LY3009120

For research use only. Not for use in humans.

目录号:S7842 别名: DP-4978

LY3009120 Chemical Structure

CAS No. 1454682-72-4

LY03009120 (DP-4978)是一种有效的泛Raf抑制剂,在A375细胞中对A-raf,B-Raf,和 C-Raf的IC50分别为44 nM,31-47 nM,和 42 nM。LY03009120 可诱导自噬。Phase 1。

规格 价格 库存 购买数量  
RMB 1207.33 现货
RMB 3906.82 现货
RMB 8154.89 现货
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客户使用Selleck生产的LY3009120发表文献39篇:

产品安全说明书

Raf抑制剂选择性比较

生物活性

产品描述 LY03009120 (DP-4978)是一种有效的泛Raf抑制剂,在A375细胞中对A-raf,B-Raf,和 C-Raf的IC50分别为44 nM,31-47 nM,和 42 nM。LY03009120 可诱导自噬。Phase 1。
靶点
C-Raf [1]
(Cell-free assay)
BRAF(V600E) [1]
(Cell-free assay)
BRAF WT [1]
(Cell-free assay)
4.3 nM 5.8 nM 15 nM
体外研究

LY3009120抑制A375和 HCT116细胞的生长,IC50分别为9.2和220 μM。LY3009120抑制酪氨酸激酶KDR,IC50为3.9 μM。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A375 MkLBRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M4PYeVczKGi{cx?= MXnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF|N{WgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KHKnc3H6eZJqdiCjc4PhfUwhUUN3ME2wMlAxQTMQvF2u MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl4NUiwOEc,OjV7NkW4NFQ9N2F-
A375 NUS4W|dwTnWwY4Tpc44h[XO|YYm= NEDvR2QyPSCvaX7z NW\meo05S2:vcHX0bZRqfmViYnnu[Ilv\yCjZn\pcol1gSC2bzDFdIhCOiCrbjDoeY1idiCDM{e1JINmdGy|IHHmeIVzKDF3IH3pcpMhcW5icILld4Vv[2Vib3[gRXRRKGGwYXzv[5VmNCCLQ{WwQVAvODMQvF2u M2XURVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OU[1PFA1Lz5{NUm2OVgxPDxxYU6=
A375 NX7ScZVoTnWwY4Tpc44h[XO|YYm= NXu0O2RiOTVibXnudy=> NELmU3NEd22yZYTpeIl3\SCkaX7kbY5oKGGoZnnubZR6KHSxIFLSRWYhcW5iaIXtZY4hSTN5NTDj[YxteyCjZoTldkAyPSCvaX7zJIlvKHC{ZYPlcoNmKG:oIFHUVEBidmGub3f1[UwhUUN3ME2wMlA{Oc7:TT6= MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl4NUiwOEc,OjV7NkW4NFQ9N2F-
A375 MVnGeY5kfGmxbjDhd5NigQ>? MYC3NkBpenN? M3TjSWlvcGmkaYTpc44hd2ZiQmLBSkBXPjByRTDteZRidnRiaX6gbJVu[W5iQUO3OUBk\WyuczDhd5Nme3OnZDDhd{BqdmirYnn0bY9vKG:oIFXST{BxcG:|cHjvdplt[XSrb36gcYVie3W{ZXSgZYZ1\XJiN{KgbJJ{KGK7IFXMTXNCKGG|c3H5MEBKSzVyPUCuNFM4|ryPLh?= NVK1RXVRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5OlU5ODRpPkK1PVY2QDB2PD;hQi=>
A375 MXLGeY5kfGmxbjDhd5NigQ>? NX3pbWwyOTVibXnudy=> MX3Dc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKFqDSzDpckBpfW2jbjDBN|c2KGOnbHzzJIFnfGW{IEG1JI1qdnNiaX6gdJJme2WwY3Wgc4YhSVSSIHHuZYxw\3WnLDDJR|UxRTBwMEO5{txONg>? M3z5dVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OU[1PFA1Lz5{NUm2OVgxPDxxYU6=
A375 MlPPSpVv[3Srb36gZZN{[Xl? NY\qelZMOTVibXnudy=> MWjDc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKEOUQV[gbY4hcHWvYX6gRVM4PSClZXzsd{Bi\nSncjCxOUBucW6|IHnuJJBz\XOnbnPlJI9nKEGWUDDhcoFtd2e3ZTygTWM2OD1yLkC0Nu69VS5? M3jLbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OU[1PFA1Lz5{NUm2OVgxPDxxYU6=
A375 M3iyXGZ2dmO2aX;uJIF{e2G7 M4G3SVE2KG2rboO= MVvDc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKEGUQV[gbY4hcHWvYX6gRVM4PSClZXzsd{Bi\nSncjCxOUBucW6|IHnuJJBz\XOnbnPlJI9nKEGWUDDhcoFtd2e3ZTygTWM2OD1yLkC0OO69VS5? MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl4NUiwOEc,OjV7NkW4NFQ9N2F-
A375 MonPSpVv[3Srb36gZZN{[Xl? NGTtWIkyPSCvaX7z NE\sfYREd22yZYTpeIl3\SCkaX7kbY5oKGGoZnnubZR6KHSxIICzPEBqdiCqdX3hckBCOzd3IHPlcIx{KGGodHXyJFE2KG2rboOgbY4heHKnc3XuZ4Uhd2ZiQWTQJIFv[WyxZ4XlMEBKSzVyPUCuNFYy|ryPLh?= NXzic48{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5OlU5ODRpPkK1PVY2QDB2PD;hQi=>
A375 M3KyXmZ2dmO2aX;uJIF{e2G7 NUXoUVBSOTVibXnudy=> NVHpT2ZIS2:vcHX0bZRqfmViYnnu[Ilv\yCjZn\pcol1gSC2bzDGXW4hcW5iaIXtZY4hSTN5NTDj[YxteyCjZoTldkAyPSCvaX7zJIlvKHC{ZYPlcoNmKG:oIFHUVEBidmGub3f1[UwhUUN3ME2wMlA6Oc7:TT6= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl4NUiwOEc,OjV7NkW4NFQ9N2F-
A375 NITaZ|FHfW6ldHnvckBie3OjeR?= M3v4NFE2KG2rboO= NFzrOZdEd22yZYTpeIl3\SCkaX7kbY5oKGGoZnnubZR6KHSxIF3BVFNMOSCrbjDoeY1idiCDM{e1JINmdGy|IHHmeIVzKDF3IH3pcpMhcW5icILld4Vv[2Vib3[gRXRRKGGwYXzv[5VmNCCLQ{WwQVAvODl6zszNMi=> NX3jXZVERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5OlU5ODRpPkK1PVY2QDB2PD;hQi=>
A375 M1zKfWZ2dmO2aX;uJIF{e2G7 NEDvO4cyPSCvaX7z MYHDc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKEWyaFK0JIlvKGi3bXHuJGE{PzViY3XscJMh[W[2ZYKgNVUhdWmwczDpckBxemW|ZX7j[UBw\iCDVGCgZY5idG:pdXWsJGlEPTB;MD6x{txONg>? MoHWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NkW4NFQoRjJ3OU[1PFA1RC:jPh?=
HCT116 NVuxT3BFTnWwY4Tpc44h[XO|YYm= NGTUUIhKdmirYnn0bY9vKG:oIFvSRXMhTzF|RDDteZRidnRiaX6gbJVu[W5iSFPUNVE3KGOnbHzzJIF{e2W|c3XkJIF{KGmwaHnibZRqd25ib3[gSXJMKHCqb4PwbI9zgWyjdHnvckBjgSCHTFnTRUwhUUN3ME2wMlE2|ryPLh?= MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl4NUiwOEc,OjV7NkW4NFQ9N2F-
A375 NGjLNY9HfW6ldHnvckBie3OjeR?= MV3JckB3cX[xIHnubIljcXSrb36gc4YhSlKDRjDWOlAxTSCvdYThcpQhcW5iaIXtZY4hSTN5NTDj[YxteyC6ZX7v[5Ji\nSnZDDpckBxdyCmb4Pl[EBPUUhiboXk[UBz[XRiYYPz[ZN{\WRiYYOgdIxie22jIHPvcoNmdnS{YYTpc44hemWzdXny[YQhfG9iaX7obYJqfCCHUlugdIhwe3Cqb4L5cIF1cW:wIHL5JFUxLSxiSV7IQVAvOTZ3zszNMi=> MmnUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV7NkW4NFQoRjJ3OU[1PFA1RC:jPh?=
HCT116 M1LIemFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MXK2O{BpenN? MVXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDh[pRmeiB4NzDodpMh[nlicnXzZZp2emmwIHHzd4F6NCCLQ{WwQVAvOjMQvF2u M1S5PVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OU[1PFA1Lz5{NUm2OVgxPDxxYU6=
A375 NFvGT2ZHfW6ldHnvckBie3OjeR?= M2LQS|E2KG2rboO= NF\lPVdEd22yZYTpeIl3\SCkaX7kbY5oKGGoZnnubZR6KHSxIFPTT{BqdiCqdX3hckBCOzd3IHPlcIx{KGGodHXyJFE2KG2rboOgbY4heHKnc3XuZ4Uhd2ZiQWTQJIFv[WyxZ4XlMEBKSzVyPUCuNlnPxE1w M{j1WFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OU[1PFA1Lz5{NUm2OVgxPDxxYU6=
A375 M4TSWmZ2dmO2aX;uJIF{e2G7 MorqNVUhdWmwcx?= MYDDc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKFOUQzDpckBpfW2jbjDBN|c2KGOnbHzzJIFnfGW{IEG1JI1qdnNiaX6gdJJme2WwY3Wgc4YhSVSSIHHuZYxw\3WnLDDJR|UxRTBwM{JOwG0v MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTl4NUiwOEc,OjV7NkW4NFQ9N2F-
A375 NYHMdGIyTnWwY4Tpc44h[XO|YYm= M1TxUFE2KG2rboO= NYDMTmlQS2:vcHX0bZRqfmViYnnu[Ilv\yCjZn\pcol1gSC2bzDBRmwhcW5iaIXtZY4hSTN5NTDj[YxteyCjZoTldkAyPSCvaX7zJIlvKHC{ZYPlcoNmKG:oIFHUVEBidmGub3f1[UwhUUN3ME2wMlM5|ryPLh?= NU\PW2pKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5OlU5ODRpPkK1PVY2QDB2PD;hQi=>
A375 MXHGeY5kfGmxbjDhd5NigQ>? NEnCWGkyPSCvaX7z NYrBUphzS2:vcHX0bZRqfmViYnnu[Ilv\yCjZn\pcol1gSC2bzDJVmFMOSCrbjDoeY1idiCDM{e1JINmdGy|IHHmeIVzKDF3IH3pcpMhcW5icILld4Vv[2Vib3[gRXRRKGGwYXzv[5VmNCCLQ{WwQVAvOzoQvF2u NVvpSFRuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5OlU5ODRpPkK1PVY2QDB2PD;hQi=>
A375 NWraSFBPTnWwY4Tpc44h[XO|YYm= M4e2S|E2KG2rboO= MWTDc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKEeFTkKgbY4hcHWvYX6gRVM4PSClZXzsd{Bi\nSncjCxOUBucW6|IHnuJJBz\XOnbnPlJI9nKEGWUDDhcoFtd2e3ZTygTWM2OD1yLkS1{txONg>? NFPSb2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm2OVgxPCd-MkW5OlU5ODR:L3G+
A375 NHPheWxHfW6ldHnvckBie3OjeR?= M{TYPVE2KG2rboO= NYnlRXZmS2:vcHX0bZRqfmViYnnu[Ilv\yCjZn\pcol1gSC2bzDKUmshcW5iaIXtZY4hSTN5NTDj[YxteyCjZoTldkAyPSCvaX7zJIlvKHC{ZYPlcoNmKG:oIFHUVEBidmGub3f1[UwhUUN3ME2wMlQ4|ryPLh?= NGjtOJA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm2OVgxPCd-MkW5OlU5ODR:L3G+
A375 MYTGeY5kfGmxbjDhd5NigQ>? NI\NfXkyPSCvaX7z MVLDc41x\XSrdHn2[UBjcW6maX7nJIFn\mmwaYT5JJRwKE2DUELLOUBqdiCqdX3hckBCOzd3IHPlcIx{KGGodHXyJFE2KG2rboOgbY4heHKnc3XuZ4Uhd2ZiQWTQJIFv[WyxZ4XlMEBKSzVyPUCuPO69VS5? NIDVdpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUm2OVgxPCd-MkW5OlU5ODR:L3G+
A375 NVvnSVlVTnWwY4Tpc44h[XO|YYm= M3ru[VE2KG2rboO= NF\v[4pEd22yZYTpeIl3\SCkaX7kbY5oKGGoZnnubZR6KHSxIFvIV|EhcW5iaIXtZY4hSTN5NTDj[YxteyCjZoTldkAyPSCvaX7zJIlvKHC{ZYPlcoNmKG:oIFHUVEBidmGub3f1[UwhUUN3ME2wMlk4|ryPLh?= M4HWRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OU[1PFA1Lz5{NUm2OVgxPDxxYU6=
HCT116 M{LKTWZ2dmO2aX;uJIF{e2G7 MWi8NVAxKG6P MoLJVIFz[WSxeHnjZYwh[WO2aY\heIlwdiCxZjDSRXMwWkGIL13FT{B{cWewYXzpcocheGG2aIfhfUBqdiCqdX3hckBJS1RzMU[gZ4VtdHNiZYjwdoV{e2mwZzD3bYxlKHS7cHWgRnJCTiCjc4Pld5Nm\CCjczDFVmsheGixc4Doc5J6dGG2aX;uJIF1KDxzMECgcm0> M{THZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3OU[1PFA1Lz5{NUm2OVgxPDxxYU6=
A375 MoTmSpVv[3Srb36gZZN{[Xl? MlnpTY5pcWKrdHnvckBw\iCmZYP0bIlw[mmxdHnuMWFVWCCjY4nsdIhwe3CqYYTlJJBzd2KnIHLpcoRqdmdidH:gRk1T[WZiaX6gbJVu[W5iQUO3OUBk\WyuczDifUBOWyCjbnHsfZNqeyxiSVO1NF0xNjB|Md88UU4> MlHpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB3Mkm1OFMoRjNyNUK5OVQ{RC:jPh?=
A375 NFfJT4lHfW6ldHnvckBie3OjeR?= M2rodWlvcGmkaYTpc44hd2ZiZHXzeIhqd2Krb4Tpck1CXFBiYXP5cJBpd3OyaHH0[UBxem:kZTDibY5lcW6pIITvJGMuWmGoIHnuJIh2dWGwIFGzO|Uh[2WubIOgZpkhVVNiYX7hcJl{cXNuIFnDOVA:OC5yNENOwG0v NXn6dFhbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1Nlk2PDNpPkOwOVI6PTR|PD;hQi=>
A375 Mo\KSpVv[3Srb36gZZN{[Xl? M{jEdmlvcGmkaYTpc44hd2ZiZHXzeIhqd2Krb4Tpck1CXFBiYXP5cJBpd3OyaHH0[UBxem:kZTDibY5lcW6pIITvJGEuWmGoIHnuJIh2dWGwIFGzO|Uh[2WubIOgZpkhVVNiYX7hcJl{cXNuIFnDOVA:OC5yNEVOwG0v NEHrdYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEWyPVU1Oyd-M{C1Nlk2PDN:L3G+
MV4-11 NGHY[2RCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NFiyXGQ4OiCqcoO= MYrBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2YND2xNUBk\WyuczDh[pRmeiB5MjDodpMh[nliQ3XscE1VcXSncjDHcI8h[XO|YYmsJGlEPTB;MD6x{txONg>? M{DnSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUK5OVQ{Lz5|MEWyPVU1OzxxYU6=
SK-MEL-2 M{nMVGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MVy3NkBpenN? NUfRT|JHSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTT{1OTUxvMjDj[YxteyCjZoTldkA4OiCqcoOgZpkhS2WubD3UbZRmeiCJbH:gZZN{[XluIFnDOVA:OC5{zszNMi=> M{TjflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUK5OVQ{Lz5|MEWyPVU1OzxxYU6=
A375 NUna[5RGSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NWS4THZRPzJiaILz MmezRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDM{e1JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFZXzsMXRqfGW{IFfsc{Bie3OjeTygTWM2OD1yLkROwG0v MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODV{OUW0N{c,OzB3Mkm1OFM9N2F-
SW579 MUHBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NGHjR2E4OiCqcoO= NVzTR2tiSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTW|U4QSClZXzsd{Bi\nSncjC3NkBpenNiYomgR4VtdC2WaYTldkBIdG9iYYPzZZktKEmFNUC9NE46|ryPLh?= NI\YWWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEWyPVU1Oyd-M{C1Nlk2PDN:L3G+
HT-29 NG\Ye2lCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MUi3NkBpenN? MYHBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiWLUK5JINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFZXzsMXRqfGW{IFfsc{Bie3OjeTygTWM2OD1yLkpOwG0v NXTCfIZRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1Nlk2PDNpPkOwOVI6PTR|PD;hQi=>
HepG2 NIrjVGpCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M4fkcVczKGi{cx?= MUXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEincFeyJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCFZXzsMXRqfGW{IFfsc{Bie3OjeTygTWM2OD1{LkdOwG0v M2i0T|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUK5OVQ{Lz5|MEWyPVU1OzxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-EGFR / EGFR / p-BRAF / BRAF / p-CRAF / CRAF / p-MEK / MEK / p-AKT / AKT; 

PubMed: 27999210     


CRC cell lines were treated with DMSO or 1 μM LY3009120 for 24 and 48 hrs. Whole cell lysates were analyzed by Western blot using antibodies against the proteins indicated.

Beclin-1 / Mcl-1 / LC3 / p62 ; 

PubMed: 28382170     


LY3009120 treatment of K1 cells increased the conversion of LCⅠ to LC3Ⅱ without influencing the expression of Beclin-1.

27999210 28382170
体内研究 在负荷BRAF V600E ST019VR PDX肿瘤的大鼠体内,LY3009120 (15 or 30 mg/kg, p.o.)剂量依赖性抑制肿瘤生长。在负荷A375异种移植物的裸鼠体内,LY3009120 (3到50 mg/kg, p.o.)单剂量口服治疗剂量依赖性抑制磷酸-ERK,4.36 mg/kg剂量下抑制50%磷酸- ERK (EC50),68.9 ng/mL或165 nM血浆浓度下达到50%磷酸- ERK (EC50) 抑制率。[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:[2]
- 合并

使用KiNativ试验测定激酶活性:

化合物在A375细胞裂解物中使用基于ATP的探针在5 µM下筛选。IC50值以微摩尔单位表示。细胞沉淀重悬浮在4体积裂解缓冲液[25 mM Tris pH 7.6,150 mM NaCl,1% CHAPS,1% Tergitol NP-40 型,1% v/v 磷酸酶抑制剂混合物II]中,使用尖端超声波仪声处理,并均质化。裂解产物通过100,000 g下离心分离30分钟除去。澄清的裂解液通过0.22 μM注射过滤器和凝胶过滤到反应缓冲液[20 mM Hepes pH 7.8,150 mM NaCl,0.1% triton X-100,1% v/v 磷酸酶抑制剂混合物II]。抑制剂处理和探针标记之前,将终浓度为20 mM 的MnCl2加入裂解液。用于IC50测定的终抑制剂浓度为10,1,0.1,和 0.01 μM。ATP竞争性实验在1,000,100,10,和1 μM ATP下进行。所有抑制剂的处理在室温下进行。
细胞实验:[1]
- 合并
  • Cell lines: A375 和 HCT116 细胞
  • Concentrations: 0.51 μM
  • Incubation Time: 67 h
  • Method: 简而言之,细胞在DMEM高浓度葡萄糖中生长,用10%胎牛血清和1%青霉素/链霉素/L-谷氨酰胺增补,在37℃,5% CO2,和95%湿度下培育。允许细胞扩增到70-95%的融合度。连续稀释的测试化合物分配加入到384孔黑色透明底板。每孔加入包含625个细胞的50 μL完全生长培养基。板在37℃,5% CO2,和95%湿度下培育67小时。然后,10 μL包含440 μM 刃天青的PBS溶液加入板的每孔中,板在37℃,5% CO2,和95%湿度下再培育5小时。板在Synergy2阅读器上使用540 nm激发波长和600 nm发射波长读取。得到的数据使用Prism软件分析以计算IC 50值。
    (Only for Reference)
动物实验:[1]
- 合并
  • Animal Models: 负荷BRAF V600E ST019VR PDX肿瘤的雌性 NIH裸鼠
  • Dosages: 30 mg/kg
  • Administration: p.o.
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 3 mg/mL warmed (7.06 mM)
Water Insoluble
Ethanol 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):
0.5% CMC Na
30mg/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 424.51
化学式

C23H29FN6O

CAS号 1454682-72-4
储存条件 粉状
溶于溶剂
别名 DP-4978

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
NCT02014116 Terminated Drug: LY3009120 capsule Neoplasms|Neoplasm Metastasis|Melanoma|Carcinoma Non-Small-Cell Lung|Colorectal Neoplasms Eli Lilly and Company November 26 2013 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

常见问题及建议解决方法

  • 问题 1:

    I am trying to figure out solubility of the drug LY3009120 Catalog #7842 for in vivo studies. I need some details on the formulation and how it is made to dissolve the chemical?

  • 回答:

    It can dissolve in 4% DMSO/30% PEG 300/5% Tween 80/ddH2O at 1 mg/ml clearly, and in 0.5% CMC Na at 30 mg/ml as a suspension.

Raf Signaling Pathway Map

相关Raf产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID