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 Ml7ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonzO|IhcA>? MXLEUXNQ NVXQUpNHUUN3ME2wMlAxOSEQvF2= M{Cwd|E4QTV4MEiw
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ALL3 MnTQR5l1d3SxeHnjJGF{e2G7 M13ZO|AvOc7:TR?= NIS2[nc4OiCq NHLqdGZFVVOR MX3JR|UxRTBwMECwOEDPxE1? NFu2SosyQTh6OUW0NC=>
CML MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnCNlAhdWmw MUTEUXNQ NXrzWXBUUUN3ME2wMlAxOSEQvF2= MWKxPVIyQTBzNh?=
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BA/F3 NUDmRYNuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY[3NkBp NVvEcYh[TE2VTx?= MkfvTY5lfWOnczDjfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCRU9HOyClZXzsd{BmgHC{ZYPzbY5oKEKFUj3BRmwhTjR6NmOgcZV1[W62IHHzd4V{e2WmIHHzJIdzd3e2aDDJcohq[mm2aX;uJJdqfGhiSVO1NEBw\iByLkCwNFnPxE1? MWGyN|MxOTdyMx?=
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BA/F3 M2HkW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfESI44OiCq Mn3ySG1UVw>? MmHITY5lfWOnczDjfZRwfG:6aXPpeJkh[WejaX7zeEBud3W|ZTDCRU9HOyClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghUW6qaXLpeIlwdiC5aYToJGlEPTBib3[gNk42|ryP NF\6Z2MzOzNyMUewNy=>
T cell M1HJ[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoOxO|IhcA>? MW\EUXNQ NGfGNFVKdmirYnn0d{BidnSrIFPEN{0h[W6mIHHueIkhS0R{OD3pcoR2[2WmIGSgZ4VtdCCycn;sbYZmemG2aX;uJJdqfGhiSVO1NEBw\iByLkCwN:69VQ>? NVrmeopPOTdzNUS1NVI>
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MALME-3M MUHDfZRwfG:6aXOgRZN{[Xl? NE\BV4Y4OiCq MX;EUXNQ MojYS2k2OD14Lk[xJO69VQ>? MXKyOFAyPTN{Nx?=
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NCI-H460 NGj4TlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3fnbFczKGh? NHfq[WlFVVOR M3PzXGlEPTB;OD65PUDPxE1? MmH3NlM2OjFyMkC=
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NCI-H661 NXvpT3lZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnT0O|IhcA>? NGf1eWNFVVOR NVHmXJhXUUN3ME23Mlgh|ryP MYOyN|U3Pzl4MB?=
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U937 M{PubGZ2dmO2aX;uJGF{e2G7 MYOxJO69VQ>? M3XFVlEhcA>? NYLsXIJLTE2VTx?= Mnu5VoVlfWOnczDMVHMucW6mdXPl[EBVVk[jbIDoZUBz\WynYYPlJIlvKGi3bXHuJHU6OzdiY3XscJM> Ml3LNVc3QDRyOUm=
murine mast cell NInh[pBHfW6ldHnvckBCe3OjeR?= M1jtTFEh|ryP NEfIfmIzPCCq MlXuSG1UVw>? NFrvSYtKdmirYnn0d{BidnSrZ3XuMYlv\HWlZXSgTWw3KHOnY4LleIlwdiCrbjDJ[2UheHKrbXXkJI1wfXOnIH3hd5Qh[2WubIOgZZQhOSC3TR?= MWmxO|Y5PDB7OR?=
BV-173 NH\OPHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLpR2lKSzVyPUCuNFAxODByMUC5JO69VQ>? NELuepZUSU6JRWK=
K-562 MoPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmK2TWM2OD1yLkCwNFAxODJ4NjFOwG0> MlTKV2FPT0WU
BL-70 NU\RbYllT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLKO3RKSzVyPUCuNFAxODByOEKyJO69VQ>? Mn7TV2FPT0WU
EM-2 Mo\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{TCfWlEPTB;MD6wNFAxODFyODFOwG0> MXTTRW5ITVJ?
LAMA-84 MlfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3zoNWlEPTB;MD6wNFAxODN{MTFOwG0> NF3MT5BUSU6JRWK=
MEG-01 M4jZSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTBwMECwNFA6QCEQvF2= M1PGc3NCVkeHUh?=
EoL-1-cell M1n0XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDmTWpPUUN3ME2wMlAxODBzM{Gg{txO MWXTRW5ITVJ?
CTV-1 M3rQeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{L6e2lEPTB;MD6wNFAxPDB2IN88US=> M4O5WHNCVkeHUh?=
TE-15 MnPuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTBwMEC1PFkh|ryP NFvBWFNUSU6JRWK=
NOS-1 Ml7WS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M323NWlEPTB;MD6wNFYyOyEQvF2= NVv6e|BxW0GQR1XS
D-336MG NYPHOXo1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlToTWM2OD1yLkCwOlMh|ryP MWnTRW5ITVJ?
LB1047-RCC MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGG4b4NKSzVyPUCuNFA6QDlizszN NHroXGtUSU6JRWK=
LB996-RCC NGr0NW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml3VTWM2OD1yLkCwPVkyKM7:TR?= MlroV2FPT0WU
SW982 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4nJbWlEPTB;MD6wNVEyPSEQvF2= MVfTRW5ITVJ?
TK10 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUHJR|UxRTBwMEGxO|Qh|ryP NYXqOm9WW0GQR1XS
A704 NUDCTodNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTBwMEG0PVEh|ryP NEK3NJhUSU6JRWK=
TE-8 NFzVb4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml64TWM2OD1yLkCxOVc3KM7:TR?= MVjTRW5ITVJ?
DOHH-2 M4rxRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPjWXdFUUN3ME2wMlAyPzF7IN88US=> MnfnV2FPT0WU
HOP-62 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTBwMEG4N|Qh|ryP MknQV2FPT0WU
TE-12 M1OwWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1L2XWlEPTB;MD6wNVg3OSEQvF2= MmHFV2FPT0WU
KGN Mn24S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1y0eWlEPTB;MD6wNVk1OiEQvF2= NHrEem1USU6JRWK=
NCI-H1648 NHLYPHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX7IOphuUUN3ME2wMlAzODFzIN88US=> NH7hZWlUSU6JRWK=
OS-RC-2 NUe3[IN2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDCTWM2OD1yLkCyNFMh|ryP NWS1c4FNW0GQR1XS
GB-1 NIm4RlRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\MZ25KSzVyPUCuNFIyPTdizszN NWn0VZNUW0GQR1XS
RXF393 MnroS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nNc2lEPTB;MD6wNlM2PyEQvF2= NVHtRYxUW0GQR1XS
LC-2-ad Mn3rS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIjQcGVKSzVyPUCuNFI2QDZizszN NFHQVohUSU6JRWK=
KS-1 M3jMb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXi3boJ1UUN3ME2wMlAzPzNizszN NFLyOXdUSU6JRWK=
ETK-1 NYDQSXlxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDydWlKSzVyPUCuNFI5OzJizszN M3j6UXNCVkeHUh?=
SW954 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\wXWFzUUN3ME2wMlAzQTJ5IN88US=> M4ntU3NCVkeHUh?=
Becker M1:1OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGTsbHRKSzVyPUCuNFMxODNizszN M4fXcHNCVkeHUh?=
MZ1-PC MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofQTWM2OD1yLkCzNVE6KM7:TR?= NWrr[GF5W0GQR1XS
ES6 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnnO|dKUUN3ME2wMlA{OTl|IN88US=> M{[2T3NCVkeHUh?=
KURAMOCHI M4Gyd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELocYtKSzVyPUCuNFM1QDdizszN NU\LWWFuW0GQR1XS
CGTH-W-1 NVzKUJozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3EempKSzVyPUCuNFM2PDhizszN NFTrTmRUSU6JRWK=
VA-ES-BJ NF\TWHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUOxPFNTUUN3ME2wMlA{QTB{IN88US=> MXfTRW5ITVJ?
LXF-289 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlntTWM2OD1yLkCzPVU3KM7:TR?= M2S3THNCVkeHUh?=
MPP-89 M2\iVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTBwMESwOFkh|ryP MVTTRW5ITVJ?
SW872 M4rwcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVXqc2pDUUN3ME2wMlA1OTZzIN88US=> NVf5doNQW0GQR1XS
SNB75 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfaTWM2OD1yLkC0OFM2KM7:TR?= MXLTRW5ITVJ?
PSN1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHDdYtKSzVyPUCuNFQ1PzRizszN MV3TRW5ITVJ?
LB831-BLC NYfpSJR7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTBwMES2NFkh|ryP MXjTRW5ITVJ?
MFH-ino NWH1VohlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYDR[nFOUUN3ME2wMlA1PzJ2IN88US=> MYrTRW5ITVJ?
TGBC24TKB M4X1c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4e5UGlEPTB;MD6wOFc3OSEQvF2= MWrTRW5ITVJ?
A388 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DXWmlEPTB;MD6wOVA6PSEQvF2= NYDrSmdiW0GQR1XS
BB30-HNC NIHxUWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4[wbWlEPTB;MD6wOVQ{PyEQvF2= NFzx[25USU6JRWK=
GI-ME-N NFHk[FRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPLTWM2OD1yLkC2NVE5KM7:TR?= MWnTRW5ITVJ?
TGBC1TKB MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4W2Z2lEPTB;MD6wOlE3PCEQvF2= NHHWe2VUSU6JRWK=
TE-10 M{PkVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmGwTWM2OD1yLkC2N|U4KM7:TR?= NFHhNpZUSU6JRWK=
A498 Mnm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWXre4s4UUN3ME2wMlA4Ojh2IN88US=> MUXTRW5ITVJ?
TE-11 NFvod3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1:3[2lEPTB;MD6wO|g2QCEQvF2= NXPoZYF3W0GQR1XS
BB65-RCC NUL0XI82T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGL0WmtKSzVyPUCuNFgzOjdizszN M{PmT3NCVkeHUh?=
C2BBe1 NILzV2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTBwMEizNFgh|ryP MlzEV2FPT0WU
NCI-H747 NV3hd|dwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTBwMEizOlIh|ryP MWXTRW5ITVJ?
IST-MES1 Mk\KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYHsWJVWUUN3ME2wMlA5PTV{IN88US=> M2HMW3NCVkeHUh?=
KALS-1 NWrZfnY2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\KTWM2OD1yLkC5OFkh|ryP MVrTRW5ITVJ?
GCIY MnrDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTBwMEm2OVYh|ryP MXXTRW5ITVJ?
RL95-2 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvkUnFJUUN3ME2wMlExOzhizszN NX;VSWE3W0GQR1XS
TE-1 NWX1OY8xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEW4ZpVKSzVyPUCuNVA2PCEQvF2= M{\JfnNCVkeHUh?=
NCI-H1355 NYrDb4plT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTBwMUGwNlgh|ryP NF;IeG9USU6JRWK=
SW962 Mn:1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jESmlEPTB;MD6xNVI6OiEQvF2= M3TCSXNCVkeHUh?=
KLE M1vrZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2D0[WlEPTB;MD6xNVMyPyEQvF2= M2DBZnNCVkeHUh?=
MC116 MnL6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2m1bmlEPTB;MD6xNVQyKM7:TR?= M4HqVXNCVkeHUh?=
NMC-G1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDLcVE6UUN3ME2wMlEyPjB4IN88US=> M4K2bHNCVkeHUh?=
KU812 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYH0VnQ1UUN3ME2wMlEyQDh|IN88US=> M1jqZXNCVkeHUh?=
COLO-829 NHXHSYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkL5TWM2OD1yLkGyNlE{KM7:TR?= NHnCcnFUSU6JRWK=
NTERA-S-cl-D1 NYCyUIc4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHXOG9KSzVyPUCuNVIzQDNizszN NWTwOodyW0GQR1XS
IST-MEL1 NUf3OI1nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1f2[GlEPTB;MD6xN|Q2KM7:TR?= NH;Zc2dUSU6JRWK=
MLMA MmXJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTBwMUSwN|Ih|ryP MWLTRW5ITVJ?
LS-123 NUXCV5h[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3n6RmlEPTB;MD6xOFA3PCEQvF2= NIX5c4pUSU6JRWK=
LB2518-MEL NXTWcFNJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7BTWM2OD1yLkG0NVYzKM7:TR?= MnyzV2FPT0WU
NB69 NHz1bJVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrRTWM2OD1yLkG0OFM3KM7:TR?= NVrhd|NNW0GQR1XS
8-MG-BA NVHFOoZCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTBwMUW0OVgh|ryP NVjQ[WpFW0GQR1XS
K5 NGDFTnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\PNY5bUUN3ME2wMlE3PDh7IN88US=> MoTUV2FPT0WU
KINGS-1 NHv6[pFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\MTWM2OD1yLkG2OlY3KM7:TR?= MlixV2FPT0WU
SF268 NICyOo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2HJe2lEPTB;MD6xO|QxPCEQvF2= MV3TRW5ITVJ?
PF-382 NUDtOXZLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUD4XoN5UUN3ME2wMlE4Pjd6IN88US=> NFXySVhUSU6JRWK=
SH-4 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrLdG91UUN3ME2wMlE5PDF|IN88US=> NUWzOmxqW0GQR1XS
NALM-6 NHnXSFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzQTWM2OD1yLkG5Nlk2KM7:TR?= MWHTRW5ITVJ?
CP66-MEL NGLRR4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTaSGlDUUN3ME2wMlE6PTNzIN88US=> NVf0[oFtW0GQR1XS
697 MmTiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzqTlJKSzVyPUCuNVk6QDdizszN MXrTRW5ITVJ?
CP67-MEL NFHWc|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV2we2s5UUN3ME2wMlIxPDh6IN88US=> NX:3RVhkW0GQR1XS
DSH1 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXnOPGpqUUN3ME2wMlI1ODBzIN88US=> NW[zSXNQW0GQR1XS
HCE-4 NWfNdJdmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnW5TWM2OD1yLkK2OFM6KM7:TR?= M1HmdHNCVkeHUh?=
MZ2-MEL M4PrT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTBwMki1N|ch|ryP NUG3TmUzW0GQR1XS
BL-41 NVvPPYZ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV\JR|UxRTBwMkmxNlMh|ryP Mn:wV2FPT0WU
HUTU-80 NX:wbW1UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfRdpFKSzVyPUCuN|E1OiEQvF2= NWqwTYhnW0GQR1XS
LOXIMVI MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXS3UZBKUUN3ME2wMlMyPTB|IN88US=> MXfTRW5ITVJ?
no-10 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVnJR|UxRTBwM{G5N|Eh|ryP M2\3c3NCVkeHUh?=
KARPAS-422 M2T4Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MU\JR|UxRTBwM{O5PVch|ryP MULTRW5ITVJ?
SW684 NI\helNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXHPFBKSzVyPUCuN|Q6QCEQvF2= NX63OZJuW0GQR1XS
SF126 NFS1SVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTBwM{W0NUDPxE1? MXPTRW5ITVJ?
D-263MG M1;BbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HURWlEPTB;MD6zOlIzPCEQvF2= NYnCS3lEW0GQR1XS
OVCAR-4 M4HCdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MojwTWM2OD1yLkO3OFM{KM7:TR?= NXzSfYlYW0GQR1XS
BB49-HNC MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NImxZZFKSzVyPUCuN|g2QTlizszN M4T2bXNCVkeHUh?=
ONS-76 M2f2Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVXJR|UxRTBwNEK5OVEh|ryP M2XxdHNCVkeHUh?=
MZ7-mel NEXJVm1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmfCTWM2OD1yLkS3PVEyKM7:TR?= M17xRXNCVkeHUh?=
RCC10RGB NVLxWFByT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DhVWlEPTB;MD60PVEyKM7:TR?= NHPJdnhUSU6JRWK=
BOKU Mm\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTFTWM2OD1yLkS5NVM{KM7:TR?= NFT2XGJUSU6JRWK=
no-11 MnnnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETmdnFKSzVyPUCuOVAzOjhizszN NUDIcnI1W0GQR1XS
IST-SL2 M4DWcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonFTWM2OD1yLkWwN|AzKM7:TR?= NX[yWXBnW0GQR1XS
RKO NFzhT2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXldJRKSzVyPUCuOVI6PjZizszN Mo\rV2FPT0WU
HT-144 NHf5ZmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1q2UWlEPTB;MD61N|YxQSEQvF2= MkLLV2FPT0WU
NCI-H446 M4OyU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTBwNkK3OkDPxE1? NUj1Wm81W0GQR1XS
QIMR-WIL NF3uTFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTQWHJoUUN3ME2wMlcxPjJ7IN88US=> MorzV2FPT0WU
MHH-PREB-1 M3\6Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPaTWM2OD1yLke0OFY6KM7:TR?= MXXTRW5ITVJ?
EW-16 MlPlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37remlEPTB;MD63OlE4QCEQvF2= MmrBV2FPT0WU
EW-24 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTNTWM2OD1yLke4NVY2KM7:TR?= MWDTRW5ITVJ?
LB373-MEL-D NVTPZWltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjoTWM2OD1yLkiyOVA5KM7:TR?= Ml\MV2FPT0WU
TE-9 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlvlTWM2OD1yLki3OVMzKM7:TR?= MV;TRW5ITVJ?
A3-KAW NUnKOmI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HnfGlEPTB;MD65PFQ2OiEQvF2= NFHYT3VUSU6JRWK=
A101D MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mof1TWM2OD1zLkCzNFQ{KM7:TR?= MX\TRW5ITVJ?
OCUB-M MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHrbmROUUN3ME2xMlA1PDF{IN88US=> MoTTV2FPT0WU
ES4 M3PCVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfnfGFKSzVyPUGuNFUyPDVizszN MnTOV2FPT0WU
TE-6 M4\VfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1[1fWlEPTB;MT6yNVIzPiEQvF2= M{TDdnNCVkeHUh?=
D-502MG NUKyS|h1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTuXYozUUN3ME2xMlI{Ozd4IN88US=> NXLvO3lnW0GQR1XS
KNS-42 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTFwMkS0NVIh|ryP NGTtTZdUSU6JRWK=
SNU-C2B MmHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTFwM{C1PFkh|ryP MVzTRW5ITVJ?
NCI-H1838 MmP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTFwM{C3N|Mh|ryP NXftS3g3W0GQR1XS
NKM-1 NFTvSYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTFwM{C4OVkh|ryP NFvY[HVUSU6JRWK=
GI-1 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;TWGlEPTB;MT6zOlIzKM7:TR?= MUfTRW5ITVJ?
NB5 NF;IOIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nRSWlEPTB;MT6zPVgzPyEQvF2= M1j1OXNCVkeHUh?=
CAS-1 M3P1eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\BTZdOUUN3ME2xMlQxQTl{IN88US=> MUHTRW5ITVJ?
HCE-T NYXWeYFQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTFwNU[3NVQh|ryP M2H1OnNCVkeHUh?=
SBC-1 NXTNfmxuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnvkTWM2OD1zLkW3PVg1KM7:TR?= NF[ycWhUSU6JRWK=
JiyoyeP-2003 NWrnWY9GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmL2TWM2OD1zLkezOFY3KM7:TR?= M3XGNnNCVkeHUh?=
TE-5 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTFwN{mxN|kh|ryP NWjnT49SW0GQR1XS
CAN MnntS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTFwOEKyOVIh|ryP NYLPWI5qW0GQR1XS
SK-UT-1 NFP1[|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTJwMU[2PVMh|ryP M323TnNCVkeHUh?=
JVM-2 NVzoZW1yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{\jTmlEPTB;Mj6zOlI5PCEQvF2= MUPTRW5ITVJ?
LB771-HNC MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnTSTWM2OD1{LkW3OVUyKM7:TR?= Mkf2V2FPT0WU
NCCIT NXO2bHNjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTJwOE[2NVYh|ryP MnvTV2FPT0WU
NCI-H2126 NFTESZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLMbWp4UUN3ME2yMlg4PTV{IN88US=> M4nMfnNCVkeHUh?=
Calu-6 NYjOU4hPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXFOm5xUUN3ME2zMlA2PzRzIN88US=> M2S2T3NCVkeHUh?=
SK-LMS-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnv5TWM2OD1|LkGxPFg3KM7:TR?= MorFV2FPT0WU
ARH-77 M1fnOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTNwNE[5NVUh|ryP Mo\GV2FPT0WU
NB17 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXP0UGJjUUN3ME2zMlY{QDR5IN88US=> MV3TRW5ITVJ?
A253 M2DnbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3PyOGlEPTB;Mz63N|I1PiEQvF2= NX7scZdbW0GQR1XS
OPM-2 MmPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXBTWM2OD12LkK3Olg2KM7:TR?= M1\QTnNCVkeHUh?=
MV-4-11 NUCy[llVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3TTWM2OD12LkO2OFU1KM7:TR?= M4P4VXNCVkeHUh?=
SR NIPhPY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3CdIxKSzVyPUSuOFk6PTRizszN NYjnbnpCW0GQR1XS
KG-1 Ml7iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrrTWM2OD12Lk[wPFQ2KM7:TR?= MUnTRW5ITVJ?
OCI-AML2 NH3IW2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF3VfpFKSzVyPUWuPFYyPTRizszN M1iwXHNCVkeHUh?=
D-247MG NEX3SYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTZwMUK1NVkh|ryP M33ZbHNCVkeHUh?=
DJM-1 M4TDbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXTJR|UxRTZwNEi1OVgh|ryP M4O2RnNCVkeHUh?=
RPMI-6666 NYjJeI1kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTdwMkewOlch|ryP MoCyV2FPT0WU
KARPAS-45 NUHofld[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13KOmlEPTB;Nz61NVY4OSEQvF2= M{OzU3NCVkeHUh?=
LP-1 NFLMfmZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTvOopMUUN3ME23MlU1Pzh{IN88US=> NWnYd4M{W0GQR1XS
RS4-11 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\QVYd[UUN3ME23MlY2Pzh5IN88US=> NI\GdWtUSU6JRWK=
DU-4475 MoLaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH76XoxKSzVyPUiuNlE3PTJizszN NHTyb2ZUSU6JRWK=
MONO-MAC-6 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRThwMkewOlYh|ryP M3;hbnNCVkeHUh?=
NCI-SNU-16 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljrTWM2OD16LkW2NVI5KM7:TR?= NGHsfFJUSU6JRWK=
SJSA-1 M3ztcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mne2TWM2OD16LkeyPFA2KM7:TR?= MYDTRW5ITVJ?
MMAC-SF NFe0fpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLqflV1UUN3ME24Mlc6OzB5IN88US=> MWXTRW5ITVJ?
SK-NEP-1 M4TW[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\aU|RNUUN3ME24Mlg6OTV3IN88US=> M{H0dXNCVkeHUh?=
J-RT3-T3-5 MnLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPjbG9KSzVyPUiuPVY2OjlizszN NGXtVlNUSU6JRWK=
SKM-1 MojtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTlwMEG3N|Qh|ryP MlHWV2FPT0WU
LB2241-RCC M3iy[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH3rb2xKSzVyPUmuNFIxOTJizszN MUHTRW5ITVJ?
SIG-M5 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnKTWM2OD17LkCyOFk{KM7:TR?= NYDjXmF{W0GQR1XS
EVSA-T MmjGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkjWTWM2OD17LkK3O|k{KM7:TR?= NF\MU4lUSU6JRWK=
GT3TKB NITvfo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTlwM{W1OFYh|ryP NFfnfXJUSU6JRWK=
NB6 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGrtclBKSzVyPUmuPVIzPTlizszN MV;TRW5ITVJ?
EHEB MkHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkXPTWM2OD1zMD6wOlU3KM7:TR?= MXTTRW5ITVJ?
HEL M4nyWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTFyLkS3O|Yh|ryP MVrTRW5ITVJ?
ALL-PO NGm1Sm9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfITWM2OD1zMD63PVM5KM7:TR?= M4qwPHNCVkeHUh?=
TGW M1TLemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXPd|BKSzVyPUGxMlI5OjhizszN NXK0UJRiW0GQR1XS
BC-3 NHjPTJJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HKUGlEPTB;MUKuNVE{QCEQvF2= MojZV2FPT0WU
IA-LM MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2D3e2lEPTB;MUKuOFQ1PSEQvF2= NWrvTI1KW0GQR1XS
UACC-257 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1HhTGlEPTB;MUKuPVE6QCEQvF2= MofmV2FPT0WU
KP-N-YS NWrVfldqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zobmlEPTB;MUKuPVI5OyEQvF2= MXfTRW5ITVJ?
Raji MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1H3cmlEPTB;MUOuO|Q6PyEQvF2= NGPlNWhUSU6JRWK=
SF539 NGji[XpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTF|Lki1OVch|ryP MV\TRW5ITVJ?
DMS-153 Mn:1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWmyTWVvUUN3ME2xOE4xODJ6IN88US=> NUTae2FbW0GQR1XS
L-540 NInwdJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWfJR|UxRTF3LkC2O|Ih|ryP MliyV2FPT0WU
MN-60 MojIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTF3LkG5O|kh|ryP NHfON2NUSU6JRWK=
RPMI-8866 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTF5LkS0OVQh|ryP MkLpV2FPT0WU
NCI-H510A MnTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWXJR|UxRTF7LkO5O|Mh|ryP MontV2FPT0WU
NB13 NGH5TWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTF7LkS4O|ch|ryP NF\XSVJUSU6JRWK=
HAL-01 M2WxTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;IZ4JKSzVyPUG5Mlc2PDNizszN M331enNCVkeHUh?=
NCI-H720 M1TmRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTJyLkK3N|Mh|ryP NF;mcpFUSU6JRWK=
REH NUjvU5JDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13kU2lEPTB;MkCuOlM2PyEQvF2= NXHB[Wc3W0GQR1XS
KNS-81-FD NW\6NldET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrDTWM2OD1{Mz6xOFYh|ryP NFrwOWhUSU6JRWK=
HC-1 NUHWSZpnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXIPVBKSzVyPUK0MlU2PTFizszN M1TWXnNCVkeHUh?=
NCI-H2141 M3TRZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYXJR|UxRTJ2Lke3OVQh|ryP NXPnbpZXW0GQR1XS
MOLT-4 M2PUXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTJ4Lk[3OVMh|ryP M2LSfnNCVkeHUh?=
OMC-1 M1f0V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[yXpdKSzVyPUK3MlE1OjJizszN NYPYelNCW0GQR1XS
LC-1F Ml;tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTJ5LkOyOFUh|ryP NVj5NXhjW0GQR1XS
NCI-H1304 M3m0e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTJ6LkG2Nlgh|ryP M4HRfHNCVkeHUh?=
BC-1 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfUUnNQUUN3ME2yPE43PTFizszN MXLTRW5ITVJ?
NCI-H64 M1q1V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLINohCUUN3ME2yPU43OjV|IN88US=> NHzRVnVUSU6JRWK=
MOLT-16 Mn\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUfKb2Z2UUN3ME2yPU43Ojl{IN88US=> NEfRTYNUSU6JRWK=
U-87-MG MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfrTWM2OD1|MD63OlYh|ryP NFXkZ3FUSU6JRWK=
GAK M4iyW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkG0TWM2OD1|MT6yOlg3KM7:TR?= M37WOHNCVkeHUh?=
ES8 NWXkWodmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3GUW1KSzVyPUOyMlEzPTJizszN MmTxV2FPT0WU
HCC1599 M3P1V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmSwTWM2OD1|Mj6zN|I2KM7:TR?= NWfESoloW0GQR1XS
EB-3 M1y3fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTN2LkOxNVch|ryP M{S5bnNCVkeHUh?=
HCC1187 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUe3NGlEUUN3ME2zOU45ODV{IN88US=> MVzTRW5ITVJ?
SK-PN-DW MlzjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIL2UXJKSzVyPUO2MlE6PDNizszN NWrQW4tLW0GQR1XS
JVM-3 NF3aWXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3J[ppGUUN3ME2zO{4zOzN6IN88US=> MX\TRW5ITVJ?
HCC2157 NF\oPJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTN5Lkm5OFYh|ryP MknQV2FPT0WU
A4-Fuk NVTV[WpMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHn1SoNKSzVyPUO4MlExODlizszN NWnaWWlNW0GQR1XS
COR-L279 NY\qenJHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1P4UGlEPTB;NECuNlg2OSEQvF2= MnPrV2FPT0WU
DEL NISwWGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTRzLkmwPFYh|ryP NUfBRoNyW0GQR1XS
NCI-H1395 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjw[Y9KSzVyPUSyMlAyPjNizszN M33yTnNCVkeHUh?=
MHH-NB-11 M1i1Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXzJR|UxRTR|LkC4NVgh|ryP NHXOOWNUSU6JRWK=
NCI-H2107 NF;BUXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVj6b3FzUUN3ME20N{41QDR4IN88US=> M3XyUXNCVkeHUh?=
NEC8 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\OS4ZbUUN3ME20OE4{OzZizszN M4XrdXNCVkeHUh?=
COLO-684 M3P6Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYezdJc5UUN3ME20Ok4zOjV6IN88US=> M3THfHNCVkeHUh?=
LS-411N M1fYXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3UTWM2OD12OD60O|Q5KM7:TR?= MX\TRW5ITVJ?

... 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)


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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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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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