Nilotinib (AMN-107)

Catalog No.S1033

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

Price Stock Quantity  
USD 91 In stock
USD 70 In stock
USD 210 In stock
USD 470 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Nilotinib (AMN-107) Chemical Structure

Nilotinib (AMN-107) Chemical Structure
Molecular Weight: 529.52

Validation & Quality Control

Customer Product Validation(5)

Quality Control & MSDS

Related Compound Libraries

Bcr-Abl Inhibitors with Unique Features

  • Pan Bcr-Abl Inhibitor

    Imatinib Mesylate (STI571) Multi-target inhibitor of v-Abl, c-Kit and PDGFRIC50=0.6 μM/0.1 μM/0.1 μM.

  • Most Potent Bcr-Abl Inhibitor

    GZD824 Bcr-Abl(WT), IC50=0.34 nM; Bcr-Abl(T315I), IC50=0.68 nM.

  • FDA-approved Bcr-Abl Inhibitor

    Dasatinib Approved by FDA for CML and Ph+ ALL.

  • Newest Bcr-Abl Inhibitor

    GZD824 Orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively.

Product Information

  • Compare Bcr-Abl Inhibitors
    Compare Bcr-Abl Products
  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description Nilotinib (AMN-107) is a Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells.
Targets Bcr-Abl [1]
(Murine myeloid progenitor cells)
IC50 <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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
EoL-1-cellMWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NXKzVI5vUUN3ME2wMlAxODF2NDFOwG0>M{XBcnNCVkeHUh?=
KU812MnOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MV;JR|UxRTBwMECyOFgh|ryPMlT0V2FPT0WU
EM-2MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MnnvTWM2OD1yLkCwOFEh|ryPNXr2cWZ6W0GQR1XS
LAMA-84NUjISG1JT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=Moe5TWM2OD1yLkCwOFkh|ryPNWTwR2ltW0GQR1XS
MEG-01MnHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NXjOd3dGUUN3ME2wMlAxQDJ6IN88US=>M2TaPXNCVkeHUh?=
BV-173NWXtO2dPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MVvJR|UxRTBwMEGwPFkh|ryPMn\lV2FPT0WU
KASUMI-1Mn;lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NV;4XW9VUUN3ME2wMlAzPDF|IN88US=>NVX2cY4zW0GQR1XS
NB7NYO2eWVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NF7GXmhKSzVyPUCuNVM1OzlizszNNWHQVVlMW0GQR1XS
BHT-101NYnFeHROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MoTlTWM2OD1yLk[0NlY{KM7:TR?=M1nNeHNCVkeHUh?=
CGTH-W-1MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M{nVNmlEPTB;MD62OFg4KM7:TR?=NYWxXJNZW0GQR1XS
HMV-IIMXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MUjJR|UxRTBwN{S4O|Qh|ryPMlfwV2FPT0WU
NKM-1NXnVc2w2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MWDJR|UxRTBwOUCxOUDPxE1?NGX3UpBUSU6JRWK=
LB2241-RCCM4\nUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MnziTWM2OD1zLkCyNlI5KM7:TR?=MVrTRW5ITVJ?
NCI-H1703M4e1Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MVHJR|UxRTFwMUi4O{DPxE1?MYrTRW5ITVJ?
BE-13NEnjfY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NInVfHVKSzVyPUGuNlc1OTZizszNMX;TRW5ITVJ?
ACNMnPhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MUnJR|UxRTFwNUWwO|ch|ryPNH\3TINUSU6JRWK=
A204MmHIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NYPqWWp6UUN3ME2xMlU4OjB3IN88US=>NGPtN5RUSU6JRWK=
HOP-62MkTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MVTJR|UxRTFwOEKwO|ch|ryPNXTDR2ZQW0GQR1XS
H9M3PrVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MWPJR|UxRTJwN{O3PVMh|ryPMYXTRW5ITVJ?
HCC1806NULOdFlHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MoHwTWM2OD1{Lke0N|I4KM7:TR?=NIn1TWNUSU6JRWK=
NOS-1NFy1OZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NVzsSmRkUUN3ME2yMlg4OTB{IN88US=>M1vJdHNCVkeHUh?=
RS4-11NIDxZoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NFfnVHVKSzVyPUKuPVA3OjNizszNMYHTRW5ITVJ?
JARNFHTXlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NGS2Z3BKSzVyPUKuPVIxQDRizszNMonpV2FPT0WU
T98GMYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MVrJR|UxRTNwMEGzNVMh|ryPNFy5eIJUSU6JRWK=
NCI-SNU-1NEjSWW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M4HGcmlEPTB;Mz60NFA6OiEQvF2=MnrPV2FPT0WU
SK-MEL-1M1vJbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MWnJR|UxRTNwNEOwNlkh|ryPM1zEeHNCVkeHUh?=
L-363MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NGO0R5BKSzVyPUOuOlEyODdizszNMX\TRW5ITVJ?
SW982M3rTSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MmTJTWM2OD1|Lk[0NVY6KM7:TR?=NFPOeYRUSU6JRWK=
HT-1080M173dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MUXJR|UxRTNwOUG3O|Uh|ryPM{\qfXNCVkeHUh?=
G-402M1nsSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NVnTO3FnUUN3ME20MlMyOjB|IN88US=>Mm\GV2FPT0WU
HOSNWXVdmlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MV7JR|UxRTRwOECyPFIh|ryPNY\q[WFYW0GQR1XS
SK-NEP-1MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?Mmm5TWM2OD12LkizNVkyKM7:TR?=NV\zdHp2W0GQR1XS
HAL-01NGj1VmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NIns[HJKSzVyPUSuPFgzPDJizszNMoHsV2FPT0WU
SBC-1MlK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NH3GZW1KSzVyPUSuPVA6ODdizszNMYXTRW5ITVJ?
CTV-1NVjMWlJnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M1HUb2lEPTB;NT60PFk{QCEQvF2=NX;s[VRbW0GQR1XS
LCLC-103HM1mxeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MUTJR|UxRTVwN{e0O|Eh|ryPM{Hy[HNCVkeHUh?=
RVH-421NGruR5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M4rBfWlEPTB;NT63O|U{PiEQvF2=NYOzdphmW0GQR1XS
K-562MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MmjKTWM2OD13LkmwN|Yh|ryPNVPHdopxW0GQR1XS
CAL-33MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MUnJR|UxRTZwM{GzOVkh|ryPNEfBZlVUSU6JRWK=
MDA-MB-361MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MnLjTWM2OD14LkOzOlk6KM7:TR?=M3H1VnNCVkeHUh?=
IGROV-1NWrrSHRWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MWXJR|UxRTZwNEexPVEh|ryPMX7TRW5ITVJ?
NYM1HONGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NYjYSIFXUUN3ME22MlU{PTl7IN88US=>MUfTRW5ITVJ?
Ramos-2G6-4C10M3fRXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MW\JR|UxRTZwNk[5N|Eh|ryPM{P4THNCVkeHUh?=
HuO9NHLBfHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=Mn;WTWM2OD14LkezPVY1KM7:TR?=MoPtV2FPT0WU
MS-1MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M{\2[WlEPTB;Nz6xNVk2OyEQvF2=MmXBV2FPT0WU
RPMI-8226NVLCXJg6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NI\FbHVKSzVyPUeuNlgzQDdizszNM3u1fHNCVkeHUh?=
HDLM-2MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M2PmWGlEPTB;Nz60NFE1QSEQvF2=MlX6V2FPT0WU
D-566MGNYfN[WpwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M4\GN2lEPTB;Nz60O|E2PSEQvF2=NIi0ZZFUSU6JRWK=
SK-MEL-24MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NVO1RZZyUUN3ME23MlY{Ozl{IN88US=>NX7sdW03W0GQR1XS
COLO-679MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NX7rc|Z[UUN3ME23Mlk5PjdzIN88US=>M1\TS3NCVkeHUh?=
EW-13M{[2e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MnvUTWM2OD16LkOyNFU1KM7:TR?=Mk[xV2FPT0WU
A388MorWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MYjJR|UxRThwM{i0PFEh|ryPMYjTRW5ITVJ?
UM-UC-3NXjaW|k4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NIPqZohKSzVyPUiuOFM6PTZizszNNEDscHRUSU6JRWK=
NUGC-3MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NWLYO5R4UUN3ME24MlU{PTh{IN88US=>NV7F[HhCW0GQR1XS
COLO-668NH:xXGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MnnOTWM2OD16LkW5OFkyKM7:TR?=M1TCT3NCVkeHUh?=
MOLT-4MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NXXFNG5iUUN3ME24MlYzOzV|IN88US=>MYnTRW5ITVJ?
D-423MGNV61Oo15T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NXTkfJBmUUN3ME24Mlg{PzV4IN88US=>MkexV2FPT0WU
CTB-1MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NFT2blZKSzVyPUiuPFcyOjhizszNMWDTRW5ITVJ?
BCPAPMX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MnruTWM2OD17LkCyOVYzKM7:TR?=NIjyXo1USU6JRWK=
GCTMWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MUPJR|UxRTlwMEm4N|Eh|ryPNY\4W3RiW0GQR1XS
ACHNMX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NWrUVnFTUUN3ME25MlI{PjN{IN88US=>Ml7jV2FPT0WU
KYSE-520MlTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?Mo\BTWM2OD17LkOzOFgzKM7:TR?=NWq5b|I5W0GQR1XS
LB771-HNCNXr5XZkzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MUXJR|UxRTlwN{[0PVch|ryPNFn1TWVUSU6JRWK=
MLMAM2\6Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NY\0cVRKUUN3ME2xNE4xOTN{IN88US=>NF7xUFRUSU6JRWK=
HEC-1MorES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?Mnr2TWM2OD1zMD6yPFA1KM7:TR?=NFvTbVRUSU6JRWK=
HL-60NUHXU2J7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=Mmn0TWM2OD1zMD62PFU{KM7:TR?=MkXKV2FPT0WU
A101DNUXRSYpET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NWnnb5h1UUN3ME2xNE45QTJ|IN88US=>MWPTRW5ITVJ?
A2058M2r0S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NF\tVWNKSzVyPUGwMlkzPDVizszNMYjTRW5ITVJ?
KARPAS-45NULzNnA5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MmKyTWM2OD1zMT6wOlM2KM7:TR?=M4K1b3NCVkeHUh?=
697M37wcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NVrXSG11UUN3ME2xNU4zOTBzIN88US=>MWrTRW5ITVJ?
NCI-N87NVToOHdmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MlXNTWM2OD1zMT63O|MyKM7:TR?=M2[xR3NCVkeHUh?=
DSH1Mnj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NGThbpZKSzVyPUGxMlc6PTNizszNM{m4enNCVkeHUh?=
HLENYLXOFJKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NUDRd|VvUUN3ME2xNU45QDN7IN88US=>NF3rW4ZUSU6JRWK=
NCI-H720MlzRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M2[3dWlEPTB;MUKuOlgxOSEQvF2=M{TlXnNCVkeHUh?=
EW-3NFzQelNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MlnETWM2OD1zMj65N|A4KM7:TR?=NWi2[XhwW0GQR1XS
AGSM2nyXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NXf0eXVUUUN3ME2xN{4xOzVzIN88US=>Mm\DV2FPT0WU
ES5MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NWHFdoJ2UUN3ME2xN{4xPTF{IN88US=>M3XhZXNCVkeHUh?=
DBM{P4TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MnjnTWM2OD1zMz6zNlU3KM7:TR?=NXTiN414W0GQR1XS
A4-FukMonlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MU\JR|UxRTF|LkSxNFIh|ryPNUXxXoxVW0GQR1XS
A427MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NVHZ[GNWUUN3ME2xN{41QTd{IN88US=>NUfSdG11W0GQR1XS
MN-60M1ixNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NYf5TpE1UUN3ME2xN{42QDR|IN88US=>NUHETotNW0GQR1XS
HCC2218MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M33kPGlEPTB;MUOuOVg2PiEQvF2=M1zuVXNCVkeHUh?=
MV-4-11MlHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M3:4SmlEPTB;MUOuPFE{PyEQvF2=M{jpNHNCVkeHUh?=
GI-1M{T5PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M36xNmlEPTB;MUSuNVE5PCEQvF2=MXnTRW5ITVJ?
JVM-3NHqxO45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M1LzOWlEPTB;MUSuNlY2PiEQvF2=MVXTRW5ITVJ?
NCI-H2029NVHIeWF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NHXDUJdKSzVyPUG0MlI4OjdizszNNX\6WIVUW0GQR1XS
TE-12NG[1S5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MWDJR|UxRTF2Lk[wOFYh|ryPMYTTRW5ITVJ?
WM-115M2HsdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7Mlj0TWM2OD1zNT61Olg{KM7:TR?=NYfkVIVoW0GQR1XS
BB65-RCCMUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NIG2cGJKSzVyPUG2MlAzPDFizszNMnfIV2FPT0WU
NCI-H1693MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M2HIcWlEPTB;MU[uN|gxOiEQvF2=MVvTRW5ITVJ?
KARPAS-299Mk[yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?Mn\tTWM2OD1zNj62NlA{KM7:TR?=MmHRV2FPT0WU
UACC-257NU\CWJJOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NFy3TZNKSzVyPUG3MlA2QDJizszNNWTuZld5W0GQR1XS
RKOMmKzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MoTHTWM2OD1zNz62OFM{KM7:TR?=NITrRXpUSU6JRWK=
HT-29NF\XbFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MXrJR|UxRTF5Lke4PFkh|ryPMUnTRW5ITVJ?
ES7M2CzeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M3v1bmlEPTB;MUiuNVEzOiEQvF2=M13Yc3NCVkeHUh?=
DELMnXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NXjWXoxHUUN3ME2xPE4{OTd{IN88US=>NInHRmRUSU6JRWK=
BT-549NGS2PXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NFHDfVJKSzVyPUG4MlQxQTJizszNMVTTRW5ITVJ?
NCI-H1755M2[2UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MV3JR|UxRTF6LkW3NlMh|ryPNFfmVpNUSU6JRWK=
HCE-TNFzLbmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NFXsRpVKSzVyPUG4Mlg{PDFizszNM4j1[nNCVkeHUh?=
LU-139MlTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M2XmW2lEPTB;MUmuNFQ2QCEQvF2=MkDSV2FPT0WU
ECC10MlH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MYPJR|UxRTF7LkK0O|Uh|ryPM{no[HNCVkeHUh?=
769-PM3q4fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M2XuVWlEPTB;MUmuOlM{PSEQvF2=NHHsR3NUSU6JRWK=
BALL-1NVrzSG5PT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NUjyOYtEUUN3ME2xPU43Pzd3IN88US=>Mm\oV2FPT0WU
LXF-289MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NUfmNYw4UUN3ME2xPU45QTd7IN88US=>NFfIZYdUSU6JRWK=
TYK-nuNEjrd4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M{XzVWlEPTB;MUmuPVMyPSEQvF2=MmTmV2FPT0WU
NCI-H630NFzHPWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NYD5Z2wyUUN3ME2xPU46Ozd6IN88US=>NHzocGpUSU6JRWK=
EW-18MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MnjVTWM2OD1{MD6zPFAzKM7:TR?=NXz4UXB7W0GQR1XS
KYSE-150MlS4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NE\leJVKSzVyPUKwMlcxPDdizszNNFqxXXlUSU6JRWK=
LOXIMVINFjDZ4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MVXJR|UxRTJyLke1PFYh|ryPMWXTRW5ITVJ?
HuP-T3MmHNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MUnJR|UxRTJzLkC4OVIh|ryPNEG5[lBUSU6JRWK=
MFE-280MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NVfL[WVIUUN3ME2yNU42Pjd7IN88US=>M3W3cXNCVkeHUh?=
SK-OV-3M1i0fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NXS2XGpLUUN3ME2yNU45PDB6IN88US=>M13RNnNCVkeHUh?=
QIMR-WILM4Xjemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M1;tcWlEPTB;MkKuNFQ4QCEQvF2=M{LU[XNCVkeHUh?=
NCI-H69M{nSNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M4fXUmlEPTB;MkKuOFI6QSEQvF2=NFTtdZdUSU6JRWK=
TE-5NEC2R|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=Mon6TWM2OD1{Mj60PVY2KM7:TR?=NI\UNnlUSU6JRWK=
NCI-H1993M3eyemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NEK0UWxKSzVyPUKyMlQ6PzFizszNMVnTRW5ITVJ?
NCI-H1092M4i0c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MmX4TWM2OD1{Mz6yPFQ{KM7:TR?=MnjpV2FPT0WU
RH-1NGP2NpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M3fxfWlEPTB;MkOuOVM2PyEQvF2=NYrHUlRZW0GQR1XS
DBTRG-05MGMWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M4\DcmlEPTB;MkOuPFQ4OiEQvF2=NEDqRYJUSU6JRWK=
Mo-TMmLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M1jGNmlEPTB;MkOuPUDPxE1?NUDzbVBCW0GQR1XS
HD-MY-ZNIHSTIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NWLTNW9nUUN3ME2yOE4zOzZ{IN88US=>M2CzN3NCVkeHUh?=
NCI-H2342Ml\TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M4XiTGlEPTB;MkSuOlc3PyEQvF2=NGjUZnZUSU6JRWK=
C32NXHKNo13T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M3\BbGlEPTB;MkSuPVU4PiEQvF2=M2f4PHNCVkeHUh?=
HTC-C3MoLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M4\uVmlEPTB;MkWuN|U4PyEQvF2=M2WwO3NCVkeHUh?=
NCI-H358NWDpO216T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=M3nufWlEPTB;MkWuN|k1OyEQvF2=MWrTRW5ITVJ?
CAL-85-1MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NEH6V4RKSzVyPUK1MlQ2PzdizszNM3fj[nNCVkeHUh?=
HT-1197NWfCVVF3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=Mn3XTWM2OD1{NT61N|E6KM7:TR?=MYTTRW5ITVJ?
A172NYXvZ2EzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MlfkTWM2OD1{NT63NVM3KM7:TR?=NH;jfJBUSU6JRWK=
SW1573MnLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NGqwfFhKSzVyPUK1Mlc4QDVizszNNX3iemE6W0GQR1XS
EW-24M1ezdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NVH6PFFzUUN3ME2yOU46PjJizszNNF3Q[|BUSU6JRWK=
SK-MEL-2MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NX36fVlOUUN3ME2yOk4xOzF{IN88US=>NVvWSGpRW0GQR1XS
LU-65NX\IZ|ZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MY\JR|UxRTJ4LkC0OVIh|ryPMX7TRW5ITVJ?
KMOE-2MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M3:5[2lEPTB;Mk[uNFkyPSEQvF2=MoLMV2FPT0WU
H-EMC-SSNHnnUHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NH\PZ5dKSzVyPUK2MlQyOTRizszNNEmzNY5USU6JRWK=
H4MmfyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M1jZRWlEPTB;Mk[uOFI1OyEQvF2=NEL3dGRUSU6JRWK=
DU-4475NInXT2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MoXKTWM2OD1{Nz6xPFczKM7:TR?=NXPjV4NHW0GQR1XS
HCT-116NYfyO2cxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MnPZTWM2OD1{Nz60N|Q6KM7:TR?=Ml30V2FPT0WU
MSTO-211HM1rmZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MkHLTWM2OD1{Nz62NlU2KM7:TR?=NWDRbWQ1W0GQR1XS
NCI-H292NF\JVppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NUfCO5lHUUN3ME2yO{46PjF5IN88US=>Mnn6V2FPT0WU
NCI-H446Ml\OS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M1fKXWlEPTB;MkiuNlExPSEQvF2=MYfTRW5ITVJ?
NCI-H2009MkfmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NYPZdoxJUUN3ME2yPU4yPDNzIN88US=>NVjuWWdGW0GQR1XS
MHH-ES-1M1;PZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7M2DxU2lEPTB;MkmuN|Y5PSEQvF2=MV;TRW5ITVJ?
TI-73MnXOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NWT1R5ltUUN3ME2yPU41ODBzIN88US=>NG\wRWZUSU6JRWK=
NCI-H2228NXzZSHJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NXG5epBFUUN3ME2yPU41PThizszNMlS4V2FPT0WU
MHH-PREB-1NULlfncxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NUXU[|NRUUN3ME2yPU42PTB3IN88US=>NVPLZlZkW0GQR1XS
ChaGo-K-1MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M4LXfGlEPTB;MkmuOlA6PyEQvF2=NH64dZZUSU6JRWK=
KY821MlHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MY\JR|UxRTJ7Lk[0N|Mh|ryPMYrTRW5ITVJ?
NCI-H209MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MnntTWM2OD1{OT64N|Y3KM7:TR?=MoPnV2FPT0WU
NBsusSRNV21bYdET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MoHnTWM2OD1{OT65PVA1KM7:TR?=MVjTRW5ITVJ?
NCI-H1304NYXhVYJWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NFnrbZNKSzVyPUOwMlU4OTZizszNMknOV2FPT0WU
NB14M3Had2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MXXJR|UxRTNzLkC0OFYh|ryPMWnTRW5ITVJ?
HCC1419NHzEe2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NF;pd4tKSzVyPUOxMlI1KM7:TR?=NF63WpZUSU6JRWK=
KG-1MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MWHJR|UxRTNzLke0Nlkh|ryPNWDFdZh2W0GQR1XS
A2780MoqwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NEnwNXFKSzVyPUOxMlg{PThizszNNWPGe41TW0GQR1XS
NCI-H28NF\wdHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M{PYPWlEPTB;M{GuPVg3OSEQvF2=NYnhfVNmW0GQR1XS
C2BBe1M{nGSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NViwXYcxUUN3ME2zNk4zPjN2IN88US=>MULTRW5ITVJ?
VA-ES-BJNGnMbYFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MmryTWM2OD1|Mj6zNUDPxE1?NIXrOm1USU6JRWK=
SBC-5M2PqT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7M4LtdWlEPTB;M{KuPFUyOSEQvF2=MUHTRW5ITVJ?
OVCAR-4MlHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MkHpTWM2OD1|Mz60PFQ5KM7:TR?=NIfWeY1USU6JRWK=
COR-L88NIDTZ5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=Ml3NTWM2OD1|ND6wO|QyKM7:TR?=NY\5cmpiW0GQR1XS
SW954MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M120dGlEPTB;M{SuNFc2OiEQvF2=Mn;SV2FPT0WU
COLO-684NIfTWI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NX;iN3hqUUN3ME2zOE4{PDB2IN88US=>MXjTRW5ITVJ?
HCC70MnLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NWDHd4Z7UUN3ME2zOE46PTF2IN88US=>MVvTRW5ITVJ?
NCI-H1770M3r6O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MXnJR|UxRTN2Lkm2NUDPxE1?NXLVTpVmW0GQR1XS
NCI-H1666MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MlSyTWM2OD1|NT64NlU{KM7:TR?=NHKxW3BUSU6JRWK=
YH-13MoHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M{DQTmlEPTB;M{WuPVIh|ryPM1LESnNCVkeHUh?=
DJM-1MkLJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NWCxWotlUUN3ME2zOk45ODR7IN88US=>M2PLXnNCVkeHUh?=
KNS-62M4nFfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NWKwTGtmUUN3ME2zOk46PDN6IN88US=>MYHTRW5ITVJ?
SK-MEL-30MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MUfJR|UxRTN5Lki3N|ch|ryPM1;tdXNCVkeHUh?=
SJRH30Mnz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MWrJR|UxRTN6LkezOFEh|ryPNHvRZXBUSU6JRWK=
GP5dNV7Ub3dmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MVzJR|UxRTN6Lki2OVMh|ryPMWrTRW5ITVJ?
SW1116MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MWnJR|UxRTN7LkK4NFUh|ryPNFztS2RUSU6JRWK=
COLO-800Ml;hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NUiwNGRlUUN3ME2zPU4{PjN6IN88US=>NVTydXB1W0GQR1XS
RDMmLpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M{\3fmlEPTB;M{muOVI2QCEQvF2=M1z3UnNCVkeHUh?=
NCI-SNU-5NUHCbWFCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NX7hVnVNUUN3ME2zPU43QTF4IN88US=>M3z0TnNCVkeHUh?=
HuO-3N1Ml;TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MXPJR|UxRTRyLkGwPEDPxE1?NFjYbY5USU6JRWK=
SK-UT-1M4Xvemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MWXJR|UxRTRyLkW2O|Qh|ryPNWH6NnNPW0GQR1XS
SK-MEL-3MkP6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MVTJR|UxRTRyLkW5N|Ih|ryPMnL4V2FPT0WU
SK-MEL-28NFy5VI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=MkTsTWM2OD12MD62OFM2KM7:TR?=M3i0e3NCVkeHUh?=
SCC-4MkfZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?Mm\hTWM2OD12MT6yNVM4KM7:TR?=MnXaV2FPT0WU
no-11M3HNW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7MXrJR|UxRTRzLkezOVQh|ryPM1;nTHNCVkeHUh?=
HT-144M{foVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M2Tvd2lEPTB;NEKuNFU3PyEQvF2=NXL1S|dWW0GQR1XS
MFM-223MoLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MlfWTWM2OD12Mj60NFIh|ryPMkjoV2FPT0WU
ONS-76MmXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?Mm\4TWM2OD12Mj64NFE5KM7:TR?=NVqzU3B1W0GQR1XS
ES8NFX2enVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NFG2OoNKSzVyPUSzMlM3QThizszNMoHJV2FPT0WU
T-24NEi0bZJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NVruW3B4UUN3ME20N{41OzZ7IN88US=>M2nwcnNCVkeHUh?=
GAMGMUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?Mlj5TWM2OD12Mz60OVE4KM7:TR?=NFfHXIdUSU6JRWK=
LU-135M1ztVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M2ez[GlEPTB;NESuNFkzOyEQvF2=NIHtTWxUSU6JRWK=
HCC1187MmT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?NH\5emdKSzVyPUS0MlgzPjJizszNM4TrNHNCVkeHUh?=
TE-1NXfUeHRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NVjubFE5UUN3ME20OU4yPjV2IN88US=>MV;TRW5ITVJ?
J-RT3-T3-5NIHjcWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=M2fs[GlEPTB;NEWuOFMyPSEQvF2=MVvTRW5ITVJ?
GI-ME-NMXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MYPJR|UxRTR3Lki5OVIh|ryPNEfhOnFUSU6JRWK=
D-392MGMWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MkfFTWM2OD12NT65NlU3KM7:TR?=Ml;jV2FPT0WU
KALS-1M1rnWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7M2r0cmlEPTB;NE[uO|I2PyEQvF2=MleyV2FPT0WU
MMAC-SFNGP6VGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NHO1V4hKSzVyPUS2Mlk6PTJizszNNGPkdVlUSU6JRWK=
HSC-3NHvqUplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NVfOV3E6UUN3ME20O{4{PjB6IN88US=>Mo\pV2FPT0WU
KM-H2NI\RfZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=NYDBS2U6UUN3ME20O{43ODB5IN88US=>NEHTc4NUSU6JRWK=
LoVoNWPjRm5TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MVnJR|UxRTR6LkGwNFIh|ryPMV3TRW5ITVJ?
NCI-H510AM3HNV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7NHXwdlJKSzVyPUS4MlE5PzFizszNMmXpV2FPT0WU
EW-11NXe3Z3pnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NI\WNZZKSzVyPUS4MlI{PDhizszNNITpRndUSU6JRWK=
HCC2998MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?MX3JR|UxRTR6Lk[yN|Yh|ryPMXvTRW5ITVJ?
J82MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NUCxSmhZUUN3ME20PE44OjR{IN88US=>NGnQeW1USU6JRWK=
ML-2Ml32S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M1rjemlEPTB;NEmuOFYxPSEQvF2=NUW1Z2x6W0GQR1XS
NCI-H2030Mn7ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?MXrJR|UxRTR7LkexNVch|ryPM4G2[XNCVkeHUh?=
NCI-H1792MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?M2LzTGlEPTB;NEmuPFUyQCEQvF2=MYXTRW5ITVJ?

... 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]
Features A selective inhibitor of native and mutant Bcr-Abl.

Protocol(Only for Reference)

Cell Assay: [4]

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.

Animal Study: [6]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Weisberg E, et al. Blood. 2007, 109(5), 2112-2120.

[2] Liu Y, et al. J Hepatol. 2011, 55(3), 612-625.

view more

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-05-29)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02709083 Not yet recruiting Chronic Phase Chronic Myelogenous Leukemia, BCR-ABL1 Positive Emory University May 2016 Phase 2
NCT02774512 Not yet recruiting Colon Cancer Institut Bergonié|Novartis Pharmaceuticals May 2016 Phase 0
NCT02611492 Recruiting Philadelphia Chromosome Positive Adult Acute Lymphoblastic Leukemia Assistance Publique - Hôpitaux de Paris April 2016 Phase 3
NCT02602314 Not yet recruiting Chronyc Myeloid Leukemia Gruppo Italiano Malattie EMatologiche dellAdulto March 2016 Phase 4
NCT02546674 Recruiting Chronic Myeloid Leukemia Novartis Pharmaceuticals|Novartis February 2016 Phase 4

view more

Chemical Information

Download Nilotinib (AMN-107) SDF
Molecular Weight (MW) 529.52
Formula

C28H22F3N7O

CAS No. 641571-10-0
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 27 mg/mL (50.98 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
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 Name 4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-(4-(pyridin-3-yl)pyrimidin-2-ylamino)benzamide

Customer Product Validation (5)


Click to enlarge
Rating
Source FASEB J 2011 25, 3661-3673. Nilotinib (AMN-107) purchased from Selleck
Method Analyzing cell apoptosis
Cell Lines Ba/F3-p210T315I cells
Concentrations 0-5 μM
Incubation Time 24 h
Results In a parallel study using imatinib/PDMP or nilotinib/PDMP combinations, to our surprise, similar significant synergy in Ba/F3-p210T315I cells was observed.

Click to enlarge
Rating
Source Molecules 2014 19, 3356-75. Nilotinib (AMN-107) purchased from Selleck
Method Western blot
Cell Lines K562, CD34+CD38- cells
Concentrations 0, 0.01, 0.1, 1 uM
Incubation Time 12 h
Results Since nilotinib targets the Bcr-Abl kinase in CML cells, we evaluated its ability to inhibit kinase activity in ABCB1- and ABCG2-overexpressing CD34+CD38- cells. In K562 cells, nilotinib effectively inhibited the phosphorylation of Bcr-Abl and CrkL (a surrogate marker of Bcr-Abl activity) at a concentration of 0.1 umol/L. However, in CD34+CD38- cells, nilotinib failed to completely inhibit the phosphorylation of Bcr-Abl and CrkL even when cells were exposed to concentration up to 1.0 umol/L.

Click to enlarge
Rating
Source Leukemia Res 2012 36, 1311-1314. Nilotinib (AMN-107) purchased from Selleck
Method Thymidine uptake Uptake assay
Cell Lines K562, MEG-01 cells
Concentrations 0.1-10uM
Incubation Time 20 min
Results Nilotinib was much more potent than imatinib to inhibit nucleoside transport. It prevented the uptake of thymidine in K562 cells by 97% at 10 uM, a level that was similar to the one obtained with the vasodilatator molecule dipyridamole. Nilotinib was also very efficient at 1 and 0.1 uM; it blocked the entry of thymidine by 90 and 74%, respectively (Fig. 2a). With the MEG-01 cell line, nilotinib was also extremely potent and blocked the entry of thymidine by 96, 92 and 60% with 10, 1 and 0.1 uM nilotinib, respectively (Fig. 2b).

Click to enlarge
Rating
Source Urol Oncol 2014 0.1016/j.urolonc.2014.06.001. Nilotinib (AMN-107) purchased from Selleck
Method Immunoblot analyses
Cell Lines LNCaP, PC-3, DU-145 cells
Concentrations 10 uM
Incubation Time 24 h
Results It shows a robust overexpression of phospho-ERK1/2 T202/Y204 in nilotinib-treated DU-145 cells (B). An up-regulation of phospho-ERK1/2 T202/Y204 was also detectable in nilotinib-treated LNCaP cells, albeit at a lower level, and was not found in PC-3 cells (C).

Click to enlarge
Rating
Source Urol Oncol 2014 0.1016/j.urolonc.2014.06.001. Nilotinib (AMN-107) purchased from Selleck
Method Immunohistochemical staining
Cell Lines Xenografted DU-145 cells
Concentrations 5 mg/kg/d
Incubation Time 21 days
Results Accoding to published animals experiments, DU-145 xenografts from a representative experiment in which nilotinib was used at a 75-mg/kg/d concentration. It's found a significant increase of phospho-ERK-positive residual tumor cells from a mean of 67.5 cells per high-powerfield in controls to 131.1 cells per high-powerfield in DU-145 xenografts treated for 21 days with nilotinib (P< 0.0005).

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.

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

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

* Indicates a Required Field

Related Bcr-Abl Products

  • PX-478 2HCl

    PX-478 2HCl is an orally active, and selective hypoxia-inducible factor-1α (HIF-1α) inhibitor. Phase 1.

  • Defactinib (VS-6063, PF-04554878)

    Defactinib (VS-6063, PF-04554878) is a selective, and orally active FAK inhibitor. Phase 2.

  • SU6656

    SU 6656 is a selective Src family kinase inhibitor with IC50 of 280 nM, 20 nM, 130 nM, and 170 nM for Src, Yes, Lyn, and Fyn, respectively.

  • Imatinib Mesylate (STI571)

    Imatinib Mesylate (STI571) is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively.

  • Ponatinib (AP24534)

    Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively.

  • Bafetinib (INNO-406)

    Bafetinib (INNO-406) is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit. Phase 2.

    Features:Dual Bcr-Abl/Lyn inhibitor.

  • Degrasyn (WP1130)

    Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT).

    Features:WP1130 has an advantage over imatinib mesylate in that its activity is not inhibited by a variety of Abl kinase mutations, including T315I.

  • DCC-2036 (Rebastinib)

    DCC-2036 (Rebastinib) is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, also inhibits SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit. Phase 1.

    Features:A conformational control inhibitor of Abl1 and T315I Abl1.

  • GZD824 Dimesylate

    GZD824 Dimesylate is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively.

  • GNF-2

    GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl, shows no activity to Flt3-ITD, Tel-PDGFR, TPR-MET and Tel-JAK1 transformed tumor cells.

Recently Viewed Items

Tags: buy Nilotinib (AMN-107) | Nilotinib (AMN-107) ic50 | Nilotinib (AMN-107) price | Nilotinib (AMN-107) cost | Nilotinib (AMN-107) solubility dmso | Nilotinib (AMN-107) purchase | Nilotinib (AMN-107) manufacturer | Nilotinib (AMN-107) research buy | Nilotinib (AMN-107) order | Nilotinib (AMN-107) mouse | Nilotinib (AMN-107) chemical structure | Nilotinib (AMN-107) mw | Nilotinib (AMN-107) molecular weight | Nilotinib (AMN-107) datasheet | Nilotinib (AMN-107) supplier | Nilotinib (AMN-107) in vitro | Nilotinib (AMN-107) cell line | Nilotinib (AMN-107) concentration | Nilotinib (AMN-107) nmr
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us