Nilotinib (AMN-107)

For research use only. Not for use in humans.

Catalog No.S1033

60 publications

Nilotinib (AMN-107) Chemical Structure

Molecular Weight(MW): 529.52

Nilotinib (AMN-107) is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells.

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Selleck's Nilotinib (AMN-107) has been cited by 60 publications

Purity & Quality Control

Choose Selective Bcr-Abl Inhibitors

Biological Activity

Description Nilotinib (AMN-107) is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells.
Features A selective inhibitor of native and mutant Bcr-Abl.
Targets
Bcr-Abl [1]
(Murine myeloid progenitor cells)
<30 nM
In vitro

Nilotinib inhibits proliferation, migration, and actin filament formation, as well as the expression of α-SMA and collagen in activated HSCs. Nilotinib induces apoptosis of HSCs, which is correlated with reduced bcl-2 expression, increases p53 expression, cleavage of PARP, as well as increases expression of PPARγ and TRAIL-R. Nilotinib also induces cell cycle arrest, accompanied by increased expression of p27 and downregulation of cyclin D1. Interestingly, Nilotinib not only inhibits activation of PDGFR, but also TGFRII through Src. Nilotinib significantly inhibits PDGF and TGFβ-simulated phosphorylation of ERK and Akt. Furthermore, PDGF- and TGFβ-activated phosphorylated form(s) of Abl in human HSCs are inhibited by Nilotinib. [2] Nilotinib inhibits most imatinib-resistant Bcr-Abl mutations, except for T315I. [3] Nilotinib inhibits PDGF-DD-mediated ERK1/2 activation, basal and PDGF-DD-mediated activation of PDGFRβ and Akt, and schwannoma proliferation. Nilotinib is more potent than imatinib, exerting its maximal inhibitory effect at concentrations lower than steady-state trough plasma levels. [4] Nilotinib also significantly reduces the expression levels of the genes for TGF-β1 and platelet-derived growth factor (PDGF). Nilotinib treatment also significantly inhibits the PDGF-induced proliferation of lung fibroblasts. [5] Nilotinib inhibits the proliferation of Ba/F3 cells expressing p210- and p190-Bcr-Abl, or K562 and Ku-812F cells with IC50 values ≤12 nM. [6]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
EoL-1-cell MmjlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTBwMECwNVQ1KM7:TR?= M37K[XNCVkeHUh?=
KU812 NWTrb4RoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTyPW5KSzVyPUCuNFAzPDhizszN NU\INoJbW0GQR1XS
EM-2 Mo\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULveWRTUUN3ME2wMlAxPDFizszN M33XbHNCVkeHUh?=
LAMA-84 MmnPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{LyNGlEPTB;MD6wNFQ6KM7:TR?= NHP1e4tUSU6JRWK=
MEG-01 NHfMOXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFTUOItKSzVyPUCuNFA5OjhizszN MWLTRW5ITVJ?
BV-173 M{\NZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml2zTWM2OD1yLkCxNFg6KM7:TR?= NVj2Z4RQW0GQR1XS
KASUMI-1 NUDUeXpTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFLR[WZKSzVyPUCuNFI1OTNizszN M3zXbnNCVkeHUh?=
NB7 NInwV3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIn2cGlKSzVyPUCuNVM1OzlizszN NGe4fJhUSU6JRWK=
BHT-101 NEWyOm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvNdIhKSzVyPUCuOlQzPjNizszN MUXTRW5ITVJ?
CGTH-W-1 NFfr[XRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITnO3BKSzVyPUCuOlQ5PyEQvF2= MVjTRW5ITVJ?
HMV-II MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HNd2lEPTB;MD63OFg4PCEQvF2= NILwU4lUSU6JRWK=
NKM-1 NFT5Uo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1q5NmlEPTB;MD65NFE2KM7:TR?= NWnCdYRpW0GQR1XS
LB2241-RCC NX;idpNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\3PWlEPTB;MT6wNlIzQCEQvF2= NGniWpBUSU6JRWK=
NCI-H1703 MoLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTQRYdXUUN3ME2xMlE5QDdizszN MVfTRW5ITVJ?
BE-13 MorJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7jTWM2OD1zLkK3OFE3KM7:TR?= MVnTRW5ITVJ?
ACN MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYrJR|UxRTFwNUWwO|ch|ryP NYDPR2hLW0GQR1XS
A204 NGGyXXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPVTWM2OD1zLkW3NlA2KM7:TR?= NX3OXHlXW0GQR1XS
HOP-62 MnPHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPXTWM2OD1zLkiyNFc4KM7:TR?= Mke3V2FPT0WU
H9 NG\iTIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXHQeIdNUUN3ME2yMlc{Pzl|IN88US=> NFjH[YVUSU6JRWK=
HCC1806 NILyeFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfhUlVPUUN3ME2yMlc1OzJ5IN88US=> NYrWVFQ6W0GQR1XS
NOS-1 Mm[4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PyOWlEPTB;Mj64O|ExOiEQvF2= NVrKUIhZW0GQR1XS
RS4-11 MkH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPETWM2OD1{LkmwOlI{KM7:TR?= M2rIO3NCVkeHUh?=
JAR MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HQb2lEPTB;Mj65NlA5PCEQvF2= M4G4T3NCVkeHUh?=
T98G M4HQfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHXJVoZKSzVyPUOuNFE{OTNizszN NHHDXmhUSU6JRWK=
NCI-SNU-1 MnTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTNwNECwPVIh|ryP MUnTRW5ITVJ?
SK-MEL-1 MoHSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\xTWM2OD1|LkSzNFI6KM7:TR?= NYrsSmtTW0GQR1XS
L-363 M1fRcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DrVmlEPTB;Mz62NVExPyEQvF2= Mn;hV2FPT0WU
SW982 Mnn6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3[0VmlEPTB;Mz62OFE3QSEQvF2= NFT6R|ZUSU6JRWK=
HT-1080 M4\Mc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX;JR|UxRTNwOUG3O|Uh|ryP NEDZTpVUSU6JRWK=
G-402 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2qyVmlEPTB;ND6zNVIxOyEQvF2= M{nTXHNCVkeHUh?=
HOS MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVu5VnRLUUN3ME20MlgxOjh{IN88US=> M3fQUHNCVkeHUh?=
SK-NEP-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\Uc2lEPTB;ND64N|E6OSEQvF2= NVPlSmNxW0GQR1XS
HAL-01 Ml;IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTFTWM2OD12Lki4NlQzKM7:TR?= NUXRO5BOW0GQR1XS
SBC-1 MoflS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1L3SWlEPTB;ND65NFkxPyEQvF2= MV;TRW5ITVJ?
CTV-1 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mor4TWM2OD13LkS4PVM5KM7:TR?= NFzL[IFUSU6JRWK=
LCLC-103H NIDRZoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7tbZY6UUN3ME21Mlc4PDdzIN88US=> MWHTRW5ITVJ?
RVH-421 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkK2TWM2OD13Lke3OVM3KM7:TR?= NUi5PJltW0GQR1XS
K-562 M1HUN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHrK[mdKSzVyPUWuPVA{PiEQvF2= MkHxV2FPT0WU
CAL-33 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTQTWM2OD14LkOxN|U6KM7:TR?= NUm0TmtlW0GQR1XS
MDA-MB-361 NWrI[GpsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV[zNZlJUUN3ME22MlM{Pjl7IN88US=> NYH2R2R2W0GQR1XS
IGROV-1 NX\tZXdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF64NmlKSzVyPU[uOFcyQTFizszN NUX1Z3VxW0GQR1XS
NY MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHIc25KSzVyPU[uOVM2QTlizszN NV;OcVdTW0GQR1XS
Ramos-2G6-4C10 NEHjZYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXmTWM2OD14Lk[2PVMyKM7:TR?= NIjJOFNUSU6JRWK=
HuO9 M2nESmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTZwN{O5OlQh|ryP NVm1[od[W0GQR1XS
MS-1 NIW2OWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoLVTWM2OD15LkGxPVU{KM7:TR?= NIfSWoNUSU6JRWK=
RPMI-8226 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjiTWM2OD15LkK4Nlg4KM7:TR?= M3\hR3NCVkeHUh?=
HDLM-2 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTdwNECxOFkh|ryP MUnTRW5ITVJ?
D-566MG NYnwbHRRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nFVGlEPTB;Nz60O|E2PSEQvF2= Ml\sV2FPT0WU
SK-MEL-24 NGK3WJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTdwNkOzPVIh|ryP MofZV2FPT0WU
COLO-679 MkjPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFvlWXBKSzVyPUeuPVg3PzFizszN MnP4V2FPT0WU
EW-13 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRThwM{KwOVQh|ryP M3rJOXNCVkeHUh?=
A388 MorzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\2TWM2OD16LkO4OFgyKM7:TR?= MXTTRW5ITVJ?
UM-UC-3 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRThwNEO5OVYh|ryP NVLpdXFNW0GQR1XS
NUGC-3 NU\YcHNHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37tUmlEPTB;OD61N|U5OiEQvF2= MVrTRW5ITVJ?
COLO-668 MmS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mle1TWM2OD16LkW5OFkyKM7:TR?= MmP2V2FPT0WU
MOLT-4 M13PRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TjTGlEPTB;OD62NlM2OyEQvF2= NY[5ZppwW0GQR1XS
D-423MG MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRThwOEO3OVYh|ryP M1rYXnNCVkeHUh?=
CTB-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF32VVRKSzVyPUiuPFcyOjhizszN M4PISnNCVkeHUh?=
BCPAP M2izZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHkenhZUUN3ME25MlAzPTZ{IN88US=> NEn3WpFUSU6JRWK=
GCT NFrEVXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jCNmlEPTB;OT6wPVg{OSEQvF2= NWnUPIVpW0GQR1XS
ACHN NVy3NG9LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUD0bGNjUUN3ME25MlI{PjN{IN88US=> MV;TRW5ITVJ?
KYSE-520 MnnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnTjTWM2OD17LkOzOFgzKM7:TR?= M4jyenNCVkeHUh?=
LB771-HNC NUnwRZpxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIW2UYVKSzVyPUmuO|Y1QTdizszN NGLjZo5USU6JRWK=
MLMA Mn3CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjpTWM2OD1zMD6wNVMzKM7:TR?= MVrTRW5ITVJ?
HEC-1 MlfXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfUNFRKSzVyPUGwMlI5ODRizszN NF7McIVUSU6JRWK=
HL-60 NXezOmd5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTFyLk[4OVMh|ryP MVzTRW5ITVJ?
A101D M{jvS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1vlPGlEPTB;MUCuPFkzOyEQvF2= M2i2RXNCVkeHUh?=
A2058 MoKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3ERokyUUN3ME2xNE46OjR3IN88US=> Mln6V2FPT0WU
KARPAS-45 NXn2SJg6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHrTWM2OD1zMT6wOlM2KM7:TR?= MVTTRW5ITVJ?
697 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\yTWlEPTB;MUGuNlExOSEQvF2= Mon2V2FPT0WU
NCI-N87 NHzhc4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDqdmdKSzVyPUGxMlc4OzFizszN MYnTRW5ITVJ?
DSH1 M4rvZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLVcGJZUUN3ME2xNU44QTV|IN88US=> MmjBV2FPT0WU
HLE MlXiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HuemlEPTB;MUGuPFg{QSEQvF2= MoDIV2FPT0WU
NCI-H720 M1TSbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1fYUmlEPTB;MUKuOlgxOSEQvF2= M4LIW3NCVkeHUh?=
EW-3 Mnu1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTF{LkmzNFch|ryP NUfVbHF{W0GQR1XS
AGS MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfGWFBKSzVyPUGzMlA{PTFizszN NXXo[lVLW0GQR1XS
ES5 NFTxOIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHrTWM2OD1zMz6wOVEzKM7:TR?= NHjCO5pUSU6JRWK=
DB MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFHKT5pKSzVyPUGzMlMzPTZizszN NFXnN4hUSU6JRWK=
A4-Fuk NHnUfmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTodpZ6UUN3ME2xN{41OTB{IN88US=> NIfHdmtUSU6JRWK=
A427 Ml;US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MofzTWM2OD1zMz60PVczKM7:TR?= MlLGV2FPT0WU
MN-60 MnrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{DHd2lEPTB;MUOuOVg1OyEQvF2= M1K3d3NCVkeHUh?=
HCC2218 NEDCZ2tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTF|LkW4OVYh|ryP NHHO[XVUSU6JRWK=
MV-4-11 NE\MU3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnkbJpnUUN3ME2xN{45OTN5IN88US=> M17WfXNCVkeHUh?=
GI-1 NHTGRnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{W1OmlEPTB;MUSuNVE5PCEQvF2= NHHRSXVUSU6JRWK=
JVM-3 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnq3TWM2OD1zND6yOlU3KM7:TR?= NXfkfZNQW0GQR1XS
NCI-H2029 NH\jOXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDtNpNKSzVyPUG0MlI4OjdizszN M2qxZ3NCVkeHUh?=
TE-12 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\pTWM2OD1zND62NFQ3KM7:TR?= NFXid2dUSU6JRWK=
WM-115 NX[1e3RrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXaTFJKSzVyPUG1MlU3QDNizszN MoHvV2FPT0WU
BB65-RCC MnW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{[4XGlEPTB;MU[uNFI1OSEQvF2= NGfWdlJUSU6JRWK=
NCI-H1693 NEK1PHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\6TZNKSzVyPUG2MlM5ODJizszN NFfaWGxUSU6JRWK=
KARPAS-299 NHP0[ndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPLb29KSzVyPUG2MlYzODNizszN M{e5VnNCVkeHUh?=
UACC-257 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTF5LkC1PFIh|ryP NFPOWIJUSU6JRWK=
RKO NH3jZpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTF5Lk[0N|Mh|ryP MX;TRW5ITVJ?
HT-29 NGD5OYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3LbYdKSzVyPUG3Mlc5QDlizszN M1;iN3NCVkeHUh?=
ES7 M3rIeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIiwV3VKSzVyPUG4MlEyOjJizszN MlzGV2FPT0WU
DEL M4rkS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX3PUYR5UUN3ME2xPE4{OTd{IN88US=> MnnCV2FPT0WU
BT-549 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLyTWM2OD1zOD60NFkzKM7:TR?= M3P3XnNCVkeHUh?=
NCI-H1755 NX75PGJsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnTTWM2OD1zOD61O|I{KM7:TR?= M2TxSnNCVkeHUh?=
HCE-T M4\iSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LuS2lEPTB;MUiuPFM1OSEQvF2= M{fGRnNCVkeHUh?=
LU-139 MlLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPvSZRiUUN3ME2xPU4xPDV6IN88US=> NHTQb2hUSU6JRWK=
ECC10 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoH1TWM2OD1zOT6yOFc2KM7:TR?= NWnLVplXW0GQR1XS
769-P NXr6fJBkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnyOGhKSzVyPUG5MlY{OzVizszN MUfTRW5ITVJ?
BALL-1 Mnv4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NInrWodKSzVyPUG5MlY4PzVizszN MWHTRW5ITVJ?
LXF-289 NX;6XWhLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRTF7Lki5O|kh|ryP NUHLTIJjW0GQR1XS
TYK-nu NX\UU|RtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7HTWM2OD1zOT65N|E2KM7:TR?= NHjtNItUSU6JRWK=
NCI-H630 M2rld2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX[2dZZJUUN3ME2xPU46Ozd6IN88US=> NHjQTJdUSU6JRWK=
EW-18 MnW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTJyLkO4NFIh|ryP MXPTRW5ITVJ?
KYSE-150 NWf5W5dQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTJyLkewOFch|ryP M2nSUXNCVkeHUh?=
LOXIMVI M2Gybmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTzXpN[UUN3ME2yNE44PTh4IN88US=> MUHTRW5ITVJ?
HuP-T3 MmG0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTJzLkC4OVIh|ryP NIflZWZUSU6JRWK=
MFE-280 NUHXWpZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TRR2lEPTB;MkGuOVY4QSEQvF2= NV\jeG5NW0GQR1XS
SK-OV-3 M2XCNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTJzLki0NFgh|ryP MmjLV2FPT0WU
QIMR-WIL MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIi3[oVKSzVyPUKyMlA1PzhizszN MoPIV2FPT0WU
NCI-H69 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTJ{LkSyPVkh|ryP NGPPfItUSU6JRWK=
TE-5 M3rGWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTJ{LkS5OlUh|ryP M1PJRnNCVkeHUh?=
NCI-H1993 NXWxbYlLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7N[npCUUN3ME2yNk41QTdzIN88US=> MnL6V2FPT0WU
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NCI-H1770 M3L5cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3WwO2lEPTB;M{SuPVYyKM7:TR?= NIfMeXBUSU6JRWK=
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GP5d MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37abGlEPTB;M{iuPFY2OyEQvF2= NVTRdo9DW0GQR1XS
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RD M3WwSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPsOFJGUUN3ME2zPU42OjV6IN88US=> Mn\tV2FPT0WU
NCI-SNU-5 MoTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTN7Lk[5NVYh|ryP M2PKUnNCVkeHUh?=
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SK-MEL-28 NVj6coxnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TpRmlEPTB;NECuOlQ{PSEQvF2= NFPZOJBUSU6JRWK=
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HT-144 NFP2U|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTR{LkC1Olch|ryP M2LQcnNCVkeHUh?=
MFM-223 NX3Nc2FtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXWV|hKSzVyPUSyMlQxOiEQvF2= M1zRd3NCVkeHUh?=
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GAMG NX7FR|cxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\DW2xKSzVyPUSzMlQ2OTdizszN MY\TRW5ITVJ?
LU-135 M33HVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHmTWM2OD12ND6wPVI{KM7:TR?= M1TkRnNCVkeHUh?=
HCC1187 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2GwdGlEPTB;NESuPFI3OiEQvF2= NFLNVGpUSU6JRWK=
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D-392MG MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTEbGZKSzVyPUS1MlkzPTZizszN M1nzVXNCVkeHUh?=
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HSC-3 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTR5LkO2NFgh|ryP MXzTRW5ITVJ?
KM-H2 M{fPeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTR5Lk[wNFch|ryP NVWzSpZSW0GQR1XS
LoVo NFvlSoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fz[GlEPTB;NEiuNVAxOiEQvF2= NIrLVGhUSU6JRWK=
NCI-H510A M{n0cGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYrUOopWUUN3ME20PE4yQDdzIN88US=> NI[wPIpUSU6JRWK=
EW-11 NHji[mhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7oW|JKSzVyPUS4MlI{PDhizszN NGPxelBUSU6JRWK=
HCC2998 M3joUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIO1dXJKSzVyPUS4MlYzOzZizszN NVrlcJlWW0GQR1XS
J82 NEHtcpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXwTlNrUUN3ME20PE44OjR{IN88US=> MUjTRW5ITVJ?
ML-2 NW\iOmxYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2L6e2lEPTB;NEmuOFYxPSEQvF2= MYXTRW5ITVJ?
NCI-H2030 NU\sdZI6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLHbIpKSzVyPUS5MlcyOTdizszN NVLwWmFnW0GQR1XS
NCI-H1792 MoXsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTObW5KSzVyPUS5Mlg2OThizszN MWHTRW5ITVJ?

... 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
In vivo Nilotinib reduces collagen deposition and α-SMA expression in CCl4 and BDL-induced fibrosis. Nilotinib could induce HSC undergoing apoptosis, which is correlated with downregulation of bcl-2. [2] Nilotinib attenuates the extent of lung injury and fibrosis. Nilotinib therapy significantly reduces the levels of hydroxyproline on days 14 and 21, which is accompanied by decreased expression levels of transforming growth factor (TGF)-β1 and PDGFRβ. [5] AMN107 prolongs survival of mice injected with Bcr-Abl-transformed hematopoietic cell lines or primary marrow cells, and prolongs survival in imatinib-resistant CML mouse models. [6]

Protocol

Cell Research:[4]
- Collapse
  • Cell lines: Human primary Schwann and schwannoma cells
  • Concentrations: 1-10 μM
  • Incubation Time: 72 hours
  • Method: Human primary Schwann and schwannoma cells are seeded on precoated 96-well plates. Nilotinib is added 40 minutes before stimulation with 100 ng/mL PDGF-DD, and cells are cultured for 72 hours (3 days). Because the half-life of Nilotinib is 18 hours, one-half of the originally added concentrations are added freshly every day. In addition to DAPI staining and determination of the total cell number, the more sensitive and accurate BrdU incorporation method is used to detect proliferating cells. Total cell amount (DAPI) and number of dividing cells (BrdU-positive) are blindly counted using an inverted fluorescent microscope and 200 × magnification. All cells in every well are counted. The total cell number per well differed between various cell batches and is 100–300 cells/well.
    (Only for Reference)
Animal Research:[6]
- Collapse
  • Animal Models: Systemic 32D Bcr-Abl leukemia model in Female BALB/c mice, Bioluminescent Bcr-Abl model of CML in Female NOD-SCID mice and Bone marrow transplant Bcr-Abl model of CML in syngeneic Balb/c recipient mice
  • Formulation: 10% NMP-90% PEG300, PEG300
  • Dosages: 75 mg/kg, 100 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 27 mg/mL (50.98 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
3mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 529.52
Formula

C28H22F3N7O

CAS No. 641571-10-0
Storage powder
in solvent
Synonyms N/A
Smiles CC1=C[N](C=N1)C2=CC(=CC(=C2)C(F)(F)F)NC(=O)C3=CC=C(C)C(=C3)NC4=NC=CC(=N4)C5=CN=CC=C5

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
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    Volume
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
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    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

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) November 2019 Phase 2
NCT03942094 Not yet recruiting Drug: Nilotinib Chronic Myeloid Leukemia Chronic Phase|Nilotinib Shenzhen Second People''s Hospital June 1 2019 Phase 3
NCT03874858 Recruiting Drug: Nilotinib Chronic Myeloid Leukemia Novartis Pharmaceuticals|Novartis March 22 2019 Phase 2
NCT02973711 Suspended Drug: Nilotinib|Drug: Ruxolitinib Leukemia Chronic Myeloid University of Michigan Rogel Cancer Center January 18 2018 Phase 1|Phase 2
NCT03228303 Not yet recruiting Drug: Nilotinib 150 MG [Tasigna]|Drug: Imatinib 400mg Chronic Myeloid Leukemia Assiut University December 1 2017 Early Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Frequently Asked Questions

  • Question 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?

  • Answer:

    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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID