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17篇:

客户使用该产品的4个实验数据:

  • Tumor cells were treated with entrectinib (10 nmol/L) for 4 hours or c-PARP for 48 hours, and harvested lysates were assessed by Western blotting. Data shown are representative of three independent experiments with similar results.

    Clin Cancer Res, 2018, 24(10):2357-2369. Entrectinib (RXDX-101) purchased from Selleck.

  • (A) We transfected the EGFP/Eluc gene into KM12SM cells to establish KM12SM/Eluc cells. KM12SM/Eluc cells were inoculated into the brain of SCID mice. The mice were treated daily with or without entrectinib (15 mg/kg) for 37 days until the bioluminescence increased. Mean ± SE of total flux are shown in the lower panel. Then, the entrectinib-treated brain tumor was harvested at the point indicated by the orange triangle and cultured in vitro. The expanded tumor cells were named KM12SM-ER. (B) The sensitivity of KM12SM-ER and KM12SM cells to entrectinib was determined through cell viability assays, using a CCK-8 kit. The data (mean ± standard deviation [SD] of triplicate cultures) shown are representative of three independent experiments with similar results. (C) Tumor cells were treated with entrectinib (10 nmol/L) for 4 h or c-PARP for 48 h, and harvested lysates were assessed by western blotting. Data shown are representative of three independent experiments with similar results.

    Clin Cancer Res, 2018, doi: 10.1158/1078-0432.CCR-17-1623. Entrectinib (RXDX-101) purchased from Selleck.

  • KM12C and KM12SM cells were treated with crizotinib (1 μmol/L) or entrectinib (1 μmol/L) for 2 h. Immunoblots of cell lysates from these treated cell lines are shown. The data are representative of three independent experiments, showing similar results.

    Cancer Med, 2017, 6(12):2972-2983. Entrectinib (RXDX-101) purchased from Selleck.

  • The effect of kinase inhibitors on signal transduction in human cancer cell lines in vitro. H1975 cells were treated with osimertinib (1 μmol/L) for 2 h. NUGC4 cells were treated with crizotinib (1 μmol/L) for 2 h, and then stimulated with HGF (50 ng/mL) for 10 min. KM12C and KM12SM cells were treated with crizotinib (1 μmol/L) or entrectinib (1 μmol/L) for 2 h. Immunoblots of cell lysates from these treated cell lines are shown.

    Cancer Med, 2017, 6(12):2972-2983. Entrectinib (RXDX-101) purchased from Selleck.

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
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BAF3 NE\XfZJHfW6ldHnvckBie3OjeR?= NEDsZmw4OiCqcoO= NE\4cYVKdmirYnn0bY9vKG:oIHj1cYFvKFSHTDCoN|M3KHKnc3nkeYV{MSCodYPl[E1VWkuDIDi0OFAhfG9iN{m2JJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCvb4Xz[UBDSUZ|IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JINmdGxidHn0[ZIu\2yxIHHzd4F6NCCLQ{WwJF0hOC5yMEOg{txONg>? MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
BAF3 M3LCNmZ2dmO2aX;uJIF{e2G7 MXW3NkBpenN? NH3md5lKdmirYnn0bY9vKG:oIHj1cYFvKFSHTDCoN|M3KHKnc3nkeYV{MSCodYPl[E1VWkuFIDi0OVQhfG9iOEK1JJJme2mmdXXzLUApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCvb4Xz[UBDSUZ|IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JINmdGxidHn0[ZIu\2yxIHHzd4F6NCCLQ{WwJF0hOC5yMEOg{txONg>? M1T0TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
BAF3 MVLGeY5kfGmxbjDhd5NigQ>? NHjEWoE4OiCqcoO= NUDrcFQyUW6qaXLpeIlwdiCxZjDoeY1idiCWRVygLFM{PiC{ZYPp[JVmeyliZoXz[YQuWk:VMTCoNVg6OSC2bzCyN|Q4KHKnc3nkeYV{MSBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDtc5V{\SCEQV[zJINmdGy|IHHzd4V{e2WmIHHzJINmdGxiZ4Lve5RpKGmwaHnibZRqd25iYX\0[ZIhPzJiaILzJIJ6KGOnbHygeIl1\XJvZ3zvJIF{e2G7LDDJR|UxKD1iMD6wNFUh|ryPLh?= MnPqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
KM12 NYHnWXZGSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NEL4fXY4OiCqcoO= M{njTmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS12xNkBk\WyuczDlfJBz\XO|aX7nJHRTU0FicILveIVqdiCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBk\WyuIITpeIVzNWeubzDhd5NigSxiSVO1NEA:KDBwMEG3JO69VS5? NWfVPHhnRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
SU-DHL1 M1XBRmFvfGmycn;sbYZmemG2aY\lJIF{e2G7 MoHtO|IhcHK| NYDQWHN3SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTWU1FUExzIHPlcIx{KGW6cILld5NqdmdiQVzLJJBzd3SnaX6gbY5kfWKjdHXkJIZweiB5MjDodpMh[nliY3XscEB1cXSncj3ncI8h[XO|YYmsJGlEPTBiPTCwMlAzPCEQvF2u MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
BAF3 NHTCWpFHfW6ldHnvckBie3OjeR?= MV23NkBpenN? M3PKfmlvcGmkaYTpc44hd2Zid3ns[EB1gXCnIFXNUFQuSUyNIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJI1wfXOnIFLBSlMh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliY3XscEB1cXSncj3ncI8h[XO|YYmsJGlEPTBiPTCwMlAzQCEQvF2u M3X2dFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
KARPAS299 NWD4OGwySW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MojyO|IhcHK| NGDQUYxCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvBVnBCWzJ7OTDj[YxteyCrbnP1ZoF1\WRiZn;yJFczKGi{czDifUBk\WyuIITpeIVzNWeubzDhd5NigSxiSVO1NEA:KDBwMEOxJO69VS5? Mk\IQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
SUP-M2 MnjuRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NIXieI84OiCqcoO= NUnnb3ZNSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTWXAuVTJiY3XscJMh\XiycnXzd4lv\yCDTFugdJJwfGWrbjDpcoN2[mG2ZXSg[o9zKDd{IHjyd{BjgSClZXzsJJRqfGW{LXfsc{Bie3OjeTygTWM2OCB;IECuNFQyKM7:TT6= NE[4NlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
BAF3 MlzOSpVv[3Srb36gZZN{[Xl? NH[0WFI4OiCqcoO= MmPQTY5pcWKrdHnvckBw\iCHTVy0MWFNUyCOMUG5Om0hdXW2YX70JEh2dmuwb4fuJI9zcWerbjmg[ZhxemW|c3XkJIlvKG2xdYPlJGJCTjNiY3XscJMh[XO|ZYPz[YQh[XNiY3XscEBoem:5dHigbY5pcWKrdHnvckBi\nSncjC3NkBpenNiYomgZ4VtdCC2aYTldk1odG9iYYPzZZktKEmFNUCgQUAxNjB4NzFOwG0v Ml\EQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
NCI-H2228 MXnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NWHicnBQPzJiaILz MWnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE6FST3INlIzQCClZXzsd{BmgHC{ZYPzbY5oKEGOSzDwdo91\WmwIHnuZ5Vj[XSnZDDmc5IhPzJiaILzJIJ6KGOnbHygeIl1\XJvZ3zvJIF{e2G7LDDJR|UxKD1iMD6wOlgh|ryPLh?= NWfSSZM2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
MV411 NUjlflVUSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NGfnToI4OiCqcoO= M3u1NWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTW[0NVEh[2WubIOgbY5kfWKjdHXkJIZweiB5MjDodpMh[nliY3XscEB1cXSncj3ncI8h[XO|YYmsJGlEPTBiPTCwMlA5OSEQvF2u M364VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
SR786 MV7BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MY[3NkBpenN? MWnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFOUN{i2JINmdGy|IHX4dJJme3OrbnegRWxMKHC{b4TlbY4hcW6ldXLheIVlKG[xcjC3NkBpenNiYomgZ4VtdCC2aYTldk1odG9iYYPzZZktKEmFNUCgQUAxNjB6MTFOwG0v NGn3PJk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
BAF3 MnnhSpVv[3Srb36gZZN{[Xl? NFnNSHE4OiCqcoO= M2HWcmlvcGmkaYTpc44hd2ZiRV3MOE1CVEtiR{GyNFJTKG23dHHueEApfW6tbn;3ckBwemmpaX6pJIV5eHKnc4Pl[EBqdiCvb4Xz[UBDSUZ|IHPlcIx{KGG|c3Xzd4VlKGG|IHPlcIwh\3Kxd4ToJIlvcGmkaYTpc44h[W[2ZYKgO|IhcHK|IHL5JINmdGxidHn0[ZIu\2yxIHHzd4F6NCCLQ{WwJF0hOC56OUeg{txONg>? NE\ld2Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
BA/F3 NIqwV4VEgXSxdH;4bYNqfHliYYPzZZk> NXPnPFJXPzJiaILz NF3B[mtEgXSxdH;4bYNqfHliYXfhbY5{fCCvb4Xz[UBKVC1|IHTldIVv\GWwdDDCRU9HOyClZXzsd{BqdmO3YnH0[YQh\m:{IEeyJIhzeyCkeTDj[YxtKHSrdHXyMYdtdyCjc4PhfUwhUUN3MDC9JFIvOTB2IN88UU4> MkHXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
KM12 M{T0eGZ2dmO2aX;uJIF{e2G7 MXSyJIhzew>? MnTjTY5pcWKrdHnvckBw\iCWUF2zMXRTU0FicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEuPMUKgZ4VtdHNiYYSgcI94KGOxbnPlcpRz[XSrb36gZYZ1\XJiMjDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NWXVZ5dJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
KM12 MofaSpVv[3Srb36gZZN{[Xl? NXHCe|NkOiCqcoO= M{OxVGlvcGmkaYTpc44hd2ZiVGDNN{1VWkuDIIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCNTUGyJINmdGy|IHHzd4V{e2WmIHHzJJN2eHC{ZYPzbY9vKG:oIF3BVGsheGixc4Doc5J6dGG2aX;uJIF1KGyxdzDjc45k\W62cnH0bY9vKGGodHXyJFIhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NEe0Wm49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
KM12 Mnu3SpVv[3Srb36gZZN{[Xl? NFfZWY8zKGi{cx?= NYTCO456UW6qaXLpeIlwdiCxZjDUVG0{NVSUS1GgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFvNNVIh[2WubIOgZZN{\XO|ZXSgZZMhe3WycILld5Nqd25ib3[gVGxE\2GvbXGxJJBpd3OyaH;yfYxifGmxbjDheEBtd3diY3;uZ4VvfHKjdHnvckBi\nSncjCyJIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> NGHYTJc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
KM12 Mmj2SpVv[3Srb36gZZN{[Xl? M2jKNlIhcHK| NEjTZ4FKdmirYnn0bY9vKG:oIGTQUVMuXFKNQTDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iS12xNkBk\WyuczDhd5Nme3OnZDDhd{B{fXCycnXzd4lwdiCxZjDBT3QheGixc4Doc5J6dGG2aX;uJIF1KGyxdzDjc45k\W62cnH0bY9vKGGodHXyJFIhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
KM12 MknsSpVv[3Srb36gZZN{[Xl? M3W4PFIhcHK| MlT2TY5pcWKrdHnvckBw\iCWUF2zMXRTU0FicHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKEuPMUKgZ4VtdHNiYYPz[ZN{\WRiYYOgd5VxeHKnc4Ppc44hd2ZiU{[gdIhwe3Cqb4L5cIF1cW:wIHH0JIxwfyClb37j[Y51emG2aX;uJIFnfGW{IEKgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> MlL0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
KARPAS299 NEnWUnRHfW6ldHnvckBie3OjeR?= MVe2NEBu\y:tZx?= MYexNkBpenN? M1;udmV5KH[rdn:gbY5pcWKrdHnvckBw\iCQUF2tRWxMKHCqb4PwbI9zgWyjdHnvckBqdiCVQ1nEJI1wfXOnIIjlco9oemGodHXkJJdqfGhiaIXtZY4hU0GUUFHTNlk6KGOnbHzzJIF1KDZyIH3nM4toNCCybzDh[I1qdmm|dHXy[YQh[XNic3nu[4xmKGSxc3WgcYVie3W{ZXSgZYZ1\XJiMUKgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> NYPLNolRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
KARPAS299 Mlz6SpVv[3Srb36gZZN{[Xl? Mof2OlAhdWdxa3e= NF[1WXEyQCCqcoO= NVn0cVg5TXhidnn2c{BqdmirYnn0bY9vKG:oIF7QUU1CVEticHjvd5Bpd3K7bHH0bY9vKGmwIGPDTWQhdW:3c3WgfIVvd2e{YX\0[YQhf2m2aDDoeY1idiCNQWLQRXMzQTliY3XscJMh[XRiNkCgcYcwc2duIIDvJIFldWmwaYP0[ZJm\CCjczDzbY5odGViZH;z[UBu\WG|dYLl[EBi\nSncjCxPEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ MlrCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
KARPAS299 MULGeY5kfGmxbjDhd5NigQ>? M4\sb|YxKG2pL3vn MYqxNkBpenN? MXTFfEB3cX[xIHnubIljcXSrb36gc4YhVlCPLVHMT{BxcG:|cHjvdplt[XSrb36gbY4hW0OLRDDtc5V{\SC6ZX7v[5Ji\nSnZDD3bZRpKGi3bXHuJGtCWlCDU{K5PUBk\WyuczDhd5Nme3OnZDDhd{B{fXCycnXzd4lwdiCxZjDTWGFVOyCyaH;zdIhwenmuYYTpc44h[XRiNkCgcYcwc2duIIDvJIFldWmwaYP0[ZJm\CCjczDzbY5odGViZH;z[UBu\WG|dYLl[EBi\nSncjCxNkBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
KARPAS299 MYPGeY5kfGmxbjDhd5NigQ>? NGLWNZc3OCCvZz;r[y=> MWOxPEBpenN? MXHJckB3cX[xIHnubIljcXSrb36gc4YhVlCPLVHMT{BxcG:|cHjvdplt[XSrb36gbY4hW0OLRDDtc5V{\SC6ZX7v[5Ji\nSnZDD3bZRpKGi3bXHuJGtCWlCDU{K5PUBk\WyuczDhd5Nme3OnZDDhd{B{fXCycnXzd4lwdiCxZjDTWGFVOyCyaH;zdIhwenmuYYTpc44h[XRiNkCgcYcwc2duIIDvJIFldWmwaYP0[ZJm\CCjczDzbY5odGViZH;z[UBu\WG|dYLl[EBi\nSncjCxPEBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
NCI-H2228 NWLwZ|R{SW62aYT1cY9zKGG|c3H5 M33hWVMxKHSxIE[wJI1oN2up MlvJNVAh\GG7cx?= MonvRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgzOjJ6IHPlcIx{KHinbn;ndoFnfGWmIHnuJIF1cHmvaXOgcpUwdnVibX;1d4Uh[XO|ZYPz[YQh[XNidIXtc5Ih\3Kxd4ToJIlvcGmkaYTpc44h[XRiM{CgeI8hPjBibXevb4ctKHCxIHLp[EBi\G2rbnnzeIVz\WRiZn;yJFExKGSjeYO= MkLCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
NCI-H2228 Mon5SpVv[3Srb36gZZN{[Xl? MlX1OlAhdWdxa3e= Mn3ZNVIhcHK| M{HyTmV5KH[rdn:gbY5pcWKrdHnvckBw\iCHTVy0MWFNUyCyaH;zdIhwenmuYYTpc44hcW5iYYTofY1q[yCwdT;ueUBud3W|ZTD4[Y5w\3KjZoTl[EB4cXSqIHj1cYFvKE6FST3INlIzQCClZXzsd{BifCB4MDDt[{9s\yxicH:gZYRucW6rc4TldoVlKGG|IIPpcodt\SCmb4PlJI1m[XO3cnXkJIFnfGW{IEGyJIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzByM{e2NUc,OjdyMEO3OlE9N2F-
NCI-H2228 NHW1fHlHfW6ldHnvckBie3OjeR?= M2XGelYxKG2pL3vn M3nVXFE5KGi{cx?= MWrFfEB3cX[xIHnubIljcXSrb36gc4YhTU2OND3BUGsheGixc4Doc5J6dGG2aX;uJIlvKGG2aIntbYMhdnVxboWgcY92e2VieHXuc4dz[W[2ZXSge4l1cCCqdX3hckBPS0lvSEKyNlgh[2WubIOgZZQhPjBibXevb4ctKHCxIHHkcYlvcXO2ZYLl[EBieyC|aX7ncIUh\G:|ZTDt[YF{fXKnZDDh[pRmeiBzODDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz M1TvN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ5MECzO|YyLz5{N{CwN|c3OTxxYU6=
NCI-H2228 NYHXWGw2TnWwY4Tpc44h[XO|YYm= MWq2NEBu\y:tZx?= NVnNXoNlOTJiaILz NXm3T2UzTXhidnn2c{BqdmirYnn0bY9vKG:oIFXNUFQuSUyNIIDoc5NxcG:{eXzheIlwdiCrbjDheIh6dWmlIH71M452KG2xdYPlJJhmdm:pcnHmeIVlKHerdHigbJVu[W5iTlPJMWgzOjJ6IHPlcIx{KGG|c3Xzd4VlKGG|IIP1dJBz\XO|aX;uJI9nKEGNVDDwbI9{eGixconsZZRqd25iYYSgOlAhdWdxa3esJJBwKGGmbXnubZN1\XKnZDDhd{B{cW6pbHWg[I9{\SCvZXHzeZJm\CCjZoTldkAyOiCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m| NVrtbpJ3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
NCI-H2228 M2DhUWZ2dmO2aX;uJIF{e2G7 NEXTN3A3OCCvZz;r[y=> NXvhd2pHOThiaILz M3jqemV5KH[rdn:gbY5pcWKrdHnvckBw\iCHTVy0MWFNUyCyaH;zdIhwenmuYYTpc44hcW5iYYTofY1q[yCwdT;ueUBud3W|ZTD4[Y5w\3KjZoTl[EB4cXSqIHj1cYFvKE6FST3INlIzQCClZXzsd{Bie3Onc4Pl[EBieyC|dYDwdoV{e2mxbjDv[kBCU1RicHjvd5Bpd3K7bHH0bY9vKGG2IE[wJI1oN2upLDDwc{Bi\G2rbnnzeIVz\WRiYYOgd4lv\2ynIHTvd4UhdWWjc4Xy[YQh[W[2ZYKgNVghcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NV:yNWNJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkewNFM4PjFpPkK3NFA{PzZzPD;hQi=>
KARPAS299 NUnhc5Y5SW62aYT1cY9zKGG|c3H5 MYezNEB1dyB4MDDt[{9s\w>? NUjGboR4OTBiZHH5dy=> NGHEbHpCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLRXJRSVN{OUmgZ4VtdHNieHXuc4dz[W[2ZXSgbY4hW0OLRDDtc5V{\SCjc4Pld5Nm\CCjczD0eY1weiCpcn;3eIghcW6qaXLpeIlwdiCjdDCzNEB1dyB4MDDt[{9s\yxicH:gZollKGGmbXnubZN1\XKnZDDmc5IhOTBiZHH5dy=> MnHHQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=
KARPAS299 NX\3WVE3SW62aYT1cY9zKGG|c3H5 NVP1SphLOzBidH:gOlAhdWdxa3e= NHjiWoYyOCCmYYnz M3HwVWFvfGm2dX3vdkBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvBVnBCWzJ7OTDj[YxteyC6ZX7v[5Ji\nSnZDDpckBUS0mGIH3veZNmKGG|c3Xzd4VlKGG|IIT1cY9zKG[{ZXWgZ5Vz\WRibX;1d4Uh[XRiM{CgeI8hPjBibXevb4ctKHCxIHLp[EBi\G2rbnnzeIVz\WRiZn;yJFExKGSjeYOgcYVie3W{ZXSgc44h\GG7IEmw NHXvS4w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
KARPAS299 MVvGeY5kfGmxbjDhd5NigQ>? MnrhNkBpenN? M4nqcWlvcGmkaYTpc44hd2ZiTmDNM2FNUyCjdYTvdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFvBVnBCWzJ7OTDj[YxteyCjdDD2[ZJ6KGyxdzDjc45k\W62cnH0bY9vKGGodHXyJFIhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? NGXBN3o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{CwN|c3OSd-MkewNFM4PjF:L3G+
NCI-H2228 MVPGeY5kfGmxbjDhd5NigQ>? M3HrTlIhcHK| M1jzbGlvcGmkaYTpc44hd2ZiTmDNM2FNUyCjdYTvdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIF7DTU1JOjJ{ODDj[YxteyCjdDD2[ZJ6KGyxdzDjc45k\W62cnH0bY9vKGGodHXyJFIhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqew>? MlvnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdyMEO3OlEoRjJ5MECzO|YyRC:jPh?=

... 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、MSDS / 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、MSDS / 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