Dasatinib 化学構造
分子量: 488.01

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Quality Control & MSDS

製品説明

  • Compare Src Inhibitors
    Src製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法

製品の説明

生物活性

製品説明 Dasatinib は、野生型ablとSrcのためのSrc/abl阻害剤で、IC50 がそれぞれ 0.6 nM と 0.8 nMです。
ターゲット Abl Src c-Kit (WT)/c-Kit (D816V)
IC50

0.6 nM

0.8 nM [1]

79 nM/37 nM [2]
In vitro試験 Dasatinib is more effective than imatinib in inhibiting the proliferation of Ba/F3 cells expressing wild-type Bcr-Abl and Bcr-Abl mutants, with the exception of T315I. Dasatinib has a two-log (∼325-fold) increased potency relative to imatinib. Dasatinib potently inhibits wild-type Abl kinase and all mutants except T315I over a narrow range. Dasatinib directly targets wild-type and mutant Abl kinase domains and inhibits autophosphorylation and substrate phosphorylation in a concentration-dependent manner. Dasatinib displays 325-fold greater potency compared with imatinib against cells expressing wild-type Bcr-Abl. [1] The percent of colonies of TgE bone marrow cells are decreased from 100% in untreated wells to 4.12% in Dasatinib treated wells. In the presence of Dasatinib, the difference in the percentage of colonies formed by WT and TgE bone marrow cells is statistically significant. Expression of LMP2A is able to promote B lymphocyte survival and proliferation, which can be inhibited by targeting Lyn and/or c-Abl kinases through Dasatinib. [3] Dasatinib treatment inhibits Src signaling, decreases growth, and induces cell cycle arrest and apoptosis in a subset of thyroid cancer cells. Treatment with increasing doses of Dasatinib (0.019 μM to 1.25 μM) for 3 days inhibits the growth of the C643, TPC1, BCPAP, and SW1736 cell lines by about 50% at low nanomolar concentrations, while higher concentrations are required to inhibit the growth of the K1 cell line. Treatment with 10 nM or 50 nM Dasatinib results in a 9-22% increase of cells in the G1 population among BCPAP and SW1736 and K1 cells, and a corresponding 7-18% decrease in the percentage of cells in the S phase. [4]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
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M07e NF61NVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3vO|IhcA>? M{npPWROW09? NFnPRYJKSzVyPUCuNFAyOiEQvF2= NVLRVGlTOTd7NU[wPFA>
ALL3 M4rJfWN6fG:2b4jpZ{BCe3OjeR?= MU[wMlHPxE1? MnfFO|IhcA>? MXzEUXNQ NWfqeIN4UUN3ME2wMlAxODRizszN NEK0XFAyQTh6OUW0NC=>
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BA/F3 NGjTcIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnYdpJUPzJiaB?= NELnTXJFVVOR Mk[5TWM2OD14LkW4PUDPxE1? Mmr6NlMxQDh4NES=
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T cell MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWm3NkBp NUPkeVY3TE2VTx?= Ml7ITY5pcWKrdIOgZY51cSCFREOtJIFv\CCjboTpJGNFOjhvaX7keYNm\CCWIHPlcIwheHKxbHnm[ZJifGmxbjD3bZRpKEmFNUCgc4YhOC5yMEROwG0> MlzBNVcyPTR3MUK=
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MALME-3M M2\FS2N6fG:2b4jpZ{BCe3OjeR?= MnTuO|IhcA>? M1LITWROW09? NFLoXoRIUTVyPU[uOlEh|ryP NEDYW3czPDBzNUOyOy=>
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U937 MWnGeY5kfGmxbjDBd5NigQ>? NXnpdZpuOSEQvF2= NW[1VG5JOSCq MUDEUXNQ NW\zeZM6WmWmdXPld{Bj[XOjbDDUUmZidHCqYTDy[Yxm[XOnIHnuJIh2dWGwIGW5N|ch[2WubIO= Ml\JNVc3QDRyOUm=
U937 M3v0b2Z2dmO2aX;uJGF{e2G7 NIjrNncyKM7:TR?= M17qXFEhcA>? MmTHSG1UVw>? MnjaVoVlfWOnczDMVHMucW6mdXPl[EBVVk[jbIDoZUBz\WynYYPlJIlvKGi3bXHuJHU6OzdiY3XscJM> Mn;rNVc3QDRyOUm=
murine mast cell NIe0dJhHfW6ldHnvckBCe3OjeR?= NW[4Ro9kOSEQvF2= MWiyOEBp NXr6UZJTTE2VTx?= NXXmcXM2UW6qaXLpeJMh[W62aXflck1qdmS3Y3XkJGlNPiC|ZXPy[ZRqd25iaX6gTYdGKHC{aX3l[EBud3W|ZTDtZZN1KGOnbHzzJIF1KDFidV2= NVu5eJBGOTd4OESwPVk>
BV-173 NV7CcWl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTBwMECwNFAxOTB7IN88US=> NGHX[4tUSU6JRWK=
K-562 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGLKVHRKSzVyPUCuNFAxODByMk[2JO69VQ>? NHjLVFRUSU6JRWK=
BL-70 MmXYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXDTWM2OD1yLkCwNFAxODh{MjFOwG0> NV3zVZY4W0GQR1XS
EM-2 NFvFeHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTBwMECwNFAyODhizszN M3XHOHNCVkeHUh?=
LAMA-84 NGLqU4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPPZ5Z[UUN3ME2wMlAxODByM{KxJO69VQ>? NH;jbohUSU6JRWK=
MEG-01 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LzXmlEPTB;MD6wNFAxODl6IN88US=> M324fHNCVkeHUh?=
EoL-1-cell MkT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTBwMECwNFE{OSEQvF2= MWDTRW5ITVJ?
CTV-1 NI\4XW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIS4b|BKSzVyPUCuNFAxODRyNDFOwG0> MXvTRW5ITVJ?
TE-15 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTBwMEC1PFkh|ryP Mn7tV2FPT0WU
NOS-1 M4rRV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjvTWM2OD1yLkCwOlE{KM7:TR?= NVK1b2M{W0GQR1XS
D-336MG MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13qeWlEPTB;MD6wNFY{KM7:TR?= NWLGOZFpW0GQR1XS
LB1047-RCC NFjadIRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7JTWM2OD1yLkCwPVg6KM7:TR?= MUDTRW5ITVJ?
LB996-RCC M4rze2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M13vV2lEPTB;MD6wNFk6OSEQvF2= M1;HTnNCVkeHUh?=
SW982 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXPJR|UxRTBwMEGxNVUh|ryP M2PuSXNCVkeHUh?=
TK10 NFjnWoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDEcFVKSzVyPUCuNFEyPzRizszN M2T0e3NCVkeHUh?=
A704 NXK4VYZTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEexc4ZKSzVyPUCuNFE1QTFizszN MkTVV2FPT0WU
TE-8 NYjBZVJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEW2fGVKSzVyPUCuNFE2PzZizszN NFzzeIJUSU6JRWK=
DOHH-2 Mlr0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HSV2lEPTB;MD6wNVcyQSEQvF2= MYHTRW5ITVJ?
HOP-62 M4DDVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHFTWM2OD1yLkCxPFM1KM7:TR?= Ml\5V2FPT0WU
TE-12 M1XGfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHTdHZKSzVyPUCuNFE5PjFizszN NVnJRYJsW0GQR1XS
KGN MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rGVWlEPTB;MD6wNVk1OiEQvF2= NVz6V3FZW0GQR1XS
NCI-H1648 NGfrfpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTBwMEKwNVEh|ryP M3vXN3NCVkeHUh?=
OS-RC-2 NV;lOI9IT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPSTWM2OD1yLkCyNFMh|ryP NWizXFltW0GQR1XS
GB-1 M4qwV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\QOmlEPTB;MD6wNlE2PyEQvF2= MnfEV2FPT0WU
RXF393 M{O0e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjoTWM2OD1yLkCyN|U4KM7:TR?= MVzTRW5ITVJ?
LC-2-ad NUH6[Jk6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fGU2lEPTB;MD6wNlU5PiEQvF2= NFPnRodUSU6JRWK=
KS-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M170dGlEPTB;MD6wNlc{KM7:TR?= NH:4WXRUSU6JRWK=
ETK-1 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrBXVJKSzVyPUCuNFI5OzJizszN M3TsbHNCVkeHUh?=
SW954 NIfXc2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLsS2xnUUN3ME2wMlAzQTJ5IN88US=> NXnzSVJUW0GQR1XS
Becker NVziVFV{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PDXmlEPTB;MD6wN|AxOyEQvF2= MUHTRW5ITVJ?
MZ1-PC MkDWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjzbphKSzVyPUCuNFMyOTlizszN NHjJfZFUSU6JRWK=
ES6 NXXyZ3lwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vBfGlEPTB;MD6wN|E6OyEQvF2= MUPTRW5ITVJ?
KURAMOCHI MmPaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTBwMEO0PFch|ryP MWfTRW5ITVJ?
CGTH-W-1 M4jKemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH7DSpNKSzVyPUCuNFM2PDhizszN NW\vfY15W0GQR1XS
VA-ES-BJ MnjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PCcWlEPTB;MD6wN|kxOiEQvF2= MmH2V2FPT0WU
LXF-289 NYG3eZRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn3xTWM2OD1yLkCzPVU3KM7:TR?= NVjxRW94W0GQR1XS
MPP-89 NXHIToV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mmf2TWM2OD1yLkC0NFQ6KM7:TR?= NV3iU4l7W0GQR1XS
SW872 Ml24S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTBwMESxOlEh|ryP NIXJVY1USU6JRWK=
SNB75 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjvTWM2OD1yLkC0OFM2KM7:TR?= NYLseZd3W0GQR1XS
PSN1 NGr3[pVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjQNG9KSzVyPUCuNFQ1PzRizszN NVm3WnhqW0GQR1XS
LB831-BLC NWfKT4pTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTBwMES2NFkh|ryP MnjJV2FPT0WU
MFH-ino MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETQXGhKSzVyPUCuNFQ4OjRizszN MWPTRW5ITVJ?
TGBC24TKB NGXSSG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXj5NlRLUUN3ME2wMlA1PzZzIN88US=> M2\D[3NCVkeHUh?=
A388 M2K4cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnK1TWM2OD1yLkC1NFk2KM7:TR?= MXvTRW5ITVJ?
BB30-HNC M2fI[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3nUcGlEPTB;MD6wOVQ{PyEQvF2= Mk\QV2FPT0WU
GI-ME-N M4D2[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTBwME[xNVgh|ryP MXfTRW5ITVJ?
TGBC1TKB NIfRSlVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTBwME[xOlQh|ryP MmC1V2FPT0WU
TE-10 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mli5TWM2OD1yLkC2N|U4KM7:TR?= M{HoZ3NCVkeHUh?=
A498 NHjpNWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17mUGlEPTB;MD6wO|I5PCEQvF2= NYrJdldIW0GQR1XS
TE-11 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlHFTWM2OD1yLkC3PFU5KM7:TR?= NHm0dlRUSU6JRWK=
BB65-RCC MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTBwMEiyNlch|ryP NXTReotLW0GQR1XS
C2BBe1 MoX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEn2bZhKSzVyPUCuNFg{ODhizszN Mm\aV2FPT0WU
NCI-H747 M{TpWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPQWFNKSzVyPUCuNFg{PjJizszN NVvWWVhWW0GQR1XS
IST-MES1 NU\tWpFYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIL1bnJKSzVyPUCuNFg2PTJizszN M12zZXNCVkeHUh?=
KALS-1 M3f0VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTBwMEm0PUDPxE1? MUDTRW5ITVJ?
GCIY NHXvdZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUnJR|UxRTBwMEm2OVYh|ryP NHvKcI5USU6JRWK=
RL95-2 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYL6XpExUUN3ME2wMlExOzhizszN M4jqRnNCVkeHUh?=
TE-1 M37JVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTBwMUC1OEDPxE1? M2H0UHNCVkeHUh?=
NCI-H1355 MoDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHEbZdKSzVyPUCuNVExOjhizszN NE\BTpZUSU6JRWK=
SW962 NFXTbZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDpdZZKSzVyPUCuNVEzQTJizszN NWLIPXJWW0GQR1XS
KLE MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnRO5FiUUN3ME2wMlEyOzF5IN88US=> M2LBV3NCVkeHUh?=
MC116 NGHBW3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTBwMUG0NUDPxE1? M4PHXnNCVkeHUh?=
NMC-G1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXS4PIFyUUN3ME2wMlEyPjB4IN88US=> M4XofXNCVkeHUh?=
KU812 M1TkZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jKWWlEPTB;MD6xNVg5OyEQvF2= NXi1e5dJW0GQR1XS
COLO-829 M2TvOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnL4TWM2OD1yLkGyNlE{KM7:TR?= MVrTRW5ITVJ?
NTERA-S-cl-D1 Mn;IS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmnkTWM2OD1yLkGyNlg{KM7:TR?= NV36eWZVW0GQR1XS
IST-MEL1 NVzIOotqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTBwMUO0OUDPxE1? MVnTRW5ITVJ?
MLMA Ml2yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI[0UXhKSzVyPUCuNVQxOzJizszN MmHJV2FPT0WU
LS-123 M3zsOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTBwMUSwOlQh|ryP M1eyeXNCVkeHUh?=
LB2518-MEL MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTBwMUSxOlIh|ryP NV\DU4FNW0GQR1XS
NB69 NXnF[nZwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUi2ZYN[UUN3ME2wMlE1PDN4IN88US=> MkjsV2FPT0WU
8-MG-BA MkfPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3r5NWlEPTB;MD6xOVQ2QCEQvF2= NHPr[GpUSU6JRWK=
K5 NIXje4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfjWItKSzVyPUCuNVY1QDlizszN Mn\DV2FPT0WU
KINGS-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfTTlJpUUN3ME2wMlE3PjZ4IN88US=> MmO5V2FPT0WU
SF268 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjQTWM2OD1yLkG3OFA1KM7:TR?= MX\TRW5ITVJ?
PF-382 NWrQW|lCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\0WlVKUUN3ME2wMlE4Pjd6IN88US=> NF\NZnNUSU6JRWK=
SH-4 NVj0R2EzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWq0S4FnUUN3ME2wMlE5PDF|IN88US=> M3rnbXNCVkeHUh?=
NALM-6 Mn\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXj6UWNmUUN3ME2wMlE6Ojl3IN88US=> MnfUV2FPT0WU
CP66-MEL NUfoOYR7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\x[mxKSzVyPUCuNVk2OzFizszN NGDlSYRUSU6JRWK=
697 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTSOlBKSzVyPUCuNVk6QDdizszN MnT3V2FPT0WU
CP67-MEL NYPw[G92T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjIPHViUUN3ME2wMlIxPDh6IN88US=> NGKz[IdUSU6JRWK=
DSH1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXXJR|UxRTBwMkSwNFEh|ryP Mln2V2FPT0WU
HCE-4 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTLd2F1UUN3ME2wMlI3PDN7IN88US=> NEPubGRUSU6JRWK=
MZ2-MEL MlL1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLU[45UUUN3ME2wMlI5PTN5IN88US=> NFnNOmxUSU6JRWK=
BL-41 NVKxS|U2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTBwMkmxNlMh|ryP MVnTRW5ITVJ?
HUTU-80 NHXUWJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTBwM{G0NkDPxE1? MkPrV2FPT0WU
LOXIMVI M3SzVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTBwM{G1NFMh|ryP Mnq4V2FPT0WU
no-10 MlLSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTBwM{G5N|Eh|ryP MkXoV2FPT0WU
KARPAS-422 NF;rR3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTBwM{O5PVch|ryP NGK1dHpUSU6JRWK=
SW684 M2fmOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mly3TWM2OD1yLkO0PVgh|ryP NH\NWpdUSU6JRWK=
SF126 NIqwPHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGS4OIlKSzVyPUCuN|U1OSEQvF2= Mo\kV2FPT0WU
D-263MG NXHXSYlDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\ZTWM2OD1yLkO2NlI1KM7:TR?= MUnTRW5ITVJ?
OVCAR-4 M3X3cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXKyXFRNUUN3ME2wMlM4PDN|IN88US=> NWjjWoREW0GQR1XS
BB49-HNC Ml3FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rYO2lEPTB;MD6zPFU6QSEQvF2= NVLwZZFiW0GQR1XS
ONS-76 M2fZTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX36fJE3UUN3ME2wMlQzQTVzIN88US=> MmiyV2FPT0WU
MZ7-mel MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTBwNEe5NVEh|ryP M3;tU3NCVkeHUh?=
RCC10RGB NXTlZZViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTBwNEmxNUDPxE1? Mn7TV2FPT0WU
BOKU MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3jOV2lEPTB;MD60PVE{OyEQvF2= M2PQd3NCVkeHUh?=
no-11 MlXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXPVHBKSzVyPUCuOVAzOjhizszN NXPvZZJqW0GQR1XS
IST-SL2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfWcHVKSzVyPUCuOVA{ODJizszN MoXTV2FPT0WU
RKO NH:2[XFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjNTWM2OD1yLkWyPVY3KM7:TR?= Moq5V2FPT0WU
HT-144 NHnoU4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml\VTWM2OD1yLkWzOlA6KM7:TR?= NHvHbnJUSU6JRWK=
NCI-H446 MmH3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2qwVWlEPTB;MD62Nlc3KM7:TR?= NI\aR3BUSU6JRWK=
QIMR-WIL MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTBwN{C2Nlkh|ryP NHfKSmNUSU6JRWK=
MHH-PREB-1 NHnUXGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn31TWM2OD1yLke0OFY6KM7:TR?= MoLzV2FPT0WU
EW-16 M3\mNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfMTVROUUN3ME2wMlc3OTd6IN88US=> M4f2[nNCVkeHUh?=
EW-24 NYjyOG94T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{HSNmlEPTB;MD63PFE3PSEQvF2= MX;TRW5ITVJ?
LB373-MEL-D NXfBU|FVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorQTWM2OD1yLkiyOVA5KM7:TR?= MmW0V2FPT0WU
TE-9 M3jwOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUK4S2ZSUUN3ME2wMlg4PTN{IN88US=> M2fJXXNCVkeHUh?=
A3-KAW MnzzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1ry[GlEPTB;MD65PFQ2OiEQvF2= NWXmNYd{W0GQR1XS
A101D M1vKemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjNTWM2OD1zLkCzNFQ{KM7:TR?= MkLDV2FPT0WU
OCUB-M MlHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTFwMES0NVIh|ryP M120cHNCVkeHUh?=
ES4 NETNR2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXMTWM2OD1zLkC1NVQ2KM7:TR?= NFqyZ|VUSU6JRWK=
TE-6 NVf6[FJjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\ncmRwUUN3ME2xMlIyOjJ4IN88US=> NFHmN3pUSU6JRWK=
D-502MG MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDPdoJWUUN3ME2xMlI{Ozd4IN88US=> MV;TRW5ITVJ?
KNS-42 NUDlVpJST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2[3VGlEPTB;MT6yOFQyOiEQvF2= MWnTRW5ITVJ?
SNU-C2B NEjWOo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVu3eHRiUUN3ME2xMlMxPTh7IN88US=> MnzPV2FPT0WU
NCI-H1838 M3rtdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTFwM{C3N|Mh|ryP MnnwV2FPT0WU
NKM-1 NF\1WmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTFwM{C4OVkh|ryP MWPTRW5ITVJ?
GI-1 Mne3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XFUWlEPTB;MT6zOlIzKM7:TR?= MYLTRW5ITVJ?
NB5 MlvUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVz0W2h6UUN3ME2xMlM6QDJ5IN88US=> M2D4T3NCVkeHUh?=
CAS-1 Mk\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTFwNEC5PVIh|ryP NVrx[mRuW0GQR1XS
HCE-T MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4Psd2lEPTB;MT61OlcyPCEQvF2= NVnPdIZpW0GQR1XS
SBC-1 M{TyeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mon1TWM2OD1zLkW3PVg1KM7:TR?= MWrTRW5ITVJ?
JiyoyeP-2003 Mni3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTFwN{O0OlYh|ryP M1vuZ3NCVkeHUh?=
TE-5 MmLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIOyOVNKSzVyPUGuO|kyOzlizszN Mly1V2FPT0WU
CAN NUjGXFl3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTFwOEKyOVIh|ryP NWG1dpR[W0GQR1XS
SK-UT-1 NWfDfVBjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DwXmlEPTB;Mj6xOlY6OyEQvF2= Mor2V2FPT0WU
JVM-2 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTJUZNrUUN3ME2yMlM3Ojh2IN88US=> MWjTRW5ITVJ?
LB771-HNC NVPw[mN6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV[5XGd2UUN3ME2yMlU4PTVzIN88US=> NHTTN2RUSU6JRWK=
NCCIT NV\FXXJET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zsZ2lEPTB;Mj64OlYyPiEQvF2= MoXxV2FPT0WU
NCI-H2126 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTJwOEe1OVIh|ryP NXm5TWw{W0GQR1XS
Calu-6 MlLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTNwMEW3OFEh|ryP M4e5NXNCVkeHUh?=
SK-LMS-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTNwMUG4PFYh|ryP MV;TRW5ITVJ?
ARH-77 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTNwNE[5NVUh|ryP NIT6[mlUSU6JRWK=
NB17 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITkflhKSzVyPUOuOlM5PDdizszN MWrTRW5ITVJ?
A253 NF7PbmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jISmlEPTB;Mz63N|I1PiEQvF2= MX\TRW5ITVJ?
OPM-2 NGT5b49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTRwMke2PFUh|ryP NX7hU4J3W0GQR1XS
MV-4-11 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXTZnFKSzVyPUSuN|Y1PTRizszN M3[3UHNCVkeHUh?=
SR MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fUNmlEPTB;ND60PVk2PCEQvF2= NUKyXJRYW0GQR1XS
KG-1 NFXnN|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnJUIZ3UUN3ME20MlYxQDR3IN88US=> MoHpV2FPT0WU
OCI-AML2 NWfaUINkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLITWM2OD13Lki2NVU1KM7:TR?= Mn3IV2FPT0WU
D-247MG MnmyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWT3eWhRUUN3ME22MlEzPTF7IN88US=> M1X3[XNCVkeHUh?=
DJM-1 MoHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmOxTWM2OD14LkS4OVU5KM7:TR?= NGLSOmZUSU6JRWK=
RPMI-6666 NY\iNlhmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPXRVc1UUN3ME23MlI4ODZ5IN88US=> MlTkV2FPT0WU
KARPAS-45 M2r6[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XaO2lEPTB;Nz61NVY4OSEQvF2= MnT2V2FPT0WU
LP-1 NIDUc4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUfTflR6UUN3ME23MlU1Pzh{IN88US=> MkLGV2FPT0WU
RS4-11 NH\we5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mmj2TWM2OD15Lk[1O|g4KM7:TR?= NUXJc4pHW0GQR1XS
DU-4475 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEG3ZlNKSzVyPUiuNlE3PTJizszN M{DNUXNCVkeHUh?=
MONO-MAC-6 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DXNmlEPTB;OD6yO|A3PiEQvF2= NGH1TIRUSU6JRWK=
NCI-SNU-16 NYHrd3NHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRThwNU[xNlgh|ryP NGLPbJdUSU6JRWK=
SJSA-1 M3XpRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkj4TWM2OD16LkeyPFA2KM7:TR?= NXrLb|B{W0GQR1XS
MMAC-SF M1;aSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\PN5I1UUN3ME24Mlc6OzB5IN88US=> M12xeXNCVkeHUh?=
SK-NEP-1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTIXVFIUUN3ME24Mlg6OTV3IN88US=> NIKxemZUSU6JRWK=
J-RT3-T3-5 M1rsXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3H4b2lEPTB;OD65OlUzQSEQvF2= NYjIVnVLW0GQR1XS
SKM-1 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTlwMEG3N|Qh|ryP M4W5WnNCVkeHUh?=
LB2241-RCC NUn5e3BST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVz5bFJIUUN3ME25MlAzODF{IN88US=> NWPuN5N3W0GQR1XS
SIG-M5 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRTlwMEK0PVMh|ryP NEi4NpVUSU6JRWK=
EVSA-T NIDudXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYDJR|UxRTlwMke3PVMh|ryP M4rseHNCVkeHUh?=
GT3TKB Mn3pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3ThbWlEPTB;OT6zOVU1PiEQvF2= M4K3U3NCVkeHUh?=
NB6 M3jEeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4[3cWlEPTB;OT65NlI2QSEQvF2= M2j4NXNCVkeHUh?=
EHEB M3jOWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWfJR|UxRTFyLkC2OVYh|ryP MWLTRW5ITVJ?
HEL M{HOPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTFyLkS3O|Yh|ryP MnfFV2FPT0WU
ALL-PO MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojMTWM2OD1zMD63PVM5KM7:TR?= MYPTRW5ITVJ?
TGW NILWWJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTFzLkK4Nlgh|ryP MlHhV2FPT0WU
BC-3 MorSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnwTWM2OD1zMj6xNVM5KM7:TR?= NHuweIVUSU6JRWK=
IA-LM MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1L1VGlEPTB;MUKuOFQ1PSEQvF2= MWPTRW5ITVJ?
UACC-257 M2D5Z2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTF{LkmxPVgh|ryP MoHMV2FPT0WU
KP-N-YS NHft[5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGrIfG1KSzVyPUGyMlkzQDNizszN MVrTRW5ITVJ?
Raji MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2ezdGlEPTB;MUOuO|Q6PyEQvF2= MXzTRW5ITVJ?
SF539 MkjKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWDJR|UxRTF|Lki1OVch|ryP M2DzZnNCVkeHUh?=
DMS-153 MlPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPZTWM2OD1zND6wNFI5KM7:TR?= MXHTRW5ITVJ?
L-540 MnSyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3noT2lEPTB;MUWuNFY4OiEQvF2= MVfTRW5ITVJ?
MN-60 M4jTSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTF3LkG5O|kh|ryP M{CxdXNCVkeHUh?=
RPMI-8866 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHX4U3hKSzVyPUG3MlQ1PTRizszN NEPWSZlUSU6JRWK=
NCI-H510A NFPLe21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzMTWM2OD1zOT6zPVc{KM7:TR?= Mo\HV2FPT0WU
NB13 NEDpd29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\EZWlEPTB;MUmuOFg4PyEQvF2= NFnRR5NUSU6JRWK=
HAL-01 M3rxc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTF7Lke1OFMh|ryP NIr6W5BUSU6JRWK=
NCI-H720 NVfOS|JlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfyfIVKSzVyPUKwMlI4OzNizszN M3zafHNCVkeHUh?=
REH NX3WW21KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTJyLk[zOVch|ryP MWDTRW5ITVJ?
KNS-81-FD M2PFemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3;GdGlEPTB;MkOuNVQ3KM7:TR?= NVTtXHBiW0GQR1XS
HC-1 M3rCcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFy5elFKSzVyPUK0MlU2PTFizszN MWPTRW5ITVJ?
NCI-H2141 NWWzVndIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHvNfGFKSzVyPUK0Mlc4PTRizszN NWX6epZjW0GQR1XS
MOLT-4 NWq2eG1oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjVXVBKUUN3ME2yOk43PzV|IN88US=> MVjTRW5ITVJ?
OMC-1 MlzYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjrW|ZKSzVyPUK3MlE1OjJizszN NWP1VVdKW0GQR1XS
LC-1F NH;6ZYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2r1V2lEPTB;MkeuN|I1PSEQvF2= NG\sS2ZUSU6JRWK=
NCI-H1304 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPzTWM2OD1{OD6xOlI5KM7:TR?= Mo\ZV2FPT0WU
BC-1 NIjJZ49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXLWGNKSzVyPUK4MlY2OSEQvF2= M1\qXXNCVkeHUh?=
NCI-H64 NEXEdVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFXX[YpKSzVyPUK5MlYzPTNizszN Mo\ZV2FPT0WU
MOLT-16 M4jxNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3GxZ2lEPTB;MkmuOlI6OiEQvF2= MYTTRW5ITVJ?
U-87-MG NVfVZ3RjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIH3bW5KSzVyPUOwMlc3PiEQvF2= MWjTRW5ITVJ?
GAK MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkmyTWM2OD1|MT6yOlg3KM7:TR?= MVHTRW5ITVJ?
ES8 MkjIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTN{LkGyOVIh|ryP NUfVeldyW0GQR1XS
HCC1599 M1vJT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvaO5ZUUUN3ME2zNk4{OzJ3IN88US=> NGfJVpVUSU6JRWK=
EB-3 MmSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3vLTGlEPTB;M{SuN|EyPyEQvF2= NYj2XmtpW0GQR1XS
HCC1187 M2[2T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHGfIxKSzVyPUO1MlgxPTJizszN M4GweXNCVkeHUh?=
SK-PN-DW M{nMOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XlPGlEPTB;M{[uNVk1OyEQvF2= M{m4c3NCVkeHUh?=
JVM-3 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHS[5FKSzVyPUO3MlI{OzhizszN NY\s[ZJEW0GQR1XS
HCC2157 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknQTWM2OD1|Nz65PVQ3KM7:TR?= Ml\SV2FPT0WU
A4-Fuk NYPjTJZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrJTWM2OD1|OD6xNFA6KM7:TR?= MUjTRW5ITVJ?
COR-L279 M{fkNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnnWTWM2OD12MD6yPFUyKM7:TR?= MlLRV2FPT0WU
DEL NUPVRnhWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDQTWM2OD12MT65NFg3KM7:TR?= MmLGV2FPT0WU
NCI-H1395 Mo[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILLfoRKSzVyPUSyMlAyPjNizszN MWjTRW5ITVJ?
MHH-NB-11 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTR|LkC4NVgh|ryP NF3le3VUSU6JRWK=
NCI-H2107 NVXRSWZzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTR|LkS4OFYh|ryP NF;kWnBUSU6JRWK=
NEC8 NWDDWo5vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXRSGFwUUN3ME20OE4{OzZizszN M{fKSHNCVkeHUh?=
COLO-684 MoDjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPiXnhKSzVyPUS2MlIzPThizszN MkX5V2FPT0WU
LS-411N MkmxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzQ[WpKSzVyPUS4MlQ4PDhizszN NXrKOnd2W0GQR1XS

... Click to View More Cell Line Experimental Data

In vivo試験 Dasatinib reverses splenomegaly in LMP2A/MYC double transgenic mice. Dasatinib specifically prevents colony formation by LMP2A expressing bone marrow B cells and decreased spleen size in the TgE mice. Spleen mass is significantly decreased among Dasatinib treated Tg6/λ-MYC mice when compared to the control group. Dasatinib inhibits lymphadenopathy in LMP2A/MYC double transgenic mice. Dasatinib reverses splenomegaly in Rag1KO mice engrafted with tumor cells from LMP2A/MYC double transgenic mice. Dasatinib therapy inhibits Lyn phosphorylation in B lymphocyte tumors expressing LMP2A. [3]
臨床試験 Dasatinib has entered in a phase II clinical trial in the treatment of hemangiopericytoma and gastrointestinal stromal tumor.
特集

プロトコル (参考用のみ)

キナーゼアッセイ:

[1]

Kinase autophosphorylation assays Kinase assays using wild-type and mutant glutathione S-transferase (GST)-Abl fusion proteins (c-Abl amino acids 220-498) are done. GST-Abl fusion proteins are released from glutathione-Sepharose beads before use; the concentration of ATP is 5 μM. Immediately before use in kinase autophosphorylation and in vitro peptide substrate phosphorylation assays, GST-Abl kinase domain fusion proteins are treated with LAR tyrosine phosphatase. After 1-hour incubation at 30 °C, LAR phosphatase is inactivated by addition of sodium vanadate (1 mM). Immunoblot analysis comparing untreated GST-Abl kinase to dephosphorylated GST-Abl kinase is routinely done using phosphotyrosine-specific antibody 4G10 to confirm complete (>95%) dephosphorylation of tyrosine residues and c-Abl antibody CST 2862 to confirm equal loading of GST-Abl kinase. The Dasatinib concentration range is extended to 1,000 nM for mutant T315I. These same inhibitor concentrations are used for the in vitro peptide substrate phosphorylation assays. The three inhibitors are tested over these same concentration ranges against GST-Src kinase and GST-Lyn kinase.

細胞アッセイ:

[1]

細胞株 Ba/F3 cell lines
濃度 ~32 nM
反応時間 72 hours
実験の流れ

Ba/F3 cell lines are seeded in triplicate and incubated with escalating concentrations of Dasatinib for 72 hours. Proliferation is measured using a methanethiosulfonate-based viability assay. IC50 and IC90 values are reported as the mean of three independent experiments done in quadruplicate. The inhibitor concentration ranges are 0 nM to 32 nM (Dasatinib). The Dasatinib concentration range is extended to 200 nM for mutant T315I.

動物実験:

[3]

動物モデル EμLMP2A (TgE and Tg6 strains), MYC (λ-MYC), and LMP2A/λ-MYC double transgenic mice (Tg6/λ-MYC)
製剤 DMSO
投薬量 30 mg/kg
投与方法 Administered via i.p.

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

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
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

参考

化学情報

Download Dasatinib SDF
分子量 488.01
化学式

C22H26ClN7O2S

CAS No. 302962-49-8
保管 2年-20℃
6月-80℃in solvent
別名 BMS-354825
溶解度 (25°C) * In vitro DMSO 98 mg/mL (200.81 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 4% DMSO+30% PEG 300+5% Tween 80+ddH2O 5mg/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.
化学名 N-(2-chloro-6-methylphenyl)-2-(6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-ylamino)thiazole-5-carboxamide

カスタマーフィードバック (10)


Click to enlarge
Rating
Source Cell Res, 2011, 21, 1080-1087. Dasatinib purchased from Selleck
Method Microangiography
Cell Lines embryos
Concentrations 30 μM
Incubation Time
Results MEK1/2 may cooperate with VEGFR to regulate blood vessel lumen diameter. We examined this hypothesis by combining VEGFR inhibitor Sunitinib and MEK1/2 inhibitor U0126. Indeed, U0126 (10 µM) combined with Sunitinib (20 µM) resulted in a reduction of vessel lumen size (Figure F), whereas individually they did not. Combined treatment of another MAP kinase signaling pathway inhibitor Dasatinib (20 µM) with Sunitinib (20 µM) produced a similar phenotype as PP1, whereas each individual inhibitor did not result in any vessel shrinkage even at much higher concentrations ( Figure C).Since there are three major VEGF receptors, it is desirable to determine which receptor is involved in combinatory action with MEK1/2. To address this issue, additional highly selective VEGFR inhibitors PTK787 and ZM323881 were tested. Both of these inhibitors (PTK787 or ZM323881), when individually combined with Dasatinib or U0126, induced a reduction of vessel lumen size (Figure D, E, G, and H).

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Rating
Source Clin Cancer Res, 2011, 17, 762-770. Dasatinib purchased from Selleck
Method Assessment of cell viability and apoptosis
Cell Lines B-CLL patient leukemic cells
Concentrations 2-10 μM
Incubation Time 48 h
Results The Dasatinib+Nutlin-3 combination promotes synergistic cytotoxicity in primary CLL cells as well as in p53 wild-type and p53 deleted/ mutated leukemic cell lines.

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Rating
Source Clin Cancer Res, 2011, 17, 762-770. Dasatinib purchased from Selleck
Method Western blot
Cell Lines Leukemic cell lines
Concentrations 10 μM
Incubation Time 24 h
Results Dasatinib marginally affected both the basal levels of p53 and the accumulation of p53 induced by Nutlin-3 in the p53 wild -type cells (Fig. A).Interestingly, however, levels of both MDM2 and p21 proteins, 2 of the best characterized transcriptional targets of p53, weres significantly (P < 0.05) decreased in cells treated with Dasatinib+ Nutlin-3 with respect to cells treated with Nutlin-3 alone (Fig. B).

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Rating
Source Clin Cancer Res, 2011, 17, 762-770. Dasatinib purchased from Selleck
Method Phospho-kinase array analysis
Cell Lines EHEB cell lines/BJAB cell lines
Concentrations 10 μM
Incubation Time 16 h
Results Although Nutlin-3 had no effects on these pathways, Dasatinib alone as well as Dasatinib+Nutlin-3 markedly inhibited the basal phosphorylation of ERK1/2, p38/MAPK, and Akt . Of interest, the combination of Dasatinib+Nutlin-3 selectively enhanced (P < 0.05) the inhibition of Akt phosphorylation with respect to Dasatinib alone, as validated by Western blot analysis.

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Rating
Source Biochem Pharmacol , 2011, 82, 1457-1466. Dasatinib purchased from Selleck
Method MTT assay
Cell Lines MOLM-13 cells, HL-60 cells
Concentrations 1-15 μM
Incubation Time 24-72 h
Results Dasatinib and other TKI decreased the viability of the two myeloid cell lines in a dose- and time-dependent manner. Nevertheless, the anti-leukemic efficacy of Dasatinib and other TKI varied considerably in both cell lines.

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Rating
Source Biochem Pharmacol , 2011, 82, 1457-1466. Dasatinib purchased from Selleck
Method Evaluation of differentiation
Cell Lines MOLM-13 cells, HL-60 cells
Concentrations 5 μM
Incubation Time
Results In a first series of experiments, we assessed four signs of morphological differentiation, May-Gruenwald-Giemsa staining of MOLM-13 cells demonstrated that dasatinib induced a dose-dependent decrease in cytoplasmic basophilia and in the nucleo-cytoplasmic ratio. Dasatinib also led to the appearance of dented nuclei and cytoplasmic granulation( Fig.A and B).In HL-60 cells,dasatinib(5 μM) once more exhibited the highest differentiation-inducing capacity. Thus dasatinib diminished basophilia of the cytoplasm concomitantly with the nucleo-cytoplasmic ratio, and induced the appearance of nuclear lobulation and cytoplasmic granules(Fig. G). Next, we determined the degree of CD11b expression, a marker indicating myeloid differentiation, in TKI-treated MOLM-13 dasatinib exhibited the most pronounced capacity to increase CD11b surface expression( Fig. C and D).To corroborate the TKI-driven differentiation, we quantified the enzymatic activity of alkaline phosphatase by means of the NBT-reduction assay after an incubation period of 6 days in MOLM-13 cells.,Once again, the NBT-reductive activity was highest in cells treated with dasatinib, which was as active as the positive control, ATRA( Fig. E and F)

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Source Invest New Drugs , 2010, 30, 417-422. Dasatinib purchased from Selleck
Method Assessment of cell viability
Cell Lines leukemic cells
Concentrations 10 μM
Incubation Time 24/48 h
Results Dasatinib dose-dependently reduced cell viability in all leukemic cell lines, with variable efficacy irrespect ively of the p53 status. In particular, when used at 10 μM, Dasatinib induced a progressive decrease of the total number of viable cells ranging from approximately 30% (JVM-2 and MEC-2) to 50% (EHEB and BJAB) after 48 h of treat ment (Fig.a). In order to investigate whet her the decreased leukemic cell viability was mainly due to either cytotoxic or cytostatic activity, we have analyzed the effects of Dasatinib on apoptosis,As shown in Fig. b, exposure to Dasatinib induced a significant (p < 0.05) increase of apoptosis in all leukemic cell lines, as evaluated by Annexin-V/PI staining at 48 h of treatment.

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Rating
Source Invest New Drugs , 2010, 30, 417-422. Dasatinib purchased from Selleck
Method phospho-kinase array analysis
Cell Lines EHEB (p53wt) cell lines, BJAB (p53mut) B cell lines
Concentrations
Incubation Time 24 h
Results As shown in Fig. a , the most evident effects of Dasatinib in both cell models were represented by a significant down-regulation of the phosphorylation levels of p38 MAPK, ERK1/2 and CREB. In addition, densitometric analysis of the phospho-kinase array demonstrated that Dasatinib also inhibited the phosphorylation levels of several STAT family members (STAT1, STAT2, STAT3, STAT5a/b and STAT6), the most evident effect in both p53 wild-type (EHEB) and p53 mutated (BJAB) cell lines being on STAT2, STAT3 and STAT6 (Fig. b)

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Rating
Source Invest New Drugs , 2010, 30, 417-422. Dasatinib purchased from Selleck
Method Western blot
Cell Lines p53wild-type(EHEB, JVM-2) cell lines, p53mutated(MEC-2, BJAB) cell lines
Concentrations 10 μM
Incubation Time 24 h
Results "Upon exposure to Dasatinib, a decrease of phosphorylated proteins was confirmed by Western blot analys is in all cell lines investigated without significant differences between p53wild-type and p53mutated cell lines.

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Source Dr. Thomas Kruwel of Fraunhofer-Institute for Toxicology and Experimental Medicine-Dasatinib (BMS-354825) purchased from Selleck. Dasatinib purchased from Selleck
Method Cell vability assays
Cell Lines A2C12, Beta D5, Gamma A3, Gamma D12, A549, CaCo2, HepG2 cell lines
Concentrations 0.001-1000 nM
Incubation Time 24/96 h
Results

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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