Entrectinib (RXDX-101)

For research use only. Not for use in humans.

目录号:S7998 别名: NMS-E628 中文名称:恩曲替尼

Entrectinib (RXDX-101) Chemical Structure

CAS No. 1108743-60-7

Entrectinib (RXDX-101, NMS-E628) 是一种口服生物可利用的泛-TrkA/B/CROS1ALK 抑制剂,IC50范围为 0.1~1.7 nM。Entrectinib (RXDX-101) 可诱导自噬。Phase 2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 1556.1 现货
RMB 875.36 现货
RMB 3073.41 现货
RMB 6935.43 现货
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客户使用Selleck生产的Entrectinib (RXDX-101)发表文献20篇:

产品安全说明书

Trk receptor抑制剂选择性比较

生物活性

产品描述 Entrectinib (RXDX-101, NMS-E628) 是一种口服生物可利用的泛-TrkA/B/CROS1ALK 抑制剂,IC50范围为 0.1~1.7 nM。Entrectinib (RXDX-101) 可诱导自噬。Phase 2。
靶点
TrkA [1] TrkB [1] TrkC [1] ROS1 [1] ALK [1]
体外研究

Entrectinib selectively blocks proliferation of ALK-dependent cell lines and potently inhibits ALK‐dependent signaling. Entrectinib also highly inhibits cell growth of the NSCLC cell line NCI‐H2228 bearing the EML4-ALK rearrangement. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BAF3 NHWyNW1HfW6ldHnvckBie3OjeR?= NW\QeYJUPzJiaILz MnHqTY5pcWKrdHnvckBw\iCqdX3hckBVTUxiKEOzOkBz\XOrZIXld{kh\nW|ZXStWHJMSiBqNEW1JJRwKDh{MjDy[ZNq\HWnczmgLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hdW:3c3WgRmFHOyClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3MDC9JFAvODB|IN88UU4> MkXxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
BAF3 M3LQNWZ2dmO2aX;uJIF{e2G7 M4LrdVczKGi{cx?= NEW0SYZKdmirYnn0bY9vKG:oIHj1cYFvKFSHTDCoN|M3KHKnc3nkeYV{MSCodYPl[E1VWkuDIDi0OFAhfG9iN{m2JJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCvb4Xz[UBDSUZ|IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JINmdGxidHn0[ZIu\2yxIHHzd4F6NCCLQ{WwJF0hOC5yMEOg{txONg>? MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
BAF3 NIDzO3FHfW6ldHnvckBie3OjeR?= NF\se2g4OiCqcoO= NFr2[HRKdmirYnn0bY9vKG:oIHj1cYFvKFSHTDCoN|M3KHKnc3nkeYV{MSCodYPl[E1VWkuFIDi0OVQhfG9iOEK1JJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCvb4Xz[UBDSUZ|IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JINmdGxidHn0[ZIu\2yxIHHzd4F6NCCLQ{WwJF0hOC5yMEOg{txONg>? NVOxU2l6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
BAF3 NVzHN5lRTnWwY4Tpc44h[XO|YYm= M2fyV|czKGi{cx?= MmrmTY5pcWKrdHnvckBw\iCqdX3hckBVTUxiKEOzOkBz\XOrZIXld{kh\nW|ZXStVm9UOSBqMUi5NUB1dyB{M{S3JJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCvb4Xz[UBDSUZ|IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JINmdGxidHn0[ZIu\2yxIHHzd4F6NCCLQ{WwJF0hOC5yMEWg{txONg>? M{\YZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
KM12 M{DKT2FvfGmycn;sbYZmemG2aY\lJIF{e2G7 NIXrW3A4OiCqcoO= NGrxWFhCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvNNVIh[2WubIOg[ZhxemW|c3nu[{BVWkuDIIDyc5RmcW5iaX7jeYJifGWmIH\vdkA4OiCqcoOgZpkh[2WubDD0bZRmei2pbH:gZZN{[XluIFnDOVAhRSByLkCxO{DPxE1w NHLGS3c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
SU-DHL1 MkDKRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NIfxOmM4OiCqcoO= MVvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOXLVTIUFEh[2WubIOg[ZhxemW|c3nu[{BCVEticILveIVqdiCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBk\WyuIITpeIVzNWeubzDhd5NigSxiSVO1NEA:KDBwMEK0JO69VS5? NX[0O4p2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
BAF3 M1rhOmZ2dmO2aX;uJIF{e2G7 MkTWO|IhcHK| NV6zbYRyUW6qaXLpeIlwdiCxZjD3bYxlKHS7cHWgSW1NPC2DTFugLJVvc26xd36gc5Jq\2mwKTDlfJBz\XO|ZXSgbY4hdW:3c3WgRmFHOyClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3MDC9JFAvODJ6IN88UU4> Mn3HQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
KARPAS299 MUjBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MkLDO|IhcHK| M2HzWmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1HSVGFUOjl7IHPlcIx{KGmwY4XiZZRm\CCob4KgO|IhcHK|IHL5JINmdGxidHn0[ZIu\2yxIHHzd4F6NCCLQ{WwJF0hOC5yM{Gg{txONg>? NWLxS5doRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
SUP-M2 M33ReWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MXu3NkBpenN? MmXYRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCVVWCtUVIh[2WubIOg[ZhxemW|c3nu[{BCVEticILveIVqdiCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBk\WyuIITpeIVzNWeubzDhd5NigSxiSVO1NEA:KDBwMESxJO69VS5? MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
BAF3 NUnO[XVMTnWwY4Tpc44h[XO|YYm= MXu3NkBpenN? NEP2bpJKdmirYnn0bY9vKG:oIFXNUFQuSUyNIFyxNVk3VSCvdYThcpQhMHWwa37ve44hd3KrZ3nuLUBmgHC{ZYPz[YQhcW5ibX;1d4UhSkGIMzDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKGe{b4f0bEBqdmirYnn0bY9vKGGodHXyJFczKGi{czDifUBk\WyuIITpeIVzNWeubzDhd5NigSxiSVO1NEA:KDBwME[3JO69VS5? NEHoOlY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
NCI-H2228 NFHjTG5CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NHjN[Yc4OiCqcoO= NWHQN5M{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDOR2kuUDJ{MkigZ4VtdHNiZYjwdoV{e2mwZzDBUGsheHKxdHXpckBqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3MDC9JFAvODZ6IN88UU4> MofPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
MV411 NF\VdWhCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= NUXQdZZwPzJiaILz NHO3WWZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3WOFEyKGOnbHzzJIlv[3WkYYTl[EBnd3JiN{KgbJJ{KGK7IHPlcIwhfGm2ZYKt[4xwKGG|c3H5MEBKSzVyIE2gNE4xQDFizszNMi=> NYX3UoJyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
SR786 MVnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MVO3NkBpenN? MXLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOUN{i2JINmdGy|IHX4dJJme3OrbnegRWxMKHC{b4TlbY4hcW6ldXLheIVlKG[xcjC3NkBpenNiYomgZ4VtdCC2aYTldk1odG9iYYPzZZktKEmFNUCgQUAxNjB6MTFOwG0v M2D3blxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
BAF3 MoTJSpVv[3Srb36gZZN{[Xl? NYDPb2JtPzJiaILz NVe3colJUW6qaXLpeIlwdiCxZjDFUWw1NUGOSzDHNVIxOlJibYX0ZY51KCi3bnvuc5dvKG:{aXfpckkh\XiycnXzd4VlKGmwIH3veZNmKEKDRkOgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkA4OiCqcoOgZpkh[2WubDD0bZRmei2pbH:gZZN{[XluIFnDOVAhRSByLki5O{DPxE1w M3\XT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
BA/F3 Ml7KR5l1d3SxeHnjbZR6KGG|c3H5 NYnsTJdxPzJiaILz MYnDfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDJUE0{KGSncHXu[IVvfCCEQT;GN{Bk\WyuczDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSClZXzsJJRqfGW{LXfsc{Bie3OjeTygTWM2OCB;IEKuNVA1KM7:TT6= M{DDNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
KM12 NEm2fI1HfW6ldHnvckBie3OjeR?= M1PofVIhcHK| NWDSeVJ4UW6qaXLpeIlwdiCxZjDUVG0{NVSUS1GgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFvNNVIh[2WubIOgZZQhdG:5IHPvcoNmdnS{YYTpc44h[W[2ZYKgNkBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ M1i1blxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
KM12 NFL1NHpHfW6ldHnvckBie3OjeR?= NX73OYpNOiCqcoO= MmPoTY5pcWKrdHnvckBw\iCWUF2zMXRTU0FicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEuPMUKgZ4VtdHNiYYPz[ZN{\WRiYYOgd5VxeHKnc4Ppc44hd2ZiTVHQT{BxcG:|cHjvdplt[XSrb36gZZQhdG:5IHPvcoNmdnS{YYTpc44h[W[2ZYKgNkBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ NH74e4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
KM12 MYTGeY5kfGmxbjDhd5NigQ>? MkLWNkBpenN? M36wcGlvcGmkaYTpc44hd2ZiVGDNN{1VWkuDIIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCNTUGyJINmdGy|IHHzd4V{e2WmIHHzJJN2eHC{ZYPzbY9vKG:oIGDMR4didW2jMTDwbI9{eGixconsZZRqd25iYYSgcI94KGOxbnPlcpRz[XSrb36gZYZ1\XJiMjDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
KM12 NF;seFlHfW6ldHnvckBie3OjeR?= NYXKR5dnOiCqcoO= NHjMZ25KdmirYnn0bY9vKG:oIGTQUVMuXFKNQTDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iS12xNkBk\WyuczDhd5Nme3OnZDDhd{B{fXCycnXzd4lwdiCxZjDBT3QheGixc4Doc5J6dGG2aX;uJIF1KGyxdzDjc45k\W62cnH0bY9vKGGodHXyJFIhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? Mme2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
KM12 MoWwSpVv[3Srb36gZZN{[Xl? NF;JWoIzKGi{cx?= MkDTTY5pcWKrdHnvckBw\iCWUF2zMXRTU0FicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEuPMUKgZ4VtdHNiYYPz[ZN{\WRiYYOgd5VxeHKnc4Ppc44hd2ZiU{[gdIhwe3Cqb4L5cIF1cW:wIHH0JIxwfyClb37j[Y51emG2aX;uJIFnfGW{IEKgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> NG\PUnA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
KARPAS299 NFLzRYVHfW6ldHnvckBie3OjeR?= M1rRT|YxKG2pL3vn NGfKe4kyOiCqcoO= MoP4SZghfmm4bzDpcohq[mm2aX;uJI9nKE6STT3BUGsheGixc4Doc5J6dGG2aX;uJIlvKFOFSVSgcY92e2VieHXuc4dz[W[2ZXSge4l1cCCqdX3hckBMSVKSQWOyPVkh[2WubIOgZZQhPjBibXevb4ctKHCxIHHkcYlvcXO2ZYLl[EBieyC|aX7ncIUh\G:|ZTDt[YF{fXKnZDDh[pRmeiBzMjDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz M2ew[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
KARPAS299 NX[0Z2x5TnWwY4Tpc44h[XO|YYm= MmezOlAhdWdxa3e= MorUNVghcHK| NX\nT3l6TXhidnn2c{BqdmirYnn0bY9vKG:oIF7QUU1CVEticHjvd5Bpd3K7bHH0bY9vKGmwIGPDTWQhdW:3c3WgfIVvd2e{YX\0[YQhf2m2aDDoeY1idiCNQWLQRXMzQTliY3XscJMh[XRiNkCgcYcwc2duIIDvJIFldWmwaYP0[ZJm\CCjczDzbY5odGViZH;z[UBu\WG|dYLl[EBi\nSncjCxPEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ NX\QfnVVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
KARPAS299 M2CwWGZ2dmO2aX;uJIF{e2G7 NVyxcGhCPjBibXevb4c> NGrL[3oyOiCqcoO= M1zjd2V5KH[rdn:gbY5pcWKrdHnvckBw\iCQUF2tRWxMKHCqb4PwbI9zgWyjdHnvckBqdiCVQ1nEJI1wfXOnIIjlco9oemGodHXkJJdqfGhiaIXtZY4hU0GUUFHTNlk6KGOnbHzzJIF{e2W|c3XkJIF{KHO3cIDy[ZN{cW:wIH;mJHNVSVR|IIDoc5NxcG:{eXzheIlwdiCjdDC2NEBu\y:tZzygdI8h[WSvaX7pd5RmemWmIHHzJJNqdmeuZTDkc5NmKG2nYYP1doVlKGGodHXyJFEzKGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? NGfsWHo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
KARPAS299 MnPJSpVv[3Srb36gZZN{[Xl? NGTR[nA3OCCvZz;r[y=> Mlu3NVghcHK| NVHjU4xZUW5idnn2c{BqdmirYnn0bY9vKG:oIF7QUU1CVEticHjvd5Bpd3K7bHH0bY9vKGmwIGPDTWQhdW:3c3WgfIVvd2e{YX\0[YQhf2m2aDDoeY1idiCNQWLQRXMzQTliY3XscJMh[XO|ZYPz[YQh[XNic4XwdJJme3Orb36gc4YhW1SDVEOgdIhwe3Cqb4L5cIF1cW:wIHH0JFYxKG2pL3vnMEBxdyCjZH3pcol{fGW{ZXSgZZMhe2mwZ3zlJIRwe2VibXXhd5Vz\WRiYX\0[ZIhOThiaILzJIJ6KFenc4Tldo4h[myxdDDhcoFtgXOrcx?= NY\V[|RyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
NCI-H2228 Mo[3RY51cXS3bX;yJIF{e2G7 NH20fmE{OCC2bzC2NEBu\y:tZx?= MUSxNEBl[Xm| MV7BcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFIzOjhiY3XscJMhgGWwb3fyZYZ1\WRiaX6gZZRpgW2rYzDueU9vfSCvb4Xz[UBie3Onc4Pl[EBieyC2dX3vdkBoem:5dHigbY5pcWKrdHnvckBifCB|MDD0c{A3OCCvZz;r[{wheG9iYnnkJIFldWmwaYP0[ZJm\CCob4KgNVAh\GG7cx?= NVG3fYZuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
NCI-H2228 NVjsZZZ1TnWwY4Tpc44h[XO|YYm= NGTsU5I3OCCvZz;r[y=> NGDabZQyOiCqcoO= MVHFfEB3cX[xIHnubIljcXSrb36gc4YhTU2OND3BUGsheGixc4Doc5J6dGG2aX;uJIlvKGG2aIntbYMhdnVxboWgcY92e2VieHXuc4dz[W[2ZXSge4l1cCCqdX3hckBPS0lvSEKyNlgh[2WubIOgZZQhPjBibXevb4ctKHCxIHHkcYlvcXO2ZYLl[EBieyC|aX7ncIUh\G:|ZTDt[YF{fXKnZDDh[pRmeiBzMjDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz M1zjNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
NCI-H2228 NULjSmtOTnWwY4Tpc44h[XO|YYm= MmK3OlAhdWdxa3e= MX6xPEBpenN? Ml\ISZghfmm4bzDpcohq[mm2aX;uJI9nKEWPTEStRWxMKHCqb4PwbI9zgWyjdHnvckBqdiCjdHj5cYlkKG63L371JI1wfXOnIIjlco9oemGodHXkJJdqfGhiaIXtZY4hVkOLLViyNlI5KGOnbHzzJIF1KDZyIH3nM4toNCCybzDh[I1qdmm|dHXy[YQh[XNic3nu[4xmKGSxc3WgcYVie3W{ZXSgZYZ1\XJiMUigbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> MkXyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
NCI-H2228 MkWwSpVv[3Srb36gZZN{[Xl? MYW2NEBu\y:tZx?= NEjxTGsyOiCqcoO= NFfkZnpGgCC4aY\vJIlvcGmkaYTpc44hd2ZiRV3MOE1CVEticHjvd5Bpd3K7bHH0bY9vKGmwIHH0bJlucWNiboWvcpUhdW:3c3WgfIVvd2e{YX\0[YQhf2m2aDDoeY1idiCQQ1mtTFIzOjhiY3XscJMh[XO|ZYPz[YQh[XNic4XwdJJme3Orb36gc4YhSUuWIIDoc5NxcG:{eXzheIlwdiCjdDC2NEBu\y:tZzygdI8h[WSvaX7pd5RmemWmIHHzJJNqdmeuZTDkc5NmKG2nYYP1doVlKGGodHXyJFEzKGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? M1\uSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
NCI-H2228 M3LrXmZ2dmO2aX;uJIF{e2G7 M3XvSlYxKG2pL3vn M1ThV|E5KGi{cx?= M1;TZmV5KH[rdn:gbY5pcWKrdHnvckBw\iCHTVy0MWFNUyCyaH;zdIhwenmuYYTpc44hcW5iYYTofY1q[yCwdT;ueUBud3W|ZTD4[Y5w\3KjZoTl[EB4cXSqIHj1cYFvKE6FST3INlIzQCClZXzsd{Bie3Onc4Pl[EBieyC|dYDwdoV{e2mxbjDv[kBCU1RicHjvd5Bpd3K7bHH0bY9vKGG2IE[wJI1oN2upLDDwc{Bi\G2rbnnzeIVz\WRiYYOgd4lv\2ynIHTvd4UhdWWjc4Xy[YQh[W[2ZYKgNVghcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NXnzdnpORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
KARPAS299 NH;5UZlCdnSrdIXtc5Ih[XO|YYm= NV\MOox6OzBidH:gOlAhdWdxa3e= NFv3PHkyOCCmYYnz M2\yUmFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvBVnBCWzJ7OTDj[YxteyC6ZX7v[5Ji\nSnZDDpckBUS0mGIH3veZNmKGG|c3Xzd4VlKGG|IIT1cY9zKGe{b4f0bEBqdmirYnn0bY9vKGG2IEOwJJRwKDZyIH3nM4toNCCybzDibYQh[WSvaX7pd5RmemWmIH\vdkAyOCCmYYnz MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
KARPAS299 NYDhcGs6SW62aYT1cY9zKGG|c3H5 MmDrN|AhfG9iNkCgcYcwc2d? NG\3epEyOCCmYYnz MofVRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS1HSVGFUOjl7IHPlcIx{KHinbn;ndoFnfGWmIHnuJHNEUURibX;1d4Uh[XO|ZYPz[YQh[XNidIXtc5Ih\nKnZTDjeZJm\CCvb4Xz[UBifCB|MDD0c{A3OCCvZz;r[{wheG9iYnnkJIFldWmwaYP0[ZJm\CCob4KgNVAh\GG7czDt[YF{fXKnZDDvckBl[XliOUC= NEjCRos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
KARPAS299 M2Lkd2Z2dmO2aX;uJIF{e2G7 M1TXU|IhcHK| NHezcJNKdmirYnn0bY9vKG:oIF7QUU9CVEtiYYX0c5Bpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDLRXJRSVN{OUmgZ4VtdHNiYYSgeoVzgSCub4egZ49v[2WwdILheIlwdiCjZoTldkAzKGi{czDifUBY\XO2ZYLuJIJtd3RiYX7hcJl{cXN? M3;rZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
NCI-H2228 M4Lhe2Z2dmO2aX;uJIF{e2G7 M1fx[lIhcHK| MlfNTY5pcWKrdHnvckBw\iCQUF2vRWxMKGG3dH;wbI9{eGixconsZZRqd25iaX6gbJVu[W5iTlPJMWgzOjJ6IHPlcIx{KGG2II\ldpkhdG:5IHPvcoNmdnS{YYTpc44h[W[2ZYKgNkBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ NWXUcXljRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
Cyclin A1 / Cyclin E1 / p27 / p21; 

PubMed: 26735175     


Expression of cell cycle regulatory proteins (p21, p27, Cyclin A1, and Cyclin E1) was validated by Western Blot 24h after treatment with entrectinib. Gapdh was used as a control of proper protein loading. Numbers indicate concentration of entrectinib (e; 䲧疝Ỵ疞㧀疜膉痘 

p-ALK / ALK / p-ERK / ERK / p-STAT3 / STAT3; 

PubMed: 26735175     


Using entrectinib (e) IC50 defined for 48h, Eventual change of ALK downstream pathway after treatment with entrectinib was validated by Western blot. 

pTrkA-Y490 / TrkA / p-PLCγ-Y783 / PLCγ ; 

PubMed: 28903424     


Western blot analysis of the changes in phosphorylation levels of TRKA and its downstream transducer PLCγ 2 hours post entrectinib and crizotinib treatment in Ba/F3-SCYL3-NTRK1 cells.

pAKT / AKT; 

PubMed: 26172300     


Western blot demonstrating Inhibition of the phosphorylation of the ALK protein and other downstream signal molecules in the EML4-ALK CRC patient tumor derived cell line after inhibition by crizotinib or entrectinib.

26735175 28903424 26172300
Growth inhibition assay
Cell viability ; 

PubMed: 26172300     


Inhibition of the growth of the EML4-ALK CRC patient derived tumor cells with 1 μM crizotinib or 1 μM entrectinib.

26172300
体内研究 In mice bearing Karpas-299 and SR-786 xenografts, Entrectinib (p.o.) induces complete tumor regression. In NPM-ALK transgenic mice, Entrectinib induces complete regression of tumor masses observed in the thymus and in lymph nodes. [2] In the NB xenograft model, Entrectinib cotreatment enhanced the efficacy of conventional chemotherapy. [3]

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)

溶解度 (25°C)

体外 DMSO 100 mg/mL (178.36 mM)
Ethanol 75 mg/mL (133.77 mM)
Water Insoluble

* 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 560.64
化学式

C31H34F2N6O2

CAS号 1108743-60-7
储存条件 粉状
溶于溶剂
别名 NMS-E628

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
NCT04551495 Recruiting Drug: Entrectinib|Drug: Letrozole|Drug: Goserelin Invasive Lobular Breast Carcinoma|ER+ Breast Cancer|HER2-negative Breast Cancer Jules Bordet Institute|Hoffmann-La Roche January 14 2021 Phase 2
NCT04226833 Recruiting Drug: entrectinib Hepatic Insufficiency Hoffmann-La Roche February 11 2020 Phase 1
NCT03796013 Completed Drug: Entrectinib Form A|Drug: Entrectinib Form C Healthy Volunteers Genentech Inc. January 10 2019 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

Trk receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID