Nilotinib (AMN-107)

Catalog No.S1033

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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  • Ba/F3-p210T315I cells were treated with indicated concentrations of nilotinib with or without PDMP for 24 h. Apoptosis was determined as in A. Data are shown as percentage of sub-G1 for apoptosis in triplicate cultures. *P<0.05.

    FASEB J 2011 25, 3661-3673. Nilotinib (AMN-107) purchased from Selleck.

    Effect of nilotinib on Bcr-Abl kinase activity in ABCB1- and ABCG2- overexpressing CD34+CD38- cells. K562 parental cells and CD34+CD38- subpopulation isolated from K562 cells were treated with nilotinib at 0.01, 0.1 and 1.0 umol/L for 12 h. Equal amount of protein was loaded for western blot analysis as described in the Experimental section. The experiments were repeated at least three times independently, and a representative experiment is shown.

    Molecules 2014 19, 3356-75. Nilotinib (AMN-107) purchased from Selleck.

  •  

    Inhibition of thymidine (a and b) and cytarabine (c and d) uptake with nilotinib. The legend is similar to Fig. 1, except that imatinib was replaced by nilotinib.

    Leukemia Res 2012 36, 1311-1314. Nilotinib (AMN-107) purchased from Selleck.

    Nilotinib up-regulates the ERK survival signal in prostate cancer cells. (B and C) Immunoblot analyses of DU-145 cells (B) or DU-145 cells in comparison with LNCaP and PC-3 cells (C) treated with nilotinib for the expression of phospho-ERK1/2 T202/Y204 and total ERK. Immunoblot for GAPDH is shown as a loading control.

    Urol Oncol 2014 0.1016/j.urolonc.2014.06.001. Nilotinib (AMN-107) purchased from Selleck.

  • Immunohistochemical staining of xenografted DU-145 cells after 21 days of treatment with 75 mg/kg/d of nilotinib for phospho-ERK1/2 T202/Y204 expression. It can be noted that tumors explanted from vehicle-treated mice showed mostly positivity at the tumor periphery, whereas tumors explanted from nilotinib-treated mice showed a more evenly distributed phospho-ERK immunostaining (left panels). Quantification of phospho-ERK-positive DU-145 xenografts explanted after 21 days of treatment. Mean and standard errors of positive cells per high-power field (HPF; x40) from at least 3 tumors are given (right panel).

    Urol Oncol 2014 0.1016/j.urolonc.2014.06.001. Nilotinib (AMN-107) purchased from Selleck.

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 M1jnO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3LCXmlEPTB;MD6wNFAyPDRizszN M{nKSnNCVkeHUh?=
KU812 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTBwMECyOFgh|ryP NIq2enJUSU6JRWK=
EM-2 MknOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTBwMEC0NUDPxE1? NGrofXhUSU6JRWK=
LAMA-84 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLLTWM2OD1yLkCwOFkh|ryP MXLTRW5ITVJ?
MEG-01 NXzn[G5wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vxUGlEPTB;MD6wNFgzQCEQvF2= M{Hxe3NCVkeHUh?=
BV-173 MnzFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2ThXmlEPTB;MD6wNVA5QSEQvF2= MknFV2FPT0WU
KASUMI-1 NXT5dIxLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHW0b4RKSzVyPUCuNFI1OTNizszN NIq2SXJUSU6JRWK=
NB7 MoLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXoTWM2OD1yLkGzOFM6KM7:TR?= MUDTRW5ITVJ?
BHT-101 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Moe3TWM2OD1yLk[0NlY{KM7:TR?= NWDBOppKW0GQR1XS
CGTH-W-1 M4PSWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjUc45KSzVyPUCuOlQ5PyEQvF2= NVHqVZlyW0GQR1XS
HMV-II MlzKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTBwN{S4O|Qh|ryP NFfve|RUSU6JRWK=
NKM-1 NHPuWY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml25TWM2OD1yLkmwNVUh|ryP NY\QfHRXW0GQR1XS
LB2241-RCC M2XPOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPHcIZSUUN3ME2xMlAzOjJ6IN88US=> M13HeHNCVkeHUh?=
NCI-H1703 NUL2WIx6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTFwMUi4O{DPxE1? MmHLV2FPT0WU
BE-13 NVL4e5pbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2q3OGlEPTB;MT6yO|QyPiEQvF2= NVO0OnNQW0GQR1XS
ACN M1\S[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTFwNUWwO|ch|ryP NWTo[m5RW0GQR1XS
A204 NVXmTYZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIG1[3FKSzVyPUGuOVczODVizszN M2\SVHNCVkeHUh?=
HOP-62 Mo\NS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTFwOEKwO|ch|ryP MYjTRW5ITVJ?
H9 NELjW5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHXTWM2OD1{LkezO|k{KM7:TR?= M2L6RnNCVkeHUh?=
HCC1806 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mmf0TWM2OD1{Lke0N|I4KM7:TR?= NF35W|FUSU6JRWK=
NOS-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrB[3hGUUN3ME2yMlg4OTB{IN88US=> Mn2wV2FPT0WU
RS4-11 MoGzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTJwOUC2NlMh|ryP NEPmcYdUSU6JRWK=
JAR NX3WenhFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHMW5hKSzVyPUKuPVIxQDRizszN M{PiO3NCVkeHUh?=
T98G MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnnTWM2OD1|LkCxN|E{KM7:TR?= NHXaeWhUSU6JRWK=
NCI-SNU-1 NULEPId3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfJfYpxUUN3ME2zMlQxODl{IN88US=> NH;USJJUSU6JRWK=
SK-MEL-1 NXj3[HNUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFyz[HZKSzVyPUOuOFMxOjlizszN NFm5fGhUSU6JRWK=
L-363 NXHZ[o01T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTNwNkGxNFch|ryP MXXTRW5ITVJ?
SW982 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{PtS2lEPTB;Mz62OFE3QSEQvF2= Mn7pV2FPT0WU
HT-1080 MmPQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHvUFRHUUN3ME2zMlkyPzd3IN88US=> MYDTRW5ITVJ?
G-402 MnzJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXDTWM2OD12LkOxNlA{KM7:TR?= MULTRW5ITVJ?
HOS MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfCbXhKSzVyPUSuPFAzQDJizszN NXzLcoNOW0GQR1XS
SK-NEP-1 MlS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDPZ3VGUUN3ME20Mlg{OTlzIN88US=> MnXqV2FPT0WU
HAL-01 Ml3OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEn1RmtKSzVyPUSuPFgzPDJizszN NWfCW5ZCW0GQR1XS
SBC-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFv3dmlKSzVyPUSuPVA6ODdizszN MkfFV2FPT0WU
CTV-1 NFTzd4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEe5UFVKSzVyPUWuOFg6OzhizszN MX3TRW5ITVJ?
LCLC-103H M4\QO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{PKNWlEPTB;NT63O|Q4OSEQvF2= MUnTRW5ITVJ?
RVH-421 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWfJR|UxRTVwN{e1N|Yh|ryP MWjTRW5ITVJ?
K-562 MlX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\u[FhZUUN3ME21MlkxOzZizszN NWmxcpBFW0GQR1XS
CAL-33 NYrv[3ZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NET1OZhKSzVyPU[uN|E{PTlizszN NEfxTpBUSU6JRWK=
MDA-MB-361 NXvVXplDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3PKTmlEPTB;Nj6zN|Y6QSEQvF2= NFq3OWNUSU6JRWK=
IGROV-1 M2XYXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTtTWM2OD14LkS3NVkyKM7:TR?= M{LUXHNCVkeHUh?=
NY NEnybWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TtXWlEPTB;Nj61N|U6QSEQvF2= NWLzWFVUW0GQR1XS
Ramos-2G6-4C10 NXrZe|VqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF62[o1KSzVyPU[uOlY6OzFizszN NWG0eYhYW0GQR1XS
HuO9 NYfGSndxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnLGTWM2OD14LkezPVY1KM7:TR?= MUHTRW5ITVJ?
MS-1 NVjmOHNZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfnZ5lKSzVyPUeuNVE6PTNizszN MUTTRW5ITVJ?
RPMI-8226 M2Tacmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTdwMkiyPFch|ryP MmL1V2FPT0WU
HDLM-2 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWK0PHNGUUN3ME23MlQxOTR7IN88US=> M2LYbnNCVkeHUh?=
D-566MG NX\oWYxrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXJWYF3UUN3ME23MlQ4OTV3IN88US=> MXTTRW5ITVJ?
SK-MEL-24 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3nIfWlEPTB;Nz62N|M6OiEQvF2= M1zDc3NCVkeHUh?=
COLO-679 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTiXWFKSzVyPUeuPVg3PzFizszN NHfUcHhUSU6JRWK=
EW-13 NVPYS2tFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PP[2lEPTB;OD6zNlA2PCEQvF2= NImycodUSU6JRWK=
A388 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFL0SnRKSzVyPUiuN|g1QDFizszN MYDTRW5ITVJ?
UM-UC-3 NUixfHRrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NISyVlRKSzVyPUiuOFM6PTZizszN M1Hw[nNCVkeHUh?=
NUGC-3 Mo[3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLUUGlmUUN3ME24MlU{PTh{IN88US=> MmnDV2FPT0WU
COLO-668 NYLTS2FtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{P0cWlEPTB;OD61PVQ6OSEQvF2= MoDrV2FPT0WU
MOLT-4 M1X3SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYqwdml4UUN3ME24MlYzOzV|IN88US=> MUPTRW5ITVJ?
D-423MG NWjrdnJVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXHIOGF1UUN3ME24Mlg{PzV4IN88US=> M4\PeXNCVkeHUh?=
CTB-1 NF60WVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrwU2NKSzVyPUiuPFcyOjhizszN MkXLV2FPT0WU
BCPAP MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTlwMEK1OlIh|ryP NWXNWGdvW0GQR1XS
GCT NEjUdYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo\lTWM2OD17LkC5PFMyKM7:TR?= NHfDfFFUSU6JRWK=
ACHN NEjUPY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjyUXNKSzVyPUmuNlM3OzJizszN NHnsTZZUSU6JRWK=
KYSE-520 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml74TWM2OD17LkOzOFgzKM7:TR?= NIO4VlRUSU6JRWK=
LB771-HNC MkHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULqXpplUUN3ME25Mlc3PDl5IN88US=> MnTxV2FPT0WU
MLMA NG\LcG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33FZmlEPTB;MUCuNFE{OiEQvF2= NWLLR3VrW0GQR1XS
HEC-1 NInNZ4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEWzXZhKSzVyPUGwMlI5ODRizszN NXfqRox[W0GQR1XS
HL-60 NWXENmhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3yxdWlEPTB;MUCuOlg2OyEQvF2= NILncXJUSU6JRWK=
A101D NEnNR3FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4Dh[2lEPTB;MUCuPFkzOyEQvF2= NWTvRVU3W0GQR1XS
A2058 M1j3Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTFyLkmyOFUh|ryP MnPNV2FPT0WU
KARPAS-45 M3yzXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX3JR|UxRTFzLkC2N|Uh|ryP NFfyTmxUSU6JRWK=
697 NHLF[IxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHTTWM2OD1zMT6yNVAyKM7:TR?= Mk\wV2FPT0WU
NCI-N87 MmXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3sTWM2OD1zMT63O|MyKM7:TR?= MXzTRW5ITVJ?
DSH1 NVvN[Jc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PjWmlEPTB;MUGuO|k2OyEQvF2= NYfU[XNNW0GQR1XS
HLE M1L1dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTFzLki4N|kh|ryP MkDnV2FPT0WU
NCI-H720 NYDpfm1iT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFT1N4pKSzVyPUGyMlY5ODFizszN MlfCV2FPT0WU
EW-3 MlXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4Lzc2lEPTB;MUKuPVMxPyEQvF2= MVvTRW5ITVJ?
AGS MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV;jNpJyUUN3ME2xN{4xOzVzIN88US=> MWXTRW5ITVJ?
ES5 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3oXHpiUUN3ME2xN{4xPTF{IN88US=> NHuzUIpUSU6JRWK=
DB M4nIRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELFe3lKSzVyPUGzMlMzPTZizszN MX\TRW5ITVJ?
A4-Fuk MmTxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIrscXRKSzVyPUGzMlQyODJizszN MYnTRW5ITVJ?
A427 M3jPfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX7McJhzUUN3ME2xN{41QTd{IN88US=> NF;uS2dUSU6JRWK=
MN-60 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTF|LkW4OFMh|ryP NELFOJZUSU6JRWK=
HCC2218 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTF|LkW4OVYh|ryP MkT0V2FPT0WU
MV-4-11 NH;pOohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVr0blVVUUN3ME2xN{45OTN5IN88US=> MYTTRW5ITVJ?
GI-1 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4S1NmlEPTB;MUSuNVE5PCEQvF2= M2HCS3NCVkeHUh?=
JVM-3 NUPFWI5VT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37NOWlEPTB;MUSuNlY2PiEQvF2= MXLTRW5ITVJ?
NCI-H2029 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LKPWlEPTB;MUSuNlczPyEQvF2= NUGzZZVzW0GQR1XS
TE-12 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTF2Lk[wOFYh|ryP MYXTRW5ITVJ?
WM-115 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUfhWGlSUUN3ME2xOU42Pjh|IN88US=> NH\jRnRUSU6JRWK=
BB65-RCC Mo\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTF4LkCyOFEh|ryP MUXTRW5ITVJ?
NCI-H1693 MnnqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HvfGlEPTB;MU[uN|gxOiEQvF2= MYXTRW5ITVJ?
KARPAS-299 NUXoW5hiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPPSo5WUUN3ME2xOk43OjB|IN88US=> NILVSlBUSU6JRWK=
UACC-257 M1XuVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;iTWM2OD1zNz6wOVgzKM7:TR?= MVPTRW5ITVJ?
RKO M1HsRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfiRZlKSzVyPUG3MlY1OzNizszN NFqxTIpUSU6JRWK=
HT-29 M3m1W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlfvTWM2OD1zNz63PFg6KM7:TR?= NXuyVoE5W0GQR1XS
ES7 Mn[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGi1cW5KSzVyPUG4MlEyOjJizszN NWOxfIlFW0GQR1XS
DEL NITBc|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF76[XFKSzVyPUG4MlMyPzJizszN MY\TRW5ITVJ?
BT-549 NWLKdHlpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHTPUlVKSzVyPUG4MlQxQTJizszN Mlm5V2FPT0WU
NCI-H1755 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTF6LkW3NlMh|ryP M4T3NnNCVkeHUh?=
HCE-T M130WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjXeXlKSzVyPUG4Mlg{PDFizszN MU\TRW5ITVJ?
LU-139 NFXQTZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjGPYRHUUN3ME2xPU4xPDV6IN88US=> M1vie3NCVkeHUh?=
ECC10 NIr4OIdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYLiNphbUUN3ME2xPU4zPDd3IN88US=> MnvBV2FPT0WU
769-P MknOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1X6V2lEPTB;MUmuOlM{PSEQvF2= NXH0Wo1qW0GQR1XS
BALL-1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHifXpKSzVyPUG5MlY4PzVizszN NHTtOWFUSU6JRWK=
LXF-289 M1i0XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXCNpNKSzVyPUG5Mlg6PzlizszN MUPTRW5ITVJ?
TYK-nu NVLUWZNyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknPTWM2OD1zOT65N|E2KM7:TR?= MXvTRW5ITVJ?
NCI-H630 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYj5Z2JmUUN3ME2xPU46Ozd6IN88US=> NF;oTXRUSU6JRWK=
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... Click to View More Cell Line Experimental Data

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]
+ Expand
  • 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]
+ Expand
  • 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 individually and in order:
4% DMSO+30% PEG 300+5% Tween 80+ddH2O
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
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02973711 Not yet recruiting Leukemia, Chronic Myeloid University of Michigan Cancer Center February 2017 Phase 1|Phase 2
NCT02954978 Recruiting Parkinson Disease|Parkinsons Disease With Dementia Georgetown University January 2017 Phase 2
NCT02947893 Recruiting Alzheimers Disease Georgetown University January 2017 Phase 2
NCT02602314 Not yet recruiting Chronyc Myeloid Leukemia Gruppo Italiano Malattie EMatologiche dellAdulto December 2016 Phase 4
NCT02709083 Recruiting Chronic Myelogenous Leukemia|Chronic Myeloid Leukemia|Leukemia Emory University October 2016 Phase 2
NCT02917720 Not yet recruiting Chronic Myeloid Leukemia European LeukemiaNet|Heidelberg University|Ludwig-Maximilians - University of Munich October 2016 Phase 2

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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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID