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 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWjJR|UxRTBwMECwNVQ1KM7:TR?= M13ZbHNCVkeHUh?=
KU812 NH7xU3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLmToJKSzVyPUCuNFAzPDhizszN Mn\3V2FPT0WU
EM-2 M2XDbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFH1UZZKSzVyPUCuNFA1OSEQvF2= NUPBbnhNW0GQR1XS
LAMA-84 MknjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmC4TWM2OD1yLkCwOFkh|ryP M1izfXNCVkeHUh?=
MEG-01 MojSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlT5TWM2OD1yLkCwPFI5KM7:TR?= NFzFfItUSU6JRWK=
BV-173 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjQR3ZKSzVyPUCuNFExQDlizszN MV\TRW5ITVJ?
KASUMI-1 NHj4bopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGX4NItKSzVyPUCuNFI1OTNizszN MWLTRW5ITVJ?
NB7 M{f0fWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MY\JR|UxRTBwMUO0N|kh|ryP MoPGV2FPT0WU
BHT-101 NUX4Vlg6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nXPWlEPTB;MD62OFI3OyEQvF2= NXr2dVlyW0GQR1XS
CGTH-W-1 NYLMSXU6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHne41KSzVyPUCuOlQ5PyEQvF2= MXrTRW5ITVJ?
HMV-II NWjIVohyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPwTWM2OD1yLke0PFc1KM7:TR?= NI\CNmlUSU6JRWK=
NKM-1 NIjYe5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFe2N3JKSzVyPUCuPVAyPSEQvF2= Mkn0V2FPT0WU
LB2241-RCC M4nrXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPXTWM2OD1zLkCyNlI5KM7:TR?= M{fZN3NCVkeHUh?=
NCI-H1703 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{K1bGlEPTB;MT6xPFg4KM7:TR?= NWXTUXhIW0GQR1XS
BE-13 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTFwMke0NVYh|ryP NXjLUpNkW0GQR1XS
ACN NYS0[3RoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mlz6TWM2OD1zLkW1NFc4KM7:TR?= M1\pRnNCVkeHUh?=
A204 NIP6c4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXXJR|UxRTFwNUeyNFUh|ryP MX7TRW5ITVJ?
HOP-62 Ml\DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoW1TWM2OD1zLkiyNFc4KM7:TR?= MXXTRW5ITVJ?
H9 M{jPR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTJwN{O3PVMh|ryP NF;NUHFUSU6JRWK=
HCC1806 NGnHb5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHyzfHlKSzVyPUKuO|Q{OjdizszN NXThTVRMW0GQR1XS
NOS-1 NGfSdW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7PTWM2OD1{Lki3NVAzKM7:TR?= NUjsVVZpW0GQR1XS
RS4-11 NFLmUlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDifopKSzVyPUKuPVA3OjNizszN MoWzV2FPT0WU
JAR MoD2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnSSmZKSzVyPUKuPVIxQDRizszN NEDORmNUSU6JRWK=
T98G M1Xae2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn64TWM2OD1|LkCxN|E{KM7:TR?= MnG1V2FPT0WU
NCI-SNU-1 M{\NSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLyTWM2OD1|LkSwNFkzKM7:TR?= Mn3PV2FPT0WU
SK-MEL-1 NUKxSlNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGTkO3FKSzVyPUOuOFMxOjlizszN MU\TRW5ITVJ?
L-363 NVPUeYVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPCb2ZLUUN3ME2zMlYyOTB5IN88US=> MkmzV2FPT0WU
SW982 MoDhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYPJR|UxRTNwNkSxOlkh|ryP M{DHcHNCVkeHUh?=
HT-1080 MlPJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mni0TWM2OD1|LkmxO|c2KM7:TR?= NXm5V|NwW0GQR1XS
G-402 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzCboZSUUN3ME20MlMyOjB|IN88US=> NVHWZpk1W0GQR1XS
HOS MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjrTWM2OD12LkiwNlgzKM7:TR?= NX3ORWxQW0GQR1XS
SK-NEP-1 M{HWbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1:zcmlEPTB;ND64N|E6OSEQvF2= M3PKU3NCVkeHUh?=
HAL-01 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3PTWM2OD12Lki4NlQzKM7:TR?= MV3TRW5ITVJ?
SBC-1 M3PQWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIi5cGtKSzVyPUSuPVA6ODdizszN Ml64V2FPT0WU
CTV-1 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVfJR|UxRTVwNEi5N|gh|ryP NHvPdWtUSU6JRWK=
LCLC-103H MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXS2NFhXUUN3ME21Mlc4PDdzIN88US=> M1[1fHNCVkeHUh?=
RVH-421 NI\LRlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\KTWM2OD13Lke3OVM3KM7:TR?= MYnTRW5ITVJ?
K-562 MnnHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\kTohDUUN3ME21MlkxOzZizszN NXHhRYRuW0GQR1XS
CAL-33 M3O0ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTZwM{GzOVkh|ryP Mn\4V2FPT0WU
MDA-MB-361 M4XnVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTZwM{O2PVkh|ryP NYm4U5hMW0GQR1XS
IGROV-1 M3j0UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{O5d2lEPTB;Nj60O|E6OSEQvF2= NWHseplFW0GQR1XS
NY M13pZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEj1dWRKSzVyPU[uOVM2QTlizszN NVyxfpZiW0GQR1XS
Ramos-2G6-4C10 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3lcoZFUUN3ME22MlY3QTNzIN88US=> MoDSV2FPT0WU
HuO9 NFHye|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITLNolKSzVyPU[uO|M6PjRizszN MXrTRW5ITVJ?
MS-1 NUTZephlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTdwMUG5OVMh|ryP NUOycWlpW0GQR1XS
RPMI-8226 NWHUUFRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHH0TXFKSzVyPUeuNlgzQDdizszN M{jxUnNCVkeHUh?=
HDLM-2 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTwPIRRUUN3ME23MlQxOTR7IN88US=> MXrTRW5ITVJ?
D-566MG MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnv6TWM2OD15LkS3NVU2KM7:TR?= NH\pWGFUSU6JRWK=
SK-MEL-24 NEey[VZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFPCW4xKSzVyPUeuOlM{QTJizszN MoXyV2FPT0WU
COLO-679 M2fJemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLTTWM2OD15Lkm4OlcyKM7:TR?= NVz6dldDW0GQR1XS
EW-13 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRThwM{KwOVQh|ryP MWnTRW5ITVJ?
A388 MoC0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWj1epFuUUN3ME24MlM5PDhzIN88US=> NES0PY5USU6JRWK=
UM-UC-3 M{Pnc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHL1PGVKSzVyPUiuOFM6PTZizszN MnfYV2FPT0WU
NUGC-3 MoDpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fQZmlEPTB;OD61N|U5OiEQvF2= NUjlWIRZW0GQR1XS
COLO-668 NVLkVnRnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Tyc2lEPTB;OD61PVQ6OSEQvF2= M1m1VHNCVkeHUh?=
MOLT-4 MlXzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlP1TWM2OD16Lk[yN|U{KM7:TR?= MX\TRW5ITVJ?
D-423MG MmHES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nYXGlEPTB;OD64N|c2PiEQvF2= MoO0V2FPT0WU
CTB-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlX2TWM2OD16Lki3NVI5KM7:TR?= NFfB[GhUSU6JRWK=
BCPAP NGHmOYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTlwMEK1OlIh|ryP NFj6V|VUSU6JRWK=
GCT MnnES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX\JR|UxRTlwMEm4N|Eh|ryP NITOOZBUSU6JRWK=
ACHN MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTlwMkO2N|Ih|ryP NF;0PIhUSU6JRWK=
KYSE-520 NVnQeXVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnizTWM2OD17LkOzOFgzKM7:TR?= MXnTRW5ITVJ?
LB771-HNC Mm[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1j1SGlEPTB;OT63OlQ6PyEQvF2= MnHLV2FPT0WU
MLMA NH\qbVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjHS2JEUUN3ME2xNE4xOTN{IN88US=> MX;TRW5ITVJ?
HEC-1 NILMdHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nacGlEPTB;MUCuNlgxPCEQvF2= NES0VXpUSU6JRWK=
HL-60 M{fuRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\hVGlEPTB;MUCuOlg2OyEQvF2= NF;Y[5hUSU6JRWK=
A101D NGXBXVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTFyLki5NlMh|ryP MVvTRW5ITVJ?
A2058 M2DuXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rt[2lEPTB;MUCuPVI1PSEQvF2= Mlj3V2FPT0WU
KARPAS-45 M1q5Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fne2lEPTB;MUGuNFY{PSEQvF2= NFq2fpRUSU6JRWK=
697 MoTIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXPJR|UxRTFzLkKxNFEh|ryP NFz0UZpUSU6JRWK=
NCI-N87 NEDKUZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlPYTWM2OD1zMT63O|MyKM7:TR?= MXrTRW5ITVJ?
DSH1 MnTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MliwTWM2OD1zMT63PVU{KM7:TR?= NV7qSGpIW0GQR1XS
HLE MlPMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTFzLki4N|kh|ryP MYfTRW5ITVJ?
NCI-H720 MmnUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUm2clQ5UUN3ME2xNk43QDBzIN88US=> MVXTRW5ITVJ?
EW-3 M2fSc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nm[2lEPTB;MUKuPVMxPyEQvF2= NIjHeXFUSU6JRWK=
AGS NGfl[VZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17x[WlEPTB;MUOuNFM2OSEQvF2= M2TIbnNCVkeHUh?=
ES5 NHzFdG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXKN|FKSzVyPUGzMlA2OTJizszN NF;nOGFUSU6JRWK=
DB MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlP1TWM2OD1zMz6zNlU3KM7:TR?= NIHIR3dUSU6JRWK=
A4-Fuk NWHUUnk2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2TxRWlEPTB;MUOuOFExOiEQvF2= MWjTRW5ITVJ?
A427 MorVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;oOW4xUUN3ME2xN{41QTd{IN88US=> M1qwR3NCVkeHUh?=
MN-60 M2fodmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33memlEPTB;MUOuOVg1OyEQvF2= NWPzSXVGW0GQR1XS
HCC2218 MoLwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXu1SnVbUUN3ME2xN{42QDV4IN88US=> M2XtWnNCVkeHUh?=
MV-4-11 M2\SbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fnOGlEPTB;MUOuPFE{PyEQvF2= Mk\OV2FPT0WU
GI-1 M4jpZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTF2LkGxPFQh|ryP MlzxV2FPT0WU
JVM-3 Mn\SS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzEVXVKSzVyPUG0MlI3PTZizszN M17D[3NCVkeHUh?=
NCI-H2029 M{C3U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4rHe2lEPTB;MUSuNlczPyEQvF2= MYXTRW5ITVJ?
TE-12 NIrNXJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXRTWM2OD1zND62NFQ3KM7:TR?= MnfoV2FPT0WU
WM-115 MofwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3v[pF7UUN3ME2xOU42Pjh|IN88US=> MkTFV2FPT0WU
BB65-RCC NXXRWZBjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvIR5J2UUN3ME2xOk4xOjRzIN88US=> M3vNWnNCVkeHUh?=
NCI-H1693 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XnUmlEPTB;MU[uN|gxOiEQvF2= MU\TRW5ITVJ?
KARPAS-299 NXXKN5pWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTF4Lk[yNFMh|ryP Mn3VV2FPT0WU
UACC-257 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoXuTWM2OD1zNz6wOVgzKM7:TR?= M{nDb3NCVkeHUh?=
RKO NIXHN3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTF5Lk[0N|Mh|ryP NFvaWXRUSU6JRWK=
HT-29 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4T5[mlEPTB;MUeuO|g5QSEQvF2= Mm\5V2FPT0WU
ES7 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;XTWM2OD1zOD6xNVIzKM7:TR?= M1TjOHNCVkeHUh?=
DEL NX;T[IU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLkTWM2OD1zOD6zNVczKM7:TR?= MkmzV2FPT0WU
BT-549 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTDUnkyUUN3ME2xPE41ODl{IN88US=> M3q4Z3NCVkeHUh?=
NCI-H1755 M1Pmbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkW3TWM2OD1zOD61O|I{KM7:TR?= NUmzTFNJW0GQR1XS
HCE-T M1W2cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWLKdpV6UUN3ME2xPE45OzRzIN88US=> M2LtZnNCVkeHUh?=
LU-139 NF7Ue4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrGc|ZKSzVyPUG5MlA1PThizszN NHrSPXhUSU6JRWK=
ECC10 NFHuXHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPzTWM2OD1zOT6yOFc2KM7:TR?= MYLTRW5ITVJ?
769-P NHLMTY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETrXFZKSzVyPUG5MlY{OzVizszN MmrSV2FPT0WU
BALL-1 MmfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\4TWlEPTB;MUmuOlc4PSEQvF2= NGHVfFVUSU6JRWK=
LXF-289 NHrVZlNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDVU|VKSzVyPUG5Mlg6PzlizszN NWrzPJg1W0GQR1XS
TYK-nu NEX0WmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTOTWM2OD1zOT65N|E2KM7:TR?= MYHTRW5ITVJ?
NCI-H630 M{TJdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3flVWlEPTB;MUmuPVM4QCEQvF2= MmSyV2FPT0WU
EW-18 Ml[2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;jVWlEPTB;MkCuN|gxOiEQvF2= MWXTRW5ITVJ?
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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 to the product individually and in order:
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
Synonyms N/A

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:

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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).

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

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

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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

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID