Dasatinib 化学構造
分子量: 488.01

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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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K562 NFTvT3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTLO|IhcA>? NHjFfIFFVVOR NFrzbolKSzVyPUCuNFAyKM7:TR?= NXjuUHA3OTd7NU[wPFA>
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ALL3 NInlV5FEgXSxdH;4bYMhSXO|YYm= M4TD[FAvOc7:TR?= MXW3NkBp MXzEUXNQ NEfaTIJKSzVyPUCuNFAxPCEQvF2= MX[xPVg5QTV2MB?=
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BA/F3 MnfES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3TR|UzPzJiaB?= M{PZb2ROW09? M3n5VGlv\HWlZYOgZ5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmEwTjNiY3XscJMh\XiycnXzd4lv\yCEQ2KtRWJNKEV|NUnWJI12fGGwdDDhd5Nme3OnZDDhd{Boem:5dHigTY5pcWKrdHnvckB4cXSqIFnDOVAhd2ZiMD6wNFE{|ryP NWfOPYZOOjN|MEG3NFM>
BA/F3 M1PnU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXG3NkBp NInTTo1FVVOR MXzJcoR2[2W|IHP5eI91d3irY3n0fUBi\2GrboP0JI1wfXOnIFLBM2Y{KGOnbHzzJIV5eHKnc4Ppcochf2muZDD0fZBmKEKFUj3BRmwh[XO|ZYPz[YQh[XNiZ4Lve5RpKEmwaHnibZRqd25id3n0bEBKSzVyIH;mJFAvODBzOd88US=> MkDQNlM{ODF5MEO=
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T cell MlX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnsU|A4OiCq MlPKSG1UVw>? MWTJcohq[mm2czDhcpRqKEOGMz2gZY5lKGGwdHmgR2QzQC2rbnT1Z4VlKFRiY3XscEBxem:uaX\ldoF1cW:wIIfpeIghUUN3MDDv[kAxNjByM988US=> M2T0R|E4OTV2NUGy
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U937 M1Hk[WZ2dmO2aX;uJGF{e2G7 M1rvblEh|ryP NHjGXnkyKGh? NH7FWItFVVOR MnfQVoVlfWOnczDiZZNidCCWTl\hcJBp[SC{ZXzlZZNmKGmwIHj1cYFvKFV7M{egZ4VtdHN? MUSxO|Y5PDB7OR?=
U937 MnzPSpVv[3Srb36gRZN{[Xl? M4PQ[VEh|ryP NF7vdnMyKGh? NEXCe2dFVVOR MX\S[YR2[2W|IFzQV{1qdmS3Y3XkJHRPTmGucHjhJJJmdGWjc3WgbY4hcHWvYX6gWVk{PyClZXzsdy=> NGH4[W4yPzZ6NEC5PS=>
murine mast cell MnW1SpVv[3Srb36gRZN{[Xl? NYHZOpJyOSEQvF2= MWmyOEBp M1q1NGROW09? MojzTY5pcWKrdIOgZY51cWenbj3pcoR2[2WmIFnMOkB{\WO{ZYTpc44hcW5iSXfFJJBzcW2nZDDtc5V{\SCvYYP0JINmdGy|IHH0JFEhfU1? NX\tWppbOTd4OESwPVk>
BV-173 NX\weoVoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlG5TWM2OD1yLkCwNFAxODFyOTFOwG0> NYDvfW9iW0GQR1XS
K-562 M2jHfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHG4VpZKSzVyPUCuNFAxODByMk[2JO69VQ>? MoPCV2FPT0WU
BL-70 NXm4XVB{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zZU2lEPTB;MD6wNFAxODB6MkKg{txO MX\TRW5ITVJ?
EM-2 M3HHSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVu3dYo1UUN3ME2wMlAxODByMUC4JO69VQ>? NV7Y[Fl6W0GQR1XS
LAMA-84 M3Hv[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTBwMECwNFA{OjFizszN NIPpRoNUSU6JRWK=
MEG-01 NEH5WHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljQTWM2OD1yLkCwNFAxQThizszN MmrBV2FPT0WU
EoL-1-cell M{TU[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXydpN5UUN3ME2wMlAxODBzM{Gg{txO M4XWPXNCVkeHUh?=
CTV-1 MmHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PmPGlEPTB;MD6wNFAxPDB2IN88US=> NWDySFBiW0GQR1XS
TE-15 NX23dFh[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37HXGlEPTB;MD6wNFU5QSEQvF2= M3jicHNCVkeHUh?=
NOS-1 M1i1O2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fWUGlEPTB;MD6wNFYyOyEQvF2= M2q1UnNCVkeHUh?=
D-336MG M2jN[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\NTWM2OD1yLkCwOlMh|ryP Mnj6V2FPT0WU
LB1047-RCC NUi1SVk4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTBwMEC5PFkh|ryP NFPnOIpUSU6JRWK=
LB996-RCC NVzvNVhTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWrqPHdiUUN3ME2wMlAxQTlzIN88US=> M4q2dXNCVkeHUh?=
SW982 Mn7lS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmPTTWM2OD1yLkCxNVE2KM7:TR?= MY\TRW5ITVJ?
TK10 MlPDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTBwMEGxO|Qh|ryP MXPTRW5ITVJ?
A704 MnjZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NULHVoFyUUN3ME2wMlAyPDlzIN88US=> MUXTRW5ITVJ?
TE-8 M2[4Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mon4TWM2OD1yLkCxOVc3KM7:TR?= NV;LR5NUW0GQR1XS
DOHH-2 M1PxW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULTfod7UUN3ME2wMlAyPzF7IN88US=> MUDTRW5ITVJ?
HOP-62 NGXxfYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4XzRmlEPTB;MD6wNVg{PCEQvF2= M3X1NnNCVkeHUh?=
TE-12 NVHjWGNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHftZ4dKSzVyPUCuNFE5PjFizszN Mn3wV2FPT0WU
KGN NHXpPHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTBwMEG5OFIh|ryP M{n6bnNCVkeHUh?=
NCI-H1648 NIG1c2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTBwMEKwNVEh|ryP Mmq5V2FPT0WU
OS-RC-2 NFLGPYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DFVGlEPTB;MD6wNlA{KM7:TR?= MkXZV2FPT0WU
GB-1 NIHNNYVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXGSllKSzVyPUCuNFIyPTdizszN M2DTVnNCVkeHUh?=
RXF393 Mn;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDnTWM2OD1yLkCyN|U4KM7:TR?= M3PoUHNCVkeHUh?=
LC-2-ad MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEW1UndKSzVyPUCuNFI2QDZizszN MmPpV2FPT0WU
KS-1 M1q5UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TDdGlEPTB;MD6wNlc{KM7:TR?= NHfQWZVUSU6JRWK=
ETK-1 NIH6NI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3z4R2lEPTB;MD6wNlg{OiEQvF2= NGTtXWpUSU6JRWK=
SW954 NYDZW2Q1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTBwMEK5Nlch|ryP NXnWNIJ3W0GQR1XS
Becker MmXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLnbY5KSzVyPUCuNFMxODNizszN NYrCSHQ{W0GQR1XS
MZ1-PC NXO2Z25KT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLaZm5KSzVyPUCuNFMyOTlizszN M1;GV3NCVkeHUh?=
ES6 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXfBV3IzUUN3ME2wMlA{OTl|IN88US=> NYD5ZnJCW0GQR1XS
KURAMOCHI M3q0OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDQXZU6UUN3ME2wMlA{PDh5IN88US=> NITWOZdUSU6JRWK=
CGTH-W-1 NVjhVVhpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\JPY5KSzVyPUCuNFM2PDhizszN Mnf5V2FPT0WU
VA-ES-BJ NVLXS3NRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXkd2lKSzVyPUCuNFM6ODJizszN NHPFcXpUSU6JRWK=
LXF-289 Mlv6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTCTWM2OD1yLkCzPVU3KM7:TR?= MVLTRW5ITVJ?
MPP-89 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TMOWlEPTB;MD6wOFA1QSEQvF2= M2TCUnNCVkeHUh?=
SW872 NIq4SYtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{WyR2lEPTB;MD6wOFE3OSEQvF2= MoPCV2FPT0WU
SNB75 M2D4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFnFVnZKSzVyPUCuNFQ1OzVizszN MmC3V2FPT0WU
PSN1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoG3TWM2OD1yLkC0OFc1KM7:TR?= NHyyRVdUSU6JRWK=
LB831-BLC NVvNfWhoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M33mUmlEPTB;MD6wOFYxQSEQvF2= NUXablBqW0GQR1XS
MFH-ino Moe1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TMXmlEPTB;MD6wOFczPCEQvF2= MWnTRW5ITVJ?
TGBC24TKB NGfQTHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnDTWM2OD1yLkC0O|YyKM7:TR?= MXnTRW5ITVJ?
A388 M{T0Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NETYepJKSzVyPUCuNFUxQTVizszN NYfRT4M2W0GQR1XS
BB30-HNC M2LOTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYC5cotjUUN3ME2wMlA2PDN5IN88US=> MmHMV2FPT0WU
GI-ME-N MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPOTWM2OD1yLkC2NVE5KM7:TR?= NYnvOnFUW0GQR1XS
TGBC1TKB NYn5WWh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fsV2lEPTB;MD6wOlE3PCEQvF2= NFr4bopUSU6JRWK=
TE-10 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkLUTWM2OD1yLkC2N|U4KM7:TR?= M{fpUXNCVkeHUh?=
A498 NGruWZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PyV2lEPTB;MD6wO|I5PCEQvF2= MUDTRW5ITVJ?
TE-11 MlrGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTBwMEe4OVgh|ryP MVvTRW5ITVJ?
BB65-RCC M4jlZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXoVoVWUUN3ME2wMlA5OjJ5IN88US=> M3fxNHNCVkeHUh?=
C2BBe1 NGPXfIxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnPITWM2OD1yLkC4N|A5KM7:TR?= MXTTRW5ITVJ?
NCI-H747 M{fmbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPlUYFiUUN3ME2wMlA5OzZ{IN88US=> MV7TRW5ITVJ?
IST-MES1 M3rOdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTBwMEi1OVIh|ryP NHrTWotUSU6JRWK=
KALS-1 NHq1S3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTJTWM2OD1yLkC5OFkh|ryP NIOxdYtUSU6JRWK=
GCIY MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTBwMEm2OVYh|ryP NVXoeI5tW0GQR1XS
RL95-2 M1nMXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXHJR|UxRTBwMUCzPEDPxE1? NFT2T3pUSU6JRWK=
TE-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1W3dGlEPTB;MD6xNFU1KM7:TR?= NUTNVWFsW0GQR1XS
NCI-H1355 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Xre2lEPTB;MD6xNVAzQCEQvF2= M37sZXNCVkeHUh?=
SW962 M3PaeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUjjfpNMUUN3ME2wMlEyOjl{IN88US=> M1XaTHNCVkeHUh?=
KLE NXu5UJZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYLJR|UxRTBwMUGzNVch|ryP NVHNT5o3W0GQR1XS
MC116 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2PFR2lEPTB;MD6xNVQyKM7:TR?= NVOzO|lzW0GQR1XS
NMC-G1 NFjMPJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTBwMUG2NFYh|ryP MojjV2FPT0WU
KU812 MmTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmP3TWM2OD1yLkGxPFg{KM7:TR?= NGjWR|hUSU6JRWK=
COLO-829 NVX1W2ZJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIqye2FKSzVyPUCuNVIzOTNizszN NIjZN29USU6JRWK=
NTERA-S-cl-D1 NXPveYRtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUPFdGl7UUN3ME2wMlEzOjh|IN88US=> MVHTRW5ITVJ?
IST-MEL1 NFT5bWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoC0TWM2OD1yLkGzOFUh|ryP NWfVdWdNW0GQR1XS
MLMA M3LIWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fmT2lEPTB;MD6xOFA{OiEQvF2= MlXlV2FPT0WU
LS-123 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnaXXo{UUN3ME2wMlE1ODZ2IN88US=> NFu5SWpUSU6JRWK=
LB2518-MEL NWnyNnZGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\4XIRKSzVyPUCuNVQyPjJizszN NYr4W2J6W0GQR1XS
NB69 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1L0SmlEPTB;MD6xOFQ{PiEQvF2= NVqxXm96W0GQR1XS
8-MG-BA MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF72N3FKSzVyPUCuNVU1PThizszN NEHXcZRUSU6JRWK=
K5 NVHkPGtPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DQ[GlEPTB;MD6xOlQ5QSEQvF2= M1fnRXNCVkeHUh?=
KINGS-1 NXuze29uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjVPHJKSzVyPUCuNVY3PjZizszN NGXPXnFUSU6JRWK=
SF268 NWnKZnRZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DJUmlEPTB;MD6xO|QxPCEQvF2= NWXJR4JkW0GQR1XS
PF-382 NF;SO3NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYPJR|UxRTBwMUe2O|gh|ryP MnjWV2FPT0WU
SH-4 NILQUHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWDJR|UxRTBwMUi0NVMh|ryP MVjTRW5ITVJ?
NALM-6 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTBwMUmyPVUh|ryP M3zte3NCVkeHUh?=
CP66-MEL MmrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlW4TWM2OD1yLkG5OVMyKM7:TR?= MV;TRW5ITVJ?
697 M4Hkd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nZc2lEPTB;MD6xPVk5PyEQvF2= M4nacnNCVkeHUh?=
CP67-MEL NX:5R4EzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTBwMkC0PFgh|ryP Mn7hV2FPT0WU
DSH1 MnjIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknMTWM2OD1yLkK0NFAyKM7:TR?= NI\xPZNUSU6JRWK=
HCE-4 NX7DRpZMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HCTWlEPTB;MD6yOlQ{QSEQvF2= NXXHNIxrW0GQR1XS
MZ2-MEL MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYP6NlhSUUN3ME2wMlI5PTN5IN88US=> NWf1bIlVW0GQR1XS
BL-41 NX[zb|FKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrxTWM2OD1yLkK5NVI{KM7:TR?= NU\4bFA4W0GQR1XS
HUTU-80 NEnQUGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTBwM{G0NkDPxE1? NHLEZllUSU6JRWK=
LOXIMVI M3fCcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTBwM{G1NFMh|ryP MWnTRW5ITVJ?
no-10 NHTxU4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX7JR|UxRTBwM{G5N|Eh|ryP M37vVnNCVkeHUh?=
KARPAS-422 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTBwM{O5PVch|ryP M3TPWnNCVkeHUh?=
SW684 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2P3PGlEPTB;MD6zOFk5KM7:TR?= MVnTRW5ITVJ?
SF126 M4L5bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTBwM{W0NUDPxE1? MlXNV2FPT0WU
D-263MG NGnYbWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfrVG9KSzVyPUCuN|YzOjRizszN MXzTRW5ITVJ?
OVCAR-4 M1XXe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVrrdJRpUUN3ME2wMlM4PDN|IN88US=> MWjTRW5ITVJ?
BB49-HNC NHrS[VdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTBwM{i1PVkh|ryP Mnv3V2FPT0WU
ONS-76 NGX3[XlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTBwNEK5OVEh|ryP NWnnSoI{W0GQR1XS
MZ7-mel M2PtWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX62d2huUUN3ME2wMlQ4QTFzIN88US=> NEPtOY5USU6JRWK=
RCC10RGB NFnSOIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3viS2lEPTB;MD60PVEyKM7:TR?= NH;kV3lUSU6JRWK=
BOKU M2fKVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGr2cYhKSzVyPUCuOFkyOzNizszN NGm4dY5USU6JRWK=
no-11 M{[0S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTBwNUCyNlgh|ryP MkPoV2FPT0WU
IST-SL2 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTBwNUCzNFIh|ryP MV3TRW5ITVJ?
RKO NW\1ephkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWnJR|UxRTBwNUK5OlYh|ryP MUHTRW5ITVJ?
HT-144 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTFSYNLUUN3ME2wMlU{PjB7IN88US=> NUfJdVlTW0GQR1XS
NCI-H446 NWjBe3BTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzHb2FqUUN3ME2wMlYzPzZizszN MV3TRW5ITVJ?
QIMR-WIL NGrYO5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXjJR|UxRTBwN{C2Nlkh|ryP M3i2T3NCVkeHUh?=
MHH-PREB-1 NHrTSHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3HTe2lEPTB;MD63OFQ3QSEQvF2= NIizO|JUSU6JRWK=
EW-16 NHewZ4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nXWmlEPTB;MD63OlE4QCEQvF2= Mn[1V2FPT0WU
EW-24 NIHSXm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn2yTWM2OD1yLke4NVY2KM7:TR?= MUXTRW5ITVJ?
LB373-MEL-D M4jxUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILlSYxKSzVyPUCuPFI2ODhizszN MXLTRW5ITVJ?
TE-9 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoLPTWM2OD1yLki3OVMzKM7:TR?= NHLrVodUSU6JRWK=
A3-KAW M2TXUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmWzTWM2OD1yLkm4OFUzKM7:TR?= MoDLV2FPT0WU
A101D M4HBcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmDSTWM2OD1zLkCzNFQ{KM7:TR?= MlXLV2FPT0WU
OCUB-M M{XlWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlS1TWM2OD1zLkC0OFEzKM7:TR?= NXXtU|dmW0GQR1XS
ES4 MnrNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnn4TWM2OD1zLkC1NVQ2KM7:TR?= NXHTRoZOW0GQR1XS
TE-6 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWHJR|UxRTFwMkGyNlYh|ryP NYXpTo5VW0GQR1XS
D-502MG NYjMN|JNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTFwMkOzO|Yh|ryP MWLTRW5ITVJ?
KNS-42 NUHiV4tHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHOWFJKSzVyPUGuNlQ1OTJizszN M1TmdnNCVkeHUh?=
SNU-C2B NWrOR2xVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrvTWM2OD1zLkOwOVg6KM7:TR?= MWXTRW5ITVJ?
NCI-H1838 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFTYXohKSzVyPUGuN|A4OzNizszN MYTTRW5ITVJ?
NKM-1 M1rxbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTFwM{C4OVkh|ryP M{T5XHNCVkeHUh?=
GI-1 NH7O[JpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnmxTWM2OD1zLkO2NlIh|ryP NGrtNHZUSU6JRWK=
NB5 MmrIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIm2cHFKSzVyPUGuN|k5OjdizszN NWK4RYhuW0GQR1XS
CAS-1 M2\meWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nZUmlEPTB;MT60NFk6OiEQvF2= MWDTRW5ITVJ?
HCE-T M4TDbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjCXZJsUUN3ME2xMlU3PzF2IN88US=> NUnXU45PW0GQR1XS
SBC-1 NHqycmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWO2Nog3UUN3ME2xMlU4QTh2IN88US=> MVHTRW5ITVJ?
JiyoyeP-2003 NG\YdnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTFwN{O0OlYh|ryP Mln2V2FPT0WU
TE-5 NIT1V2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfpTWM2OD1zLke5NVM6KM7:TR?= NIPycZRUSU6JRWK=
CAN Ml7CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3iyT2lEPTB;MT64NlI2OiEQvF2= M3nLS3NCVkeHUh?=
SK-UT-1 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTJwMU[2PVMh|ryP Mlj5V2FPT0WU
JVM-2 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnjfGZKSzVyPUKuN|YzQDRizszN Mo\XV2FPT0WU
LB771-HNC NIG5UodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rqdGlEPTB;Mj61O|U2OSEQvF2= NVHseVRIW0GQR1XS
NCCIT Ml3RS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moi1TWM2OD1{Lki2OlE3KM7:TR?= Mn\6V2FPT0WU
NCI-H2126 M1;BOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;3dIRKSzVyPUKuPFc2PTJizszN NFLpfFhUSU6JRWK=
Calu-6 Ml7oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXT1ZmJTUUN3ME2zMlA2PzRzIN88US=> M4DFWHNCVkeHUh?=
SK-LMS-1 MmixS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHOxVYxKSzVyPUOuNVE5QDZizszN NV3FU4dyW0GQR1XS
ARH-77 Ml7iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\OTWM2OD1|LkS2PVE2KM7:TR?= MVXTRW5ITVJ?
NB17 NXzl[2tKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTjTWM2OD1|Lk[zPFQ4KM7:TR?= MkHUV2FPT0WU
A253 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LQPGlEPTB;Mz63N|I1PiEQvF2= MUPTRW5ITVJ?
OPM-2 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3j5RWlEPTB;ND6yO|Y5PSEQvF2= MonnV2FPT0WU
MV-4-11 NF3Ld4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvFU|RMUUN3ME20MlM3PDV2IN88US=> M4jMWXNCVkeHUh?=
SR NGHoSZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fXbWlEPTB;ND60PVk2PCEQvF2= MmC2V2FPT0WU
KG-1 MmLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjFTWM2OD12Lk[wPFQ2KM7:TR?= M2fQOXNCVkeHUh?=
OCI-AML2 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLjNFkxUUN3ME21Mlg3OTV2IN88US=> NGnOe5dUSU6JRWK=
D-247MG M13iSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYjycoR3UUN3ME22MlEzPTF7IN88US=> M3y4enNCVkeHUh?=
DJM-1 NFO0cXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XoeWlEPTB;Nj60PFU2QCEQvF2= M{XnbXNCVkeHUh?=
RPMI-6666 M1;xdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTdwMkewOlch|ryP NVeyNZJSW0GQR1XS
KARPAS-45 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;QcWlEPTB;Nz61NVY4OSEQvF2= Mk\GV2FPT0WU
LP-1 NV3INVZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\lb4VtUUN3ME23MlU1Pzh{IN88US=> MkThV2FPT0WU
RS4-11 M1fyWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjEb49PUUN3ME23MlY2Pzh5IN88US=> NHr0OFNUSU6JRWK=
DU-4475 M{jH[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jPV2lEPTB;OD6yNVY2OiEQvF2= NV3afldzW0GQR1XS
MONO-MAC-6 Ml34S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjtR3pKSzVyPUiuNlcxPjZizszN MUPTRW5ITVJ?
NCI-SNU-16 M{HiVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRThwNU[xNlgh|ryP M{nacXNCVkeHUh?=
SJSA-1 NWj5fZlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRThwN{K4NFUh|ryP MXLTRW5ITVJ?
MMAC-SF NH7HZnRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRThwN{mzNFch|ryP MonzV2FPT0WU
SK-NEP-1 MorKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRThwOEmxOVUh|ryP NG\j[YJUSU6JRWK=
J-RT3-T3-5 NYXPfFU5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRThwOU[1Nlkh|ryP MVPTRW5ITVJ?
SKM-1 MorsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTlwMEG3N|Qh|ryP NV\HNGRNW0GQR1XS
LB2241-RCC NEPlc|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXP4T2ZFUUN3ME25MlAzODF{IN88US=> MX\TRW5ITVJ?
SIG-M5 NHeyPXpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGP4UZFKSzVyPUmuNFI1QTNizszN M3PlXHNCVkeHUh?=
EVSA-T M2KyeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXXS3lKSzVyPUmuNlc4QTNizszN M2LFN3NCVkeHUh?=
GT3TKB MmjMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3uzSGlEPTB;OT6zOVU1PiEQvF2= NXL3fYxRW0GQR1XS
NB6 NFnyPZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLyOYhKSzVyPUmuPVIzPTlizszN NXvyXJJ4W0GQR1XS
EHEB MkXWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTFyLkC2OVYh|ryP NEnBXYpUSU6JRWK=
HEL M1;Ve2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFO5bXJKSzVyPUGwMlQ4PzZizszN MnnzV2FPT0WU
ALL-PO NUjpXVNtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2n0NmlEPTB;MUCuO|k{QCEQvF2= MoXMV2FPT0WU
TGW MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1G4bWlEPTB;MUGuNlgzQCEQvF2= MULTRW5ITVJ?
BC-3 NF3iboNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXjTWM2OD1zMj6xNVM5KM7:TR?= M1;IfnNCVkeHUh?=
IA-LM MoPwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHHcXdKSzVyPUGyMlQ1PDVizszN M3;4fnNCVkeHUh?=
UACC-257 NV60PVBoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHoTWM2OD1zMj65NVk5KM7:TR?= NEDZUWpUSU6JRWK=
KP-N-YS MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLlfW1IUUN3ME2xNk46Ojh|IN88US=> MoPIV2FPT0WU
Raji M2na[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TETWlEPTB;MUOuO|Q6PyEQvF2= Ml3VV2FPT0WU
SF539 M{TZfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1zFXWlEPTB;MUOuPFU2PyEQvF2= NHz1R5RUSU6JRWK=
DMS-153 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1mxbWlEPTB;MUSuNFAzQCEQvF2= MoLiV2FPT0WU
L-540 NG\2WmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIfJUXZKSzVyPUG1MlA3PzJizszN M4TQfHNCVkeHUh?=
MN-60 Mmi2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkS3TWM2OD1zNT6xPVc6KM7:TR?= NYDmZmQ3W0GQR1XS
RPMI-8866 M{D5XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIHzZY9KSzVyPUG3MlQ1PTRizszN M{OzUHNCVkeHUh?=
NCI-H510A Mn7WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3PVOmlEPTB;MUmuN|k4OyEQvF2= NYj3R2RjW0GQR1XS
NB13 NEHtUpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLWSG1KSzVyPUG5MlQ5PzdizszN NF7ROJhUSU6JRWK=
HAL-01 MlG1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknBTWM2OD1zOT63OVQ{KM7:TR?= NFHr[YxUSU6JRWK=
NCI-H720 MlmwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rjXWlEPTB;MkCuNlc{OyEQvF2= NIrxXVZUSU6JRWK=
REH MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXGTWM2OD1{MD62N|U4KM7:TR?= NIH1[VRUSU6JRWK=
KNS-81-FD NH3KeZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV3JR|UxRTJ|LkG0OkDPxE1? NX\DT5puW0GQR1XS
HC-1 NFPac5VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1zJdmlEPTB;MkSuOVU2OSEQvF2= NGLkPItUSU6JRWK=
NCI-H2141 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXrlSHlYUUN3ME2yOE44PzV2IN88US=> NIrlTGJUSU6JRWK=
MOLT-4 MmnLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXv6O|dIUUN3ME2yOk43PzV|IN88US=> NWToSFJvW0GQR1XS
OMC-1 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV\JR|UxRTJ5LkG0NlIh|ryP M3jzZnNCVkeHUh?=
LC-1F M3fyXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTJ5LkOyOFUh|ryP NEn4TllUSU6JRWK=
NCI-H1304 NXvH[4YzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nudmlEPTB;MkiuNVYzQCEQvF2= M3PGW3NCVkeHUh?=
BC-1 MmH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH\kR4ZKSzVyPUK4MlY2OSEQvF2= NFXoe4RUSU6JRWK=
NCI-H64 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3XfnJxUUN3ME2yPU43OjV|IN88US=> M{fCNnNCVkeHUh?=
MOLT-16 M{jFNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTJ7Lk[yPVIh|ryP NGThWoxUSU6JRWK=
U-87-MG M{P3NGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TQSWlEPTB;M{CuO|Y3KM7:TR?= M1\aXnNCVkeHUh?=
GAK MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTNzLkK2PFYh|ryP NG\mOZdUSU6JRWK=
ES8 NGTXOo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDS[3l[UUN3ME2zNk4yOjV{IN88US=> M1TZ[XNCVkeHUh?=
HCC1599 M3fGemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTN{LkOzNlUh|ryP NUG1b4FUW0GQR1XS
EB-3 M{Lwbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTN2LkOxNVch|ryP NEG0[mZUSU6JRWK=
HCC1187 NXHqPFdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUnOdGFqUUN3ME2zOU45ODV{IN88US=> Mmj4V2FPT0WU
SK-PN-DW NIDWb3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTN4LkG5OFMh|ryP M3S4SXNCVkeHUh?=
JVM-3 M2HVWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPxdo5KSzVyPUO3MlI{OzhizszN NELs[mlUSU6JRWK=
HCC2157 MmK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTN5Lkm5OFYh|ryP M2TzVXNCVkeHUh?=
A4-Fuk NYTFfFBET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPxTZdnUUN3ME2zPE4yODB7IN88US=> MWPTRW5ITVJ?
COR-L279 NHiw[4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTRyLkK4OVEh|ryP M4Dub3NCVkeHUh?=
DEL MlO0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\sdodKSzVyPUSxMlkxQDZizszN MVnTRW5ITVJ?
NCI-H1395 NV3jS2t2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI[zeZpKSzVyPUSyMlAyPjNizszN NFv2e2dUSU6JRWK=
MHH-NB-11 MoHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7LTWM2OD12Mz6wPFE5KM7:TR?= MlfJV2FPT0WU
NCI-H2107 M1nGd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHuZ5hKSzVyPUSzMlQ5PDZizszN M2WzTHNCVkeHUh?=
NEC8 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfqSndXUUN3ME20OE4{OzZizszN NEXBXJVUSU6JRWK=
COLO-684 M1LFfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYTjSFhWUUN3ME20Ok4zOjV6IN88US=> Ml3OV2FPT0WU
LS-411N MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;qeWlEPTB;NEiuOFc1QCEQvF2= NVvCR2J[W0GQR1XS

... 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 1% DMSO/30% PEG 300/1% Tween 80 30 mg/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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