Nilotinib (AMN-107)

For research use only. Not for use in humans.

目录号:S1033 中文名称:尼洛替尼

Nilotinib (AMN-107) Chemical Structure

CAS No. 641571-10-0

Nilotinib (AMN-107)是一种特异性BCR-ABL抑制剂,在小鼠骨髓祖细胞中IC50低于30 nM。Nilotinib (AMN-107)可通过激活AMPK来诱导自噬。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 749.92 现货
RMB 810.81 现货
RMB 1040.13 现货
RMB 1720.01 现货
RMB 3005.73 现货
RMB 3864.35 现货
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客户使用Selleck生产的Nilotinib (AMN-107)发表文献109篇:

产品安全说明书

Bcr-Abl抑制剂选择性比较

生物活性

产品描述 Nilotinib (AMN-107)是一种特异性BCR-ABL抑制剂,在小鼠骨髓祖细胞中IC50低于30 nM。Nilotinib (AMN-107)可通过激活AMPK来诱导自噬。
特性 Nilotinib 是Abl选择性抑制剂,与BCR-ABL的ATP结合位点相互作用。
靶点
Bcr-Abl [1]
(Murine myeloid progenitor cells)
<30 nM
体外研究

Nilotinib 作用于激活的HSCs,抑制增殖,迁移,和肌动蛋白形成,及 α-SMA和胶原的表达。Nilotinib 诱导HSCs凋亡,与bcl-2 表达降低相关,且提高p53 表达, PARP分裂,以及提高 PPARγ 和TRAIL-R表达。Nilotinib 也诱导细胞周期停滞,伴随着p27 的表达和cyclin D1的下调提高。Nilotinib 不仅抑制PDGFR的激活,也 通过Src抑制TGFRII。Nilotinib 显著抑制PDGF和 TGFβ刺激的ERK 和Akt磷酸化。而且, Nilotinib作用于人HSCs,抑制PDGF和TGFβ-激活的Abl磷酸化形式。 [2]Nilotinib抑制最抗 Imatinib的BCR-ABL突变,除了T315I。[3] Nilotinib 抑制PDGF-DD调节的 ERK1/2激活,基本的和PDGF-DD调节的 PDGFR-β和AKT激活,及schwannoma细胞增殖。 Nilotinib 比Imatinib更有效,发挥其最大抑制效果时的浓度比稳态血浆水平还低。[4] Nilotinib也显著降低TGF-β1和血小板衍生的生长因子(PDGF)基因表达水平。Nilotinib处理也显著抑制PDGF诱导的肺纤维细胞增殖。[5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EoL-1-cell M{KzfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LaZWlEPTB;MD6wNFAyPDRizszN NYLGT|hIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV3OE[zM{c,W0GQR1XSQE9iRg>?
KU812 M2PZeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XaOGlEPTB;MD6wNFI1QCEQvF2= NGTHUXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTV6NkOvK|5USU6JRWK8M4E,
EM-2 NYPz[41CT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUSze5Q6UUN3ME2wMlAxPDFizszN NYOz[W86RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV3OE[zM{c,W0GQR1XSQE9iRg>?
LAMA-84 NHLOWYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVvPUlBZUUN3ME2wMlAxPDlizszN NHfPSXY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTV6NkOvK|5USU6JRWK8M4E,
MEG-01 M13DW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvwTWM2OD1yLkCwPFI5KM7:TR?= M2XtWVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2PTh4Mz:nQnNCVkeHUkyvZV4>
BV-173 NVPtco04T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkXzTWM2OD1yLkCxNFg6KM7:TR?= MW[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVU5PjNxJ{7TRW5ITVJ:L3G+
KASUMI-1 M4\wXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTBwMEK0NVMh|ryP M4\y[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2PTh4Mz:nQnNCVkeHUkyvZV4>
NB7 Mm[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTBwMUO0N|kh|ryP NFnHUVc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTV6NkOvK|5USU6JRWK8M4E,
BHT-101 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlX1TWM2OD1yLk[0NlY{KM7:TR?= MmL0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlU2QDZ|Lze+V2FPT0WUPD;hQi=>
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HMV-II Mlq4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2qwNWlEPTB;MD63OFg4PCEQvF2= M2Ph[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2PTh4Mz:nQnNCVkeHUkyvZV4>
NKM-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkX4TWM2OD1yLkmwNVUh|ryP M{DUbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2PTh4Mz:nQnNCVkeHUkyvZV4>
LB2241-RCC M3H5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;iVYdKSzVyPUGuNFIzOjhizszN NY\qenRxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV3OE[zM{c,W0GQR1XSQE9iRg>?
NCI-H1703 NH\G[nlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3lTWM2OD1zLkG4PFch|ryP M2P5bFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2PTh4Mz:nQnNCVkeHUkyvZV4>
BE-13 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4e5WGlEPTB;MT6yO|QyPiEQvF2= NWnMNJloRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV3OE[zM{c,W0GQR1XSQE9iRg>?
ACN M1[0bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLuTWM2OD1zLkW1NFc4KM7:TR?= M3\LcVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2PTh4Mz:nQnNCVkeHUkyvZV4>
A204 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlf3TWM2OD1zLkW3NlA2KM7:TR?= M1HIVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2PTh4Mz:nQnNCVkeHUkyvZV4>
HOP-62 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTFwOEKwO|ch|ryP M2PufVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2PTh4Mz:nQnNCVkeHUkyvZV4>
H9 M3XJcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3[5ZWlEPTB;Mj63N|c6OyEQvF2= M2PrN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2PTh4Mz:nQnNCVkeHUkyvZV4>
HCC1806 M33sdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnz0TWM2OD1{Lke0N|I4KM7:TR?= NVjTSHozRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV3OE[zM{c,W0GQR1XSQE9iRg>?
NOS-1 NWDMOFVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF35ZlRKSzVyPUKuPFcyODJizszN MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVU5PjNxJ{7TRW5ITVJ:L3G+
RS4-11 MnrjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTJwOUC2NlMh|ryP NHzoOGo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTV6NkOvK|5USU6JRWK8M4E,
JAR NF\RXVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPlTWM2OD1{LkmyNFg1KM7:TR?= NVHJXpRtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV3OE[zM{c,W0GQR1XSQE9iRg>?
T98G NXzJXoJiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYTGZpptUUN3ME2zMlAyOzF|IN88US=> MUe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyyOVU5PjNxJ{7TRW5ITVJ:L3G+
NCI-SNU-1 MlTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPJdVJKSzVyPUOuOFAxQTJizszN NWrV[XJ7RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV3OE[zM{c,W0GQR1XSQE9iRg>?
SK-MEL-1 Mle5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTNwNEOwNlkh|ryP NFzsb4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTV6NkOvK|5USU6JRWK8M4E,
L-363 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTNwNkGxNFch|ryP NVHBV5FtRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV3OE[zM{c,W0GQR1XSQE9iRg>?
SW982 Mom2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3wZo1KSzVyPUOuOlQyPjlizszN M323OlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2PTh4Mz:nQnNCVkeHUkyvZV4>
HT-1080 NEL5NVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX:2fGZ2UUN3ME2zMlkyPzd3IN88US=> NEPVN4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTV6NkOvK|5USU6JRWK8M4E,
G-402 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIT6TmdKSzVyPUSuN|EzODNizszN MoDoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlU2QDZ|Lze+V2FPT0WUPD;hQi=>
HOS NY\Oc|lGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXO1[ZM2UUN3ME20MlgxOjh{IN88US=> MnTBQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNlU2QDZ|Lze+V2FPT0WUPD;hQi=>
SK-NEP-1 M4jlemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTRwOEOxPVEh|ryP NHrZOI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwzPTV6NkOvK|5USU6JRWK8M4E,
HAL-01 NF\JXnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYf5VXA2UUN3ME20Mlg5OjR{IN88US=> NVr0cHNJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV3OE[zM{c,W0GQR1XSQE9iRg>?
SBC-1 MlP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnjOZBOUUN3ME20MlkxQTB5IN88US=> M3PUXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFI2PTh4Mz:nQnNCVkeHUkyvZV4>
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K-562 M172R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTVwOUCzOkDPxE1? NYH3b2pVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOjV3OE[zM{c,W0GQR1XSQE9iRg>?
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A673 MmewdWhVWyCjc4PhfS=> NXz6OWV{eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSTZ5MzDj[Yxteyl? MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
LAN-5 NEX1UnRyUFSVIHHzd4F6 MkO3dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgUGFPNTViY3XscJM> NHH4NHc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-37 NEPzSXVyUFSVIHHzd4F6 M3LxfZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGJVNTN5IHPlcIx{ NUftcmdwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh41 NVL3[nh6eUiWUzDhd5NigQ>? MXLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSbFQyKGOnbHzz NGfIb4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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OHS-50 NFj6VYVyUFSVIHHzd4F6 MUXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDPTHMuPTBiY3XscJM> NFvabmY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-SH MX\xTHRUKGG|c3H5 MlfDdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2VSDDj[Yxtew>? M1iyTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AMPKα / AMPKα / p-AMPKβ1 / AMPKγ2 / p-LKB1 / LKB1 / CaMKIIβ ; 

PubMed: 23677989     


Dose-dependent analysis of AMPK-related molecules in HCC cells. Cells were exposed to nilotinib at the indicated concentrations for 24 h.

DNMT1 / DNMT3a / DNMT3b ; 

PubMed: 28720666     


Kasumi-1 or MV4-11 cells were treated for 24 h with the indicated doses of nilotinib and subjected western blot analysis to detect the expression levels of DNMT1, DNMT3a, DNMT3b.

pABL1 / p-NF-κB1 / NF-κB / STAT3 / p-STAT3 / IL-1β / IL-6 / COX2 ; 

PubMed: 31396300     


ABL1 regulated the inflammation signaling pathway. Blocking activities of ABL1 with Imatinib and Nilotinib inhibits the inflammatory signaling pathway including activities of NF-κB1, STAT3, IL-1β, IL-6, and COX2.

23677989 28720666 31396300
Growth inhibition assay
Cell viability; 

PubMed: 23677989     


Dose-dependent effects of nilotinib on cell viability. HCC cells were treated with nilotinib at the indicated concentrations for 72 h. Cell viability was measured by MTT assay. Points, mean; bars, S.D. (n = 8). 

23677989
体内研究 Nilotinib 作用于CCl4和BDL诱导的纤维化,降低胶原沉积和α-SMA表达。 Nilotinib 可以诱导HSC发生凋亡,与bcl-2的下调相关。 [2] Nilotinib轻肺损伤和纤维化程度。Nilotinib 疗法在第14天和21天,显著降低羟脯氨酸水平 ,伴随着转化生长因子(TGF)-β1和 PDGFR-β表达水平降低。[5]

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)

细胞实验:[4]
- 合并
  • Cell lines: 人类原代Schwann 和schwannoma细胞
  • Concentrations: 1 μM -10 μM
  • Incubation Time: 72小时
  • Method: 人类原代 Schwann和 schwannoma细胞接种在预包被的96孔板上。加入Nilotinib,40分钟后,使用100 ng/mL PDGF-DD刺激处理,细胞培养72小时(3 天)。因为Nilotinib的半衰期为18小时, 每天新鲜补充的浓度为最初加入浓度的一半。除了DAPI染色和测定全部细胞数外, 使用更敏感和准确的 BrdU渗透法测定增殖细胞。 使用倒置荧光显微镜和200 ×放大倍率。计算全部细胞数(DAPI)和分裂细胞数(BrdU阳性)。计数每孔中的所有细胞。每孔中不同批次细胞的全部细胞数不同。
    (Only for Reference)
动物实验:[4]
- 合并
  • Animal Models: 雄性6周大的C57BL6小鼠
  • Dosages: 100 mg/kg
  • Administration: 口服饲喂
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 27 mg/mL (50.98 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):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
3mg/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 529.52
化学式

C28H22F3N7O

CAS号 641571-10-0
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、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
NCT04002674 Recruiting Drug: Placebo oral capsule|Drug: Nilotinib Oral Capsule Dementia With Lewy Bodies Georgetown University|National Institutes of Health (NIH) January 10 2020 Phase 2
NCT03942094 Recruiting Drug: Nilotinib Chronic Myeloid Leukemia Chronic Phase|Nilotinib Shenzhen Second People''s Hospital|Zhongshan City People''s Hospital|Affiliated Hospital of Guangdong Medical University|Huazhong University of Science and Technology Union Shenzhen Hospital|Dongguan People''s Hospital|Longgang District Central Hospital of Shenzhen June 1 2019 Phase 3
NCT03874858 Recruiting Drug: Nilotinib Chronic Myeloid Leukemia Novartis Pharmaceuticals|Novartis April 1 2019 Phase 2
NCT02108951 Terminated Drug: Nilotinib Philidelphia Positive Chronic Myeloid Leukaemia Novartis Pharmaceuticals|Novartis July 7 2014 Phase 3
NCT01735955 Active not recruiting Drug: AMN107 GIST and CML Novartis Pharmaceuticals|Novartis March 29 2013 Phase 4

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 would like to use AMN-107 for in vivo studies in mice, can you give me some suggestions about the in vivo formulation?

  • 回答:

    For in vivo study, we recommend to use 4% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 3mg/ml.

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Bcr-Abl Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID