phsPDhiaILz MVPJcohq[mm2aX;uJI9nKEJvUlHGJHY3ODCHIH31eIFvfCCrbjDtc5V{\SC6ZX7v[5Ji\nSnZDD3bZRpKGi3bXHuJGE{PzWPIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBxcG:|cHjvMW1GUyCuZY\lcEBqdiC2dX3vdkBifCBzMECgcYcwc2duIIDvJJEzPCCjZoTldkA1QCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| MoTZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|OU[2PFEoRjJ4M{m2OlgyRC:jPh?=
A375M NXzMbnp1TnWwY4Tpc44h[XO|YYm= NWCwd|FHOTByIH3nM4to M17FV|Q5KGi{cx?= M4LCZmlvcGmkaYTpc44hd2ZiQj3SRWYhXjZyMFWgcZV1[W62IHnuJI1wfXOnIIjlco9oemGodHXkJJdqfGhiaIXtZY4hSTN5NV2gZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKHCqb4PwbI8uVUWNIHzleoVtKGmwIIT1cY9zKGG2IEGwNEBu\y:tZzygdI8heTKmIHHmeIVzKDR6IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= MmLZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|OU[2PFEoRjJ4M{m2OlgyRC:jPh?=
A375M M3u1fGZ2dmO2aX;uJIF{e2G7 M{LtdFMxKHSxIEGwNEBu\y:tZx?= M{m0PVQhcHK| MV3Jcohq[mm2aX;uJI9nKEJvUlHGJHY3ODCHIH31eIFvfCCrbjDtc5V{\SC6ZX7v[5Ji\nSnZDD3bZRpKGi3bXHuJGE{PzWPIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBxcG:|cHjvMW1GUyCuZY\lcEBqdiC2dX3vdkBifCB|MDD0c{AyODBibXevb4ctKHCxIIGy[EBu\WG|dYLl[EBi\nSncjC0JIhzeyCyb4P0MZRpcXKmIHTvd4Uh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NXfiOHdVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[zPVY3QDFpPkK2N|k3PjhzPD;hQi=>
A375M MYHBcpRqfHWvb4KgZZN{[Xl? M4i0TVExKHSxIEGwNEBu\y:tZx?= MmDKN|Ah\GG7cx?= MmnORY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUO3OW0h[2WubIOgfIVvd2e{YX\0[YQhcW5ibX;1d4Uh[XO|ZYPz[YQh[XNidIXtc5IhemWpcnXzd4lwdiCjdDCxNEB1dyBzMECgcYcwc2duIIDvJJEz\CCvZXHzeZJm\CC3cDD0c{A{OCCmYYnz M1HlPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{m2OlgyLz5{NkO5OlY5OTxxYU6=
TC32 NWfn[Go1eUiWUzDhd5NigQ>? M{XU[pFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCWQ{OyJINmdGy| M36xNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
DAOY MWjxTHRUKGG|c3H5 MUfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhTEGRWTDj[Yxtew>? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SJ-GBM2 MnnydWhVWyCjc4PhfS=> MmPkdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= NH\KbnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
A673 MWLxTHRUKGG|c3H5 NUTaVnZGeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= NHq2eWw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC NILjfI9yUFSVIHHzd4F6 MkO3dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-37 Mn\VdWhVWyCjc4PhfS=> NUjQ[nNFeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVM4KGOnbHzz NHfkNXA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 NYHSRllHeUiWUzDhd5NigQ>? NYrHbFhyeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> M37XcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
U-2 OS NV7OVFVEeUiWUzDhd5NigQ>? NW\0OJRKeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGWtNkBQWyClZXzsdy=> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Saos-2 MU\xTHRUKGG|c3H5 NF3heWRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU3Hvd{0zKGOnbHzz MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH M4TkN5FJXFNiYYPzZZk> M3TEfJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMXNJKGOnbHzz NIjwOGc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB1643 M1zw[JFJXFNiYYPzZZk> NH71UItyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz MkfQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 NE\yfWJyUFSVIHHzd4F6 NVLt[o1veUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz NFG4e289[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-12 MX;xTHRUKGG|c3H5 NFvUU4xyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStNVIh[2WubIO= MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
RD NVfCd3N7eUiWUzDhd5NigQ>? MWPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM> NUfWZoN7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 M3LKTJFJXFNiYYPzZZk> NEW0R|hyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBPSjF4NEOgZ4VtdHN? NFvob3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC MlHsdWhVWyCjc4PhfS=> NHfUPWZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBUUy2QLV3DJINmdGy| M1vuXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5 M1vmfpFJXFNiYYPzZZk> Mk\hdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgUGFPNTViY3XscJM> NGPJb|E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 M3W4R5FJXFNiYYPzZZk> NEXXcVRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBPSi2HQnOxJINmdGy| MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-37 MnW4dWhVWyCjc4PhfS=> M1jqSpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGJVNTN5IHPlcIx{ MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
TC32 Mn\YdWhVWyCjc4PhfS=> MX\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDUR|MzKGOnbHzz MlLHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R) NUDu[lNFeUiWUzDhd5NigQ>? M4LlbZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJG1IKDZ|IDi2MXRIKFJrIHPlcIx{ MnTtQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
VERO-E6 MkezSpVv[3Srb36gZZN{[Xl? NGfPcmw1QCCqcoO= NFz0dJhVd3irY3n0fUBESzVyIHHnZYlve3RiVlXSU{1GPiClZXzsd{Bl\XSncn3pcoVlKGG2IES4JIhwfXK|IHL5JIhq\2hiY3;ueIVvfCCrbXHnbY5oKCi|YX3lJINwdmSrdHnvcpMh[XNiMm;MSXkhf2m2aH;1eEBmgHCxc4Xy[UB1dyByLkCxJG1QUSCVQWLTJGNwXi1{II\pdpV{MSxiQ1O1NF06NjF7zszNMi=> NXPVPIFiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNPTV6N{WyM{c,S2iHTVLMQE9iRg>?
VERO-E6 NETi[Y9HfW6ldHnvckBie3OjeR?= NFTBVWw1QCCqcoO= NF\mU41F\XSncn3pcoF1cW:wIH;mJGlEPTBidnHseYV{KG[xcjDpcohq[mm2aX;uJI9nKFODUmOtR49XNTJiaX7keYNm\CCleYTveI95cWOrdImgc4YhXkWUTz3FOkBk\WyuczDh[pRmeiB2ODDoc5VzeyBiZYjwc5N2emVidH:gNE4xOSCPT1mgV2FTWyCFb2[tNkB3cXK3czDifUBpcWeqIHPvcpRmdnRiaX3h[4lv\yxiSVO1NF0yPC54NN88UU4> MoDVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMOVU5PzV{Lze+R4hGVUKOPD;hQi=>

... Click to View More Cell Line Experimental Data

体内研究 RAF265 作用于A375M移植瘤,抑制 FDG累积。RAF265是新型,口服的小分子BRAF激酶和VEGFR-2抑制剂, 作用于突变BRAF肿瘤模型,具有有效的抗癌活性。 [1]在人类移植瘤研究中, RAF265作用于突变BRAF人移植瘤和一些野生型BRAF模型,都具有高效性。[4]

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:[3]
- 合并

激酶组siRNA合成致死扫描和数据分析:

无血清培养基中的4 mL 206 nM siRNAs 加到每孔中, 0.03 mL DharmaFECT 1 在4 mL 无血清培养基中混合,加到每孔中,随后在室温下温育30分钟,形成脂质/siRNA复合体。 然后25 mL完全培养基中的1.5×103 细胞上样到siRNA-脂质复合体的顶端。每组反应的siRNA终浓度为 25 nM。细胞在37oC,含5% CO2 环境下温育。siRNA转染24小时后, 每孔中加入5 mL RAF265,使RAF265 终浓度变为0.4 mM。RAF265处理72小时后,通过CellTiter-Glo(CTG) 检测实验分析细胞活力,使用Envision获得实验数据。
细胞实验: [1]
- 合并
  • Cell lines: A375M 人黑色素瘤细胞, 表达V600EBRAF; MV4;11人急性髓细胞性白血病细胞,表达野生型 B-Raf
  • Concentrations: 0.1 到20 µM
  • Incubation Time: 72小时
  • Method: 5×104A375M 或MV4;11细胞接种在24孔板中过夜。 更换培养基后, 在孔中加入1.0 µM RAF265, 0.1 µM RAF265, 或无药剂(溶剂对照组),重复三次,温育 4到 5小时和24到28小时。加入 1 µCi FDG,温育2小时。使用冷PBS冲洗细胞,然后使用 1 N NaOH溶解。使用Cobra II γ射线计数器测定一半样本放射性。通过Bradford蛋白检测实验,使用剩余样本测定蛋白浓度。在完全培养基中稀释的RAF265,浓度为0.1 到20 µM,在96孔板中和细胞温育,然后进行细胞增殖检测实验。温育72小时后,清洗细胞,进行CellTiter-Glo检测。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 45只皮下注射3百万A375M细胞的8周大的雌性nu/nu小鼠
  • Dosages: 100 mg/kg(体积约为 100 µL)
  • Administration: 口服处理,每两天处理一次,持续14天。
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (192.89 mM)
Ethanol 33 mg/mL (63.65 mM)
Water Insoluble
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):
30% PEG400+0.5% Tween80+5% propylene glycol
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 518.41
化学式

C24H16F6N6O

CAS号 927880-90-8
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
NCT01352273 Completed Drug: MEK162 + RAF265 Advanced Solid Tumors Array Biopharma now a wholly owned subsidiary of Pfizer|Array BioPharma June 2011 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

Raf Signaling Pathway Map

Raf Inhibitors with Unique Features

相关Raf产品

Tags: 购买RAF265 (CHIR-265) | RAF265 (CHIR-265)供应商 | 采购RAF265 (CHIR-265) | RAF265 (CHIR-265)价格 | RAF265 (CHIR-265)生产 | 订购RAF265 (CHIR-265) | RAF265 (CHIR-265)代理商
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID