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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In DMSO USD 91 In stock
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USD 210 In stock
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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 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NInQNohKSzVyPUCuNFAxOTR2IN88US=> MkHRV2FPT0WU
KU812 M3TxW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEPYUnRKSzVyPUCuNFAzPDhizszN MYDTRW5ITVJ?
EM-2 Mn75S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7MTWM2OD1yLkCwOFEh|ryP NGD5RXhUSU6JRWK=
LAMA-84 MlrqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPSOlBKSzVyPUCuNFA1QSEQvF2= M13mWnNCVkeHUh?=
MEG-01 Mn:0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\3cWlEPTB;MD6wNFgzQCEQvF2= MWHTRW5ITVJ?
BV-173 NX7BUYNXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DSXWlEPTB;MD6wNVA5QSEQvF2= NGS5[XRUSU6JRWK=
KASUMI-1 NVm5bIJMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXFTWM2OD1yLkCyOFE{KM7:TR?= NVLJcINiW0GQR1XS
NB7 NYrHZWQyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHGXHJWUUN3ME2wMlE{PDN7IN88US=> M4m5SHNCVkeHUh?=
BHT-101 MkS1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPvd|dKSzVyPUCuOlQzPjNizszN NHruTZhUSU6JRWK=
CGTH-W-1 NH3WUI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTiTWM2OD1yLk[0PFch|ryP NHXzZYdUSU6JRWK=
HMV-II NXj1[GQxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHDTWM2OD1yLke0PFc1KM7:TR?= MUnTRW5ITVJ?
NKM-1 M2K4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTBwOUCxOUDPxE1? NXThOGNoW0GQR1XS
LB2241-RCC MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPJR|UxRTFwMEKyNlgh|ryP MV3TRW5ITVJ?
NCI-H1703 M3LBRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmL5TWM2OD1zLkG4PFch|ryP NWDHXldDW0GQR1XS
BE-13 NX3TUoVjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGPINWNKSzVyPUGuNlc1OTZizszN MlW5V2FPT0WU
ACN NGXpXWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkLZTWM2OD1zLkW1NFc4KM7:TR?= MYHTRW5ITVJ?
A204 M4\ZWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XMfmlEPTB;MT61O|IxPSEQvF2= MmW5V2FPT0WU
HOP-62 NXXNbldOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHMWo5KSzVyPUGuPFIxPzdizszN MniwV2FPT0WU
H9 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFn1O45KSzVyPUKuO|M4QTNizszN NUfNcW1pW0GQR1XS
HCC1806 Ml7OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTJwN{SzNlch|ryP NHPZRmtUSU6JRWK=
NOS-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXBc|FXUUN3ME2yMlg4OTB{IN88US=> MlS5V2FPT0WU
RS4-11 Mo\wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DXcWlEPTB;Mj65NFYzOyEQvF2= MUjTRW5ITVJ?
JAR NXG3cI94T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTJwOUKwPFQh|ryP M33jfHNCVkeHUh?=
T98G MonFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTNwMEGzNVMh|ryP MorJV2FPT0WU
NCI-SNU-1 NXfpRpM3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzaTWM2OD1|LkSwNFkzKM7:TR?= M4W5S3NCVkeHUh?=
SK-MEL-1 NX\zbHdST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTNwNEOwNlkh|ryP NV[1SJpPW0GQR1XS
L-363 MlHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYSwd4JiUUN3ME2zMlYyOTB5IN88US=> M3nVVnNCVkeHUh?=
SW982 NV;kOWpET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\GR2lEPTB;Mz62OFE3QSEQvF2= MXLTRW5ITVJ?
HT-1080 MkXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LMPGlEPTB;Mz65NVc4PSEQvF2= NVXKe2loW0GQR1XS
G-402 NEXGXY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn2xTWM2OD12LkOxNlA{KM7:TR?= NHewfpVUSU6JRWK=
HOS NWqzclVHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDkV3ZKSzVyPUSuPFAzQDJizszN MU\TRW5ITVJ?
SK-NEP-1 NFTYTpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTRwOEOxPVEh|ryP M37ZXXNCVkeHUh?=
HAL-01 NUX1VmpjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEnXVm1KSzVyPUSuPFgzPDJizszN M4fuOHNCVkeHUh?=
SBC-1 M4jxTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\WTWM2OD12LkmwPVA4KM7:TR?= MkLiV2FPT0WU
CTV-1 M{jBVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\RTWM2OD13LkS4PVM5KM7:TR?= M1vue3NCVkeHUh?=
LCLC-103H M{KzRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\hTWM2OD13Lke3OFcyKM7:TR?= NHfaVWlUSU6JRWK=
RVH-421 NHzMdJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7yTWM2OD13Lke3OVM3KM7:TR?= NF\BeHVUSU6JRWK=
K-562 Mk\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LDdWlEPTB;NT65NFM3KM7:TR?= M4GwOHNCVkeHUh?=
CAL-33 Mlm4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTlTWM2OD14LkOxN|U6KM7:TR?= MoixV2FPT0WU
MDA-MB-361 MlnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PpU2lEPTB;Nj6zN|Y6QSEQvF2= MYrTRW5ITVJ?
IGROV-1 M1P5N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULlU4NJUUN3ME22MlQ4OTlzIN88US=> MofMV2FPT0WU
NY Mlu4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVnUXJczUUN3ME22MlU{PTl7IN88US=> MnTzV2FPT0WU
Ramos-2G6-4C10 Mn7rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlW3TWM2OD14Lk[2PVMyKM7:TR?= MWDTRW5ITVJ?
HuO9 M1L1UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HGUWlEPTB;Nj63N|k3PCEQvF2= NUPxbXRMW0GQR1XS
MS-1 M3zSOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;I[2lEPTB;Nz6xNVk2OyEQvF2= NWXSbFM6W0GQR1XS
RPMI-8226 MnT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3\2b2lEPTB;Nz6yPFI5PyEQvF2= MnW1V2FPT0WU
HDLM-2 M{fz[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2K3emlEPTB;Nz60NFE1QSEQvF2= MkLxV2FPT0WU
D-566MG NH7IbY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXlZ2dwUUN3ME23MlQ4OTV3IN88US=> MnvIV2FPT0WU
SK-MEL-24 NGr5R25Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTdwNkOzPVIh|ryP MoLyV2FPT0WU
COLO-679 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTdwOUi2O|Eh|ryP NGS3dWpUSU6JRWK=
EW-13 M{jjVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXyW|l2UUN3ME24MlMzODV2IN88US=> M4f5cnNCVkeHUh?=
A388 M3GzVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRThwM{i0PFEh|ryP MofaV2FPT0WU
UM-UC-3 NYG3[JhsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnGyTWM2OD16LkSzPVU3KM7:TR?= M3j3eXNCVkeHUh?=
NUGC-3 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml;qTWM2OD16LkWzOVgzKM7:TR?= MYfTRW5ITVJ?
COLO-668 Mn[5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGf5TWFKSzVyPUiuOVk1QTFizszN MVjTRW5ITVJ?
MOLT-4 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3TpfmlEPTB;OD62NlM2OyEQvF2= NHr0PJBUSU6JRWK=
D-423MG NWnnZ4pmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVn1e|RvUUN3ME24Mlg{PzV4IN88US=> MlvsV2FPT0WU
CTB-1 NInXcm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknTTWM2OD16Lki3NVI5KM7:TR?= MYPTRW5ITVJ?
BCPAP MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkT5TWM2OD17LkCyOVYzKM7:TR?= NIe5cnNUSU6JRWK=
GCT NYn3WY15T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlK4TWM2OD17LkC5PFMyKM7:TR?= MYXTRW5ITVJ?
ACHN NF2ycpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDGTWM2OD17LkKzOlMzKM7:TR?= NHPWV2ZUSU6JRWK=
KYSE-520 MnHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXLJR|UxRTlwM{O0PFIh|ryP M{Phe3NCVkeHUh?=
LB771-HNC MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEi2dIlKSzVyPUmuO|Y1QTdizszN Mlm5V2FPT0WU
MLMA MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4fFemlEPTB;MUCuNFE{OiEQvF2= MkDRV2FPT0WU
HEC-1 NIDaXJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfhT|hKSzVyPUGwMlI5ODRizszN M1rRfXNCVkeHUh?=
HL-60 M4ja[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mmi3TWM2OD1zMD62PFU{KM7:TR?= MXrTRW5ITVJ?
A101D MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFflWG9KSzVyPUGwMlg6OjNizszN MYrTRW5ITVJ?
A2058 MlHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjrTWM2OD1zMD65NlQ2KM7:TR?= NFnPelNUSU6JRWK=
KARPAS-45 MoX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7h[mFnUUN3ME2xNU4xPjN3IN88US=> MlnmV2FPT0WU
697 M4m1dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1yyRmlEPTB;MUGuNlExOSEQvF2= NVj6cIFTW0GQR1XS
NCI-N87 Mn7ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfzWW1KSzVyPUGxMlc4OzFizszN MYjTRW5ITVJ?
DSH1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlK2TWM2OD1zMT63PVU{KM7:TR?= M2XkNnNCVkeHUh?=
HLE NUnZUZlkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofkTWM2OD1zMT64PFM6KM7:TR?= MkSwV2FPT0WU
NCI-H720 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTF{Lk[4NFEh|ryP NW\O[oFjW0GQR1XS
EW-3 M1zrXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3XwbmlEPTB;MUKuPVMxPyEQvF2= NXLaNGtXW0GQR1XS
AGS Mk\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTF|LkCzOVEh|ryP MoXhV2FPT0WU
ES5 NVvWNphPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTF|LkC1NVIh|ryP M1vzcHNCVkeHUh?=
DB Mn35S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XjZWlEPTB;MUOuN|I2PiEQvF2= NGi5SW9USU6JRWK=
A4-Fuk NULrN|R3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\6fY5WUUN3ME2xN{41OTB{IN88US=> NGTSXmpUSU6JRWK=
A427 NUjicpZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHsdmtKSzVyPUGzMlQ6PzJizszN NI\JfIVUSU6JRWK=
MN-60 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDsb5N3UUN3ME2xN{42QDR|IN88US=> MXzTRW5ITVJ?
HCC2218 M2K1WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LYU2lEPTB;MUOuOVg2PiEQvF2= MVfTRW5ITVJ?
MV-4-11 MkjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTF|LkixN|ch|ryP NGWx[Y1USU6JRWK=
GI-1 MmTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\5TWM2OD1zND6xNVg1KM7:TR?= MXXTRW5ITVJ?
JVM-3 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUi4T2ROUUN3ME2xOE4zPjV4IN88US=> NFP5TGZUSU6JRWK=
NCI-H2029 NF7NcZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDsXpp{UUN3ME2xOE4zPzJ5IN88US=> MXfTRW5ITVJ?
TE-12 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnpOVRKSzVyPUG0MlYxPDZizszN MVLTRW5ITVJ?
WM-115 NIPzNVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml:4TWM2OD1zNT61Olg{KM7:TR?= M{HPbnNCVkeHUh?=
BB65-RCC MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUH0bm5lUUN3ME2xOk4xOjRzIN88US=> MlTUV2FPT0WU
NCI-H1693 NGixXplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTF4LkO4NFIh|ryP MlrHV2FPT0WU
KARPAS-299 NY\ndG9lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2fydWlEPTB;MU[uOlIxOyEQvF2= M2T2[HNCVkeHUh?=
UACC-257 NG\QO4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HiOWlEPTB;MUeuNFU5OiEQvF2= NXXsOm5FW0GQR1XS
RKO NV3TPWozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjwVHFxUUN3ME2xO{43PDN|IN88US=> M2izOHNCVkeHUh?=
HT-29 M4nidmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfZeFNKSzVyPUG3Mlc5QDlizszN M2K2VnNCVkeHUh?=
ES7 M3j0dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjBZ5lDUUN3ME2xPE4yOTJ{IN88US=> NFr5fHlUSU6JRWK=
DEL NILw[mlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHHTWM2OD1zOD6zNVczKM7:TR?= MYXTRW5ITVJ?
BT-549 NEe3R|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zOcGlEPTB;MUiuOFA6OiEQvF2= MljNV2FPT0WU
NCI-H1755 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTF6LkW3NlMh|ryP NEnL[5FUSU6JRWK=
HCE-T MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTF6LkizOFEh|ryP NGm3Wo5USU6JRWK=
LU-139 NYDzTZE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEm5SmFKSzVyPUG5MlA1PThizszN MXPTRW5ITVJ?
ECC10 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPkTWM2OD1zOT6yOFc2KM7:TR?= MnuzV2FPT0WU
769-P NEO1bpdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3jRlRwUUN3ME2xPU43OzN3IN88US=> NWK2R3RCW0GQR1XS
BALL-1 NXOzRWp3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYD0UVNXUUN3ME2xPU43Pzd3IN88US=> M4LkdHNCVkeHUh?=
LXF-289 M1G1d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTF7Lki5O|kh|ryP MVHTRW5ITVJ?
TYK-nu NXvrcY5sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MornTWM2OD1zOT65N|E2KM7:TR?= MVXTRW5ITVJ?
NCI-H630 MnLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnpbZdKSzVyPUG5Mlk{PzhizszN MYLTRW5ITVJ?
EW-18 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnjV5k1UUN3ME2yNE4{QDB{IN88US=> MmfNV2FPT0WU
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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 <1 mg/mL
Ethanol <1 mg/mL
In vivo 4% DMSO+30% PEG 300+5% Tween 80+ddH2O 3mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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

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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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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID