Dasatinib 化学構造
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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は一種の新たで、有効な多ターゲット阻害剤で、無細胞試験でAbl、Srcとc-Kitに作用する時のIC50値が1 nM以下、0.8 nMと79 nMにそれぞれ分かれることです。
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
M07ep210 MnXtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEn1dWE4OiCq NF;4VXZFVVOR MXfJR|UxRTBwMECwNFch|ryP MXqxO|k2PjB6MB?=
K562 NEnIU4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTSTJA4OiCq MYHEUXNQ MUjJR|UxRTBwMECxJO69VQ>? MWWxO|k2PjB6MB?=
M07e MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIj0O3o4OiCq M1nXUGROW09? MX\JR|UxRTBwMECxNkDPxE1? M1;jU|E4QTV4MEiw
ALL3 NGDhWlZEgXSxdH;4bYMhSXO|YYm= MX:wMlHPxE1? MVu3NkBp MmDXSG1UVw>? MVHJR|UxRTBwMECwOEDPxE1? MUCxPVg5QTV2MB?=
CML MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPxNlAhdWmw NI[5cHBFVVOR NX;GeHl[UUN3ME2wMlAxOSEQvF2= Mm\6NVkzOTlyMU[=
BA/F3 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MliwO|IhcA>? NHizdHJFVVOR Ml;XTWM2OD14LkW4PUDPxE1? NFvObHEzOzB6OE[0OC=>
BA/F3 MlPmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1T5b|czKGh? M4LhUWROW09? MmrvTY5lfWOnczDhcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IH3veZNmKEKDL1[zJINmdGy|IHX4dJJme3OrbnegRoNzNUGkbDDNN|UyXCCvdYThcpQhf2m2aDDJR|UxKG:oIECuNFAxQDQQvF2= NYHUVYxpOjNyOEi2OFQ>
BA/F3 NUPGbohNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfRcZk4OiCq MVLEUXNQ M2Ow[Glv\HWlZYOgZY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDtc5V{\SCEQT;GN{Bk\WyuczDlfJBz\XO|aX7nJJdqdGRidInw[UBD[3JvQXLsJJdqfGhiSVO1NEBw\iByLkCwOFXPxE1? Mm\hNlMxQDh4NES=
BA/F3 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmHZO|IhcA>? NF3hWphFVVOR MYrJcoR2[2W|IHHueIlxem:uaX\ldoF1cX[nIHHjeIl3cXS7IHHnZYlve3RibX;1d4UhSkFxRkOgZ4VtdHNiZYjwdoV{e2mwZzDCZ5IuSWKuIGSzNVVKKG23dHHueEB4cXSqIFnDOVAhd2ZiMT63NVTPxE1? NH;Rb|gzOzB6OE[0OC=>
BA/F3 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jLN|czKGh? MofxSG1UVw>? MYfJcoR2[2W|IHP5eI91d3irY3n0fUBi\2GrboP0JI1wfXOnIFLBM2Y{KGOnbHzzJIV5eHKnc4PpcochSkOULVHCUEBHPDh4UzDteZRidnRiYYPz[ZN{\WRiYYOg[5Jwf3SqIFnubIljcXSrb36ge4l1cCCLQ{WwJI9nKDBwMECwPe69VQ>? MVGyN|MxOTdyMx?=
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BA/F3 NVPLVFlUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3Pmb|czKGh? M2P3fmROW09? M1ixSWlv\HWlZYOgZ5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmEwTjNiY3XscJMh\XiycnXzd4lv\yC5aXzkJJR6eGViQlPSMWFDVCCjc4Pld5Nm\CCjczDndo94fGhiSX7obYJqfGmxbjD3bZRpKEmFNUCgc4YhOC5yMEG5{txO NFzTflUzOzNyMUewNy=>
BA/F3 NH7zSphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXm3NkBp Mn\ISG1UVw>? M3X3WWlv\HWlZYOgZ5l1d3SxeHnjbZR6KGGpYXnud5QhdW:3c3WgRmEwTjNiY3XscJMh\XiycnXzd4lv\yCEQ2KtRWJNKFl{NUPIJI12fGGwdDDhd5Nme3OnZDDhd{Boem:5dHigTY5pcWKrdHnvckB4cXSqIFnDOVAhd2ZiMD6wNFI{|ryP M{nUcVI{OzBzN{Cz
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T cell M17HcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUm3NkBp NYXiZ5RbTE2VTx?= NFLJUodKdmirYnn0d{BidnSrIFPEN{0h[W6mIHHueIkhS0R{OD3pcoR2[2WmIGSgZ4VtdCCycn;sbYZmemG2aX;uJJdqfGhiSVO1NEBw\iByLkCwN:69VQ>? M1;UflE4OTV2NUGy
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MDA-MB-231 NV3FNXZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HLOVczKGh? MmLYSG1UVw>? MlrOTWM2OD1yLkCxNkDPxE1? MnL6NVU3OTV3MUK=
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MALME-3M M3j4fGN6fG:2b4jpZ{BCe3OjeR?= M{K5[VczKGh? NVyyR253TE2VTx?= MUXHTVUxRTZwNkGg{txO Mo\SNlQxOTV|Mke=
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SW620 NFvUfllEgXSxdH;4bYMhSXO|YYm= NI\NSlU4OiCq NUfSRWxVTE2VTx?= NEnneFJIUTVyPUiuOFMh|ryP NUX3[ZRHOjRyMUWzNlc>
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GXF251L MYHDfZRwfG:6aXOgRZN{[Xl? MWW0JIRigXN? MWnEUXNQ M1TDUGlEPTB;Mj6yOUDPxE1? MorsNlMzPTNyN{S=
NCI-H23 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojpO|IhcA>? MYXEUXNQ NIi3OXNKSzVyPUKuNlch|ryP NHu2XFMzOzV{MUCyNC=>
HCT116 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LaUVczKGh? MmqwSG1UVw>? NWfSOINRUUN3ME2yMlMh|ryP MkTINlM2OjFyMkC=
MCF7 MkHTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHyXHI4OiCq MnnTSG1UVw>? NX[2WI17UUN3ME2yMlU4KM7:TR?= M1HDXVI{PTJzMEKw
NCI-H460 NWTi[o5vT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWDqfHVJPzJiaB?= M2CzbmROW09? NFT3SVVKSzVyPUiuPVkh|ryP NIXHTpEzOzV{MUCyNC=>
DLD1 NFu0bnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzIbYVpPzJiaB?= NHPCXZhFVVOR NEPFV2RKSzVyPUSuOkDPxE1? MXiyN|U3Pzl4MB?=
NCI-H661 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\HU49zPzJiaB?= MoDJSG1UVw>? NYPNRlM3UUN3ME23Mlgh|ryP Mn3UNlM2Pjd7NkC=
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U937 NFriPYpHfW6ldHnvckBCe3OjeR?= NInaTnYyKM7:TR?= MXKxJIg> M1u4N2ROW09? M3vSVXJm\HWlZYOgUHBUNWmwZIXj[YQhXE6IYXzwbIEhemWuZXHz[UBqdiCqdX3hckBWQTN5IHPlcIx{ NIHOZ4wyPzZ6NEC5PS=>
murine mast cell MUTGeY5kfGmxbjDBd5NigQ>? NWXWc4Z3OSEQvF2= NEDzVYIzPCCq NWDWVXN7TE2VTx?= MU\Jcohq[mm2czDhcpRq\2WwLXnu[JVk\WRiSVy2JJNm[3KndHnvckBqdiCLZ1WgdJJqdWWmIH3veZNmKG2jc4SgZ4VtdHNiYYSgNUB2VQ>? NYnSfIRoOTd4OESwPVk>
BV-173 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF7MNIlKSzVyPUCuNFAxODByMUC5JO69VQ>? NVXPPFRoW0GQR1XS
K-562 M2jD[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVTJR|UxRTBwMECwNFAxOjZ4IN88US=> M2S2Z3NCVkeHUh?=
BL-70 NELNW5RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjRTWhHUUN3ME2wMlAxODByMEiyNkDPxE1? NX\Yc3R2W0GQR1XS
EM-2 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn;vTWM2OD1yLkCwNFAxOTB6IN88US=> M2OwOXNCVkeHUh?=
LAMA-84 M{TXRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPZdnRVUUN3ME2wMlAxODByM{KxJO69VQ>? M{PLXHNCVkeHUh?=
MEG-01 MmftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTBwMECwNFA6QCEQvF2= NEfPV2FUSU6JRWK=
EoL-1-cell NVfPTph4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nWSGlEPTB;MD6wNFAxOTNzIN88US=> MmrsV2FPT0WU
CTV-1 NIm4OGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTBwMECwNFQxPCEQvF2= Ml3BV2FPT0WU
TE-15 NYTQNphHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXTRXGhWUUN3ME2wMlAxPTh7IN88US=> NWTqb5ZlW0GQR1XS
NOS-1 NEXQS2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUXJR|UxRTBwMEC2NVMh|ryP NH7FeIJUSU6JRWK=
D-336MG MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2HSUGlEPTB;MD6wNFY{KM7:TR?= MXTTRW5ITVJ?
LB1047-RCC M4\LTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVqwOXJ1UUN3ME2wMlAxQTh7IN88US=> MWPTRW5ITVJ?
LB996-RCC M{fifGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4S5ZWlEPTB;MD6wNFk6OSEQvF2= M1fFV3NCVkeHUh?=
SW982 MoLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTBwMEGxNVUh|ryP NHXtZ|RUSU6JRWK=
TK10 MmLNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLpTWM2OD1yLkCxNVc1KM7:TR?= NEe5e2lUSU6JRWK=
A704 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPTTWM2OD1yLkCxOFkyKM7:TR?= MWTTRW5ITVJ?
TE-8 NUWxWlgxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTBwMEG1O|Yh|ryP MV7TRW5ITVJ?
DOHH-2 NXXsdnQxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{GzSWlEPTB;MD6wNVcyQSEQvF2= NXTnUZJjW0GQR1XS
HOP-62 Ml24S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NImyVWVKSzVyPUCuNFE5OzRizszN MmLaV2FPT0WU
TE-12 M3LhVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPzTWM2OD1yLkCxPFYyKM7:TR?= MUDTRW5ITVJ?
KGN MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4faWmlEPTB;MD6wNVk1OiEQvF2= MljaV2FPT0WU
NCI-H1648 NHXOcGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;wOYRiUUN3ME2wMlAzODFzIN88US=> M2GwSXNCVkeHUh?=
OS-RC-2 NYfGNFU2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7WWYtDUUN3ME2wMlAzODNizszN MWfTRW5ITVJ?
GB-1 M{DVXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{\4V2lEPTB;MD6wNlE2PyEQvF2= MXXTRW5ITVJ?
RXF393 NVHS[Xh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3TtTGlEPTB;MD6wNlM2PyEQvF2= MVjTRW5ITVJ?
LC-2-ad NF\QN2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWHJR|UxRTBwMEK1PFYh|ryP NIrWNFVUSU6JRWK=
KS-1 Mk\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTYd4pNUUN3ME2wMlAzPzNizszN NUnYOI5UW0GQR1XS
ETK-1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnFcJpKSzVyPUCuNFI5OzJizszN M1P5XXNCVkeHUh?=
SW954 NIjZN|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjPOllSUUN3ME2wMlAzQTJ5IN88US=> M3zPVXNCVkeHUh?=
Becker MmKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1K1UWlEPTB;MD6wN|AxOyEQvF2= NF:4TFhUSU6JRWK=
MZ1-PC M3TYW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2L5PWlEPTB;MD6wN|EyQSEQvF2= M37GUnNCVkeHUh?=
ES6 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvk[VlRUUN3ME2wMlA{OTl|IN88US=> NUPPdGN5W0GQR1XS
KURAMOCHI MoLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moe4TWM2OD1yLkCzOFg4KM7:TR?= MXXTRW5ITVJ?
CGTH-W-1 M1T6[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{P4RmlEPTB;MD6wN|U1QCEQvF2= NELmV4FUSU6JRWK=
VA-ES-BJ M1K4bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HQSWlEPTB;MD6wN|kxOiEQvF2= NUjPXph6W0GQR1XS
LXF-289 NEHOcFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmHKTWM2OD1yLkCzPVU3KM7:TR?= MXLTRW5ITVJ?
MPP-89 NEnWXpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17rXWlEPTB;MD6wOFA1QSEQvF2= M{TlRXNCVkeHUh?=
SW872 M{PEOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\xcZhtUUN3ME2wMlA1OTZzIN88US=> NFfs[4pUSU6JRWK=
SNB75 M1TwOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWm2eWZ4UUN3ME2wMlA1PDN3IN88US=> NHz3OJZUSU6JRWK=
PSN1 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTBwMES0O|Qh|ryP MV;TRW5ITVJ?
LB831-BLC M4fzb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2jIVWlEPTB;MD6wOFYxQSEQvF2= NFzONHdUSU6JRWK=
MFH-ino MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTBwMES3NlQh|ryP M1naPXNCVkeHUh?=
TGBC24TKB M13Xcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXMTWM2OD1yLkC0O|YyKM7:TR?= NFPMXXpUSU6JRWK=
A388 M2LTb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHL2XHdKSzVyPUCuNFUxQTVizszN Mk\sV2FPT0WU
BB30-HNC NUDQOXVCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3O1[GlEPTB;MD6wOVQ{PyEQvF2= MVLTRW5ITVJ?
GI-ME-N MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTBwME[xNVgh|ryP MV\TRW5ITVJ?
TGBC1TKB NU\ueY93T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NELzNldKSzVyPUCuNFYyPjRizszN NUL0e5pxW0GQR1XS
TE-10 NEm5ZYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrl[VlKSzVyPUCuNFY{PTdizszN Mk\jV2FPT0WU
A498 NHjEfHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUjJR|UxRTBwMEeyPFQh|ryP MVTTRW5ITVJ?
TE-11 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTBwMEe4OVgh|ryP MlzVV2FPT0WU
BB65-RCC MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWi2eI1UUUN3ME2wMlA5OjJ5IN88US=> MXXTRW5ITVJ?
C2BBe1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRTBwMEizNFgh|ryP NEH6PJdUSU6JRWK=
NCI-H747 MoS5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7W[oxKSzVyPUCuNFg{PjJizszN NHnjcZhUSU6JRWK=
IST-MES1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlXTTWM2OD1yLkC4OVUzKM7:TR?= NIrQNndUSU6JRWK=
KALS-1 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mli2TWM2OD1yLkC5OFkh|ryP MXzTRW5ITVJ?
GCIY MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTBwMEm2OVYh|ryP M1n2bnNCVkeHUh?=
RL95-2 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTBwMUCzPEDPxE1? MWXTRW5ITVJ?
TE-1 NWPSSoFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVP4WVlGUUN3ME2wMlExPTRizszN NW\2NXpPW0GQR1XS
NCI-H1355 NVrmOWJRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUjQS|hKUUN3ME2wMlEyODJ6IN88US=> MX\TRW5ITVJ?
SW962 NVm0TZBqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEf5boZKSzVyPUCuNVEzQTJizszN M13xdnNCVkeHUh?=
KLE NXfaPZlYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkDMTWM2OD1yLkGxN|E4KM7:TR?= M4TYNHNCVkeHUh?=
MC116 NVLUbZdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1K4VmlEPTB;MD6xNVQyKM7:TR?= NX;kT4FiW0GQR1XS
NMC-G1 M1PTW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnj6TWM2OD1yLkGxOlA3KM7:TR?= NFnrTHVUSU6JRWK=
KU812 MlrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTBwMUG4PFMh|ryP Mm\LV2FPT0WU
COLO-829 M4HiZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHOWFJrUUN3ME2wMlEzOjF|IN88US=> M3fjenNCVkeHUh?=
NTERA-S-cl-D1 NIXMbohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXqxcWtnUUN3ME2wMlEzOjh|IN88US=> NHK0c2NUSU6JRWK=
IST-MEL1 NGrPVnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITrNoRKSzVyPUCuNVM1PSEQvF2= Mo\qV2FPT0WU
MLMA MlvDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUL1dYM5UUN3ME2wMlE1ODN{IN88US=> MX3TRW5ITVJ?
LS-123 Ml7xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEL1WpZKSzVyPUCuNVQxPjRizszN M4f2dXNCVkeHUh?=
LB2518-MEL NHnUWpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoTCTWM2OD1yLkG0NVYzKM7:TR?= NUnBWHVFW0GQR1XS
NB69 M3O4Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTBwMUS0N|Yh|ryP MojiV2FPT0WU
8-MG-BA M33ZSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlrFTWM2OD1yLkG1OFU5KM7:TR?= NW\4b241W0GQR1XS
K5 NFvoUGZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzNSXMyUUN3ME2wMlE3PDh7IN88US=> MnS3V2FPT0WU
KINGS-1 NYHEXW5nT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHPTWM2OD1yLkG2OlY3KM7:TR?= MVvTRW5ITVJ?
SF268 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2TDbGlEPTB;MD6xO|QxPCEQvF2= NGDzSWpUSU6JRWK=
PF-382 NXXDdnp5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M362SmlEPTB;MD6xO|Y4QCEQvF2= MVTTRW5ITVJ?
SH-4 M3HPNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorJTWM2OD1yLkG4OFE{KM7:TR?= NYjIeVQzW0GQR1XS
NALM-6 NGrRU5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVG4SHF1UUN3ME2wMlE6Ojl3IN88US=> MlTpV2FPT0WU
CP66-MEL MlPCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1H1V2lEPTB;MD6xPVU{OSEQvF2= MULTRW5ITVJ?
697 NH64bWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTBwMUm5PFch|ryP NV;OXIlzW0GQR1XS
CP67-MEL NXvVRVRIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zVTmlEPTB;MD6yNFQ5QCEQvF2= M{DufnNCVkeHUh?=
DSH1 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGX5TmxKSzVyPUCuNlQxODFizszN M{HmVHNCVkeHUh?=
HCE-4 MkHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfaTWM2OD1yLkK2OFM6KM7:TR?= NEHiO3NUSU6JRWK=
MZ2-MEL NXzWbIdPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\wU4NKSzVyPUCuNlg2OzdizszN NUfR[o12W0GQR1XS
BL-41 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTBwMkmxNlMh|ryP MkDkV2FPT0WU
HUTU-80 NEO3[mpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1ToTGlEPTB;MD6zNVQzKM7:TR?= M{j1eXNCVkeHUh?=
LOXIMVI MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnocFFKSzVyPUCuN|E2ODNizszN MYDTRW5ITVJ?
no-10 M3v0T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4DzTWlEPTB;MD6zNVk{OSEQvF2= NUXINWl4W0GQR1XS
KARPAS-422 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfzTWM2OD1yLkOzPVk4KM7:TR?= Mn3EV2FPT0WU
SW684 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGDtRZRKSzVyPUCuN|Q6QCEQvF2= NHHocoVUSU6JRWK=
SF126 NVzTcZZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTBwM{W0NUDPxE1? MnLUV2FPT0WU
D-263MG M{i0N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTBwM{[yNlQh|ryP MkXHV2FPT0WU
OVCAR-4 MkXyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTSTWM2OD1yLkO3OFM{KM7:TR?= NGKzW4FUSU6JRWK=
BB49-HNC MoXRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEL0NIJKSzVyPUCuN|g2QTlizszN M4j1PHNCVkeHUh?=
ONS-76 MlXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTjPVlKSzVyPUCuOFI6PTFizszN MULTRW5ITVJ?
MZ7-mel MnPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV\WOpg1UUN3ME2wMlQ4QTFzIN88US=> NFH3WmZUSU6JRWK=
RCC10RGB NXTiU3VXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWTJR|UxRTBwNEmxNUDPxE1? M2\oPHNCVkeHUh?=
BOKU NVfVUHlzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17HbGlEPTB;MD60PVE{OyEQvF2= MXTTRW5ITVJ?
no-11 NGHvfGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlm0TWM2OD1yLkWwNlI5KM7:TR?= MonCV2FPT0WU
IST-SL2 M134NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2Owd2lEPTB;MD61NFMxOiEQvF2= MYLTRW5ITVJ?
RKO NFvPV5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmS3TWM2OD1yLkWyPVY3KM7:TR?= NF;mSWhUSU6JRWK=
HT-144 Ml\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXSTWM2OD1yLkWzOlA6KM7:TR?= M{fjeHNCVkeHUh?=
NCI-H446 NGrVXmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjrS2xkUUN3ME2wMlYzPzZizszN MlnzV2FPT0WU
QIMR-WIL NXmzZWlwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3L2cWlEPTB;MD63NFYzQSEQvF2= MojIV2FPT0WU
MHH-PREB-1 NXXRUmx5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjqVXVCUUN3ME2wMlc1PDZ7IN88US=> MljRV2FPT0WU
EW-16 NH:y[G5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInLeVNKSzVyPUCuO|YyPzhizszN M{PIcHNCVkeHUh?=
EW-24 NUfQbHlvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkWyTWM2OD1yLke4NVY2KM7:TR?= MkHxV2FPT0WU
LB373-MEL-D M1\1dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFjGRVNKSzVyPUCuPFI2ODhizszN MYXTRW5ITVJ?
TE-9 MorqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnDbHVKSzVyPUCuPFc2OzJizszN MlPZV2FPT0WU
A3-KAW NH;FdFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWjIXHBiUUN3ME2wMlk5PDV{IN88US=> NWPKWXhFW0GQR1XS
A101D MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml62TWM2OD1zLkCzNFQ{KM7:TR?= M4HjOHNCVkeHUh?=
OCUB-M MnTlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIOxXolKSzVyPUGuNFQ1OTJizszN Mkm4V2FPT0WU
ES4 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrXbVlKSzVyPUGuNFUyPDVizszN MX3TRW5ITVJ?
TE-6 NELUV4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYjJR|UxRTFwMkGyNlYh|ryP NGDO[HhUSU6JRWK=
D-502MG MmjBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PIb2lEPTB;MT6yN|M4PiEQvF2= MlrhV2FPT0WU
KNS-42 Mln1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIr3O5BKSzVyPUGuNlQ1OTJizszN M3;zUXNCVkeHUh?=
SNU-C2B MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PmeGlEPTB;MT6zNFU5QSEQvF2= NHnrbZNUSU6JRWK=
NCI-H1838 MmTWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nROmlEPTB;MT6zNFc{OyEQvF2= NFTYRWRUSU6JRWK=
NKM-1 NHjiZmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mk\STWM2OD1zLkOwPFU6KM7:TR?= MUjTRW5ITVJ?
GI-1 M1KwcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHHZ4R4UUN3ME2xMlM3OjJizszN NXfDSm9kW0GQR1XS
NB5 MnfNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPvc41yUUN3ME2xMlM6QDJ5IN88US=> MlTsV2FPT0WU
CAS-1 MkLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HFS2lEPTB;MT60NFk6OiEQvF2= MVPTRW5ITVJ?
HCE-T NXLtUWR1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPESGVKSzVyPUGuOVY4OTRizszN M4\jbXNCVkeHUh?=
SBC-1 NFvpO4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjTTGFpUUN3ME2xMlU4QTh2IN88US=> NYHrUolVW0GQR1XS
JiyoyeP-2003 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofGTWM2OD1zLkezOFY3KM7:TR?= MoC5V2FPT0WU
TE-5 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\1dHJIUUN3ME2xMlc6OTN7IN88US=> M3TSR3NCVkeHUh?=
CAN MmToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTFwOEKyOVIh|ryP NF[4OWpUSU6JRWK=
SK-UT-1 NFL0dGtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFfhUFdKSzVyPUKuNVY3QTNizszN MmX6V2FPT0WU
JVM-2 NHL4cppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTKTWM2OD1{LkO2Nlg1KM7:TR?= NF7jd2pUSU6JRWK=
LB771-HNC NXfFTXlFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3i4S2lEPTB;Mj61O|U2OSEQvF2= M{fDeHNCVkeHUh?=
NCCIT MnXnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrhV|BKSzVyPUKuPFY3OTZizszN MV7TRW5ITVJ?
NCI-H2126 NG\RXFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFL6e4tKSzVyPUKuPFc2PTJizszN M4fBTnNCVkeHUh?=
Calu-6 MoDRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFq1bmxKSzVyPUOuNFU4PDFizszN NF7mUFNUSU6JRWK=
SK-LMS-1 NVP5RnRnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUe2THdYUUN3ME2zMlEyQDh4IN88US=> MWTTRW5ITVJ?
ARH-77 Mlr0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3MTWM2OD1|LkS2PVE2KM7:TR?= MXzTRW5ITVJ?
NB17 NHjFTolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofRTWM2OD1|Lk[zPFQ4KM7:TR?= MV7TRW5ITVJ?
A253 NYnRS49sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXzJR|UxRTNwN{OyOFYh|ryP NV;pNW5FW0GQR1XS
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MV-4-11 NEnoXXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFT1[YVKSzVyPUSuN|Y1PTRizszN NVrYZmg2W0GQR1XS
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KG-1 MnX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzEO2dIUUN3ME20MlYxQDR3IN88US=> MVnTRW5ITVJ?
OCI-AML2 NGnxWZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfpTWM2OD13Lki2NVU1KM7:TR?= MmLSV2FPT0WU
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SJSA-1 Mn;FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnPiTWM2OD16LkeyPFA2KM7:TR?= MVzTRW5ITVJ?
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HEL M4rqNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTFyLkS3O|Yh|ryP NETlcGxUSU6JRWK=
ALL-PO MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{WwRWlEPTB;MUCuO|k{QCEQvF2= MXnTRW5ITVJ?
TGW NEDqeJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmexTWM2OD1zMT6yPFI5KM7:TR?= MmPIV2FPT0WU
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IA-LM MljqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnEVYZKSzVyPUGyMlQ1PDVizszN MlfxV2FPT0WU
UACC-257 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHjkVWRKSzVyPUGyMlkyQThizszN NID2cnRUSU6JRWK=
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Raji NV;sWGc5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHfuO5VKSzVyPUGzMlc1QTdizszN MUfTRW5ITVJ?
SF539 NV:1[|QyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TUXmlEPTB;MUOuPFU2PyEQvF2= NF\RWYVUSU6JRWK=
DMS-153 M1rHfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1i4N2lEPTB;MUSuNFAzQCEQvF2= NXLGWY5rW0GQR1XS
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RPMI-8866 NHHoN5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEG5RlNKSzVyPUG3MlQ1PTRizszN NVzCW3V2W0GQR1XS
NCI-H510A NXO5PINvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUnJR|UxRTF7LkO5O|Mh|ryP Mo\pV2FPT0WU
NB13 NYXHdoZFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVyyfmNSUUN3ME2xPU41QDd5IN88US=> MV;TRW5ITVJ?
HAL-01 NVXob2UzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3T4NWlEPTB;MUmuO|U1OyEQvF2= NGDXcG5USU6JRWK=
NCI-H720 NYjvR3RYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX3hfXVYUUN3ME2yNE4zPzN|IN88US=> NILiXmZUSU6JRWK=
REH NFv0dm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTJyLk[zOVch|ryP M1PyNHNCVkeHUh?=
KNS-81-FD NEfDTI9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TNZ2lEPTB;MkOuNVQ3KM7:TR?= M3XGW3NCVkeHUh?=
HC-1 MnHoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLZTWM2OD1{ND61OVUyKM7:TR?= NV71N3FjW0GQR1XS
NCI-H2141 MkfWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLiSlVmUUN3ME2yOE44PzV2IN88US=> M{nRXXNCVkeHUh?=
MOLT-4 NX3sd5pNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTOTWM2OD1{Nj62O|U{KM7:TR?= NVi3bml7W0GQR1XS
OMC-1 MnPFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrDd4dzUUN3ME2yO{4yPDJ{IN88US=> M{\WXXNCVkeHUh?=
LC-1F MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn[4TWM2OD1{Nz6zNlQ2KM7:TR?= MV;TRW5ITVJ?
NCI-H1304 NVf6OoduT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTJ6LkG2Nlgh|ryP M3TqeHNCVkeHUh?=
BC-1 NVz1N3B6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHydWRKSzVyPUK4MlY2OSEQvF2= NVXRT5p5W0GQR1XS
NCI-H64 MlTCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzISoVKSzVyPUK5MlYzPTNizszN MXPTRW5ITVJ?
MOLT-16 NHHoOWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DHb2lEPTB;MkmuOlI6OiEQvF2= M1O1O3NCVkeHUh?=
U-87-MG M2C2cWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVftfJRxUUN3ME2zNE44PjZizszN NFHZd2tUSU6JRWK=
GAK NInnSWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnkU29KSzVyPUOxMlI3QDZizszN NX3jTow3W0GQR1XS
ES8 M2\Udmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrYc2ZyUUN3ME2zNk4yOjV{IN88US=> NHKxR3ZUSU6JRWK=
HCC1599 M{fXcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTN{LkOzNlUh|ryP MkjNV2FPT0WU
EB-3 M4XjTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWK0NIg{UUN3ME2zOE4{OTF5IN88US=> NYDDeYhRW0GQR1XS
HCC1187 NFjDUHdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTzTWM2OD1|NT64NFUzKM7:TR?= NVvXNHpmW0GQR1XS
SK-PN-DW NGXJTI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVfZc|NjUUN3ME2zOk4yQTR|IN88US=> NWn1Rlc3W0GQR1XS
JVM-3 NIm0TWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NITUT25KSzVyPUO3MlI{OzhizszN NHvJSHVUSU6JRWK=
HCC2157 NEX4[ItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDwW2hKSzVyPUO3Mlk6PDZizszN M2DIdXNCVkeHUh?=
A4-Fuk M1LzWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDhPFFVUUN3ME2zPE4yODB7IN88US=> M3\iT3NCVkeHUh?=
COR-L279 NULqRXkyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWO0N4NzUUN3ME20NE4zQDVzIN88US=> MkTXV2FPT0WU
DEL MnTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjudWdqUUN3ME20NU46ODh4IN88US=> MXrTRW5ITVJ?
NCI-H1395 NW\SV5B3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXLHTZlFUUN3ME20Nk4xOTZ|IN88US=> NEfoOGhUSU6JRWK=
MHH-NB-11 MnnFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYTJR|UxRTR|LkC4NVgh|ryP M3\NOXNCVkeHUh?=
NCI-H2107 NWnmSZFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\hUFFKSzVyPUSzMlQ5PDZizszN NYeyTJh4W0GQR1XS
NEC8 NXLye2FZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13XNWlEPTB;NESuN|M3KM7:TR?= MULTRW5ITVJ?
COLO-684 NEnGTJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILC[lBKSzVyPUS2MlIzPThizszN MmfBV2FPT0WU
LS-411N NH23bJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{W0WmlEPTB;NEiuOFc1QCEQvF2= M2i2WnNCVkeHUh?=

... 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 3年-20℃
2年-80℃in solvent
別名 BMS-354825
溶解度 (25°C) * In vitro DMSO 98 mg/mL (200.81 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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

文献中の引用 (62)

Frequently Asked Questions

  • Question 1
    what’s the difference between S1021 and S7782? Which one is better for in vivo studies?

    Answer: Usually, hydrate will be more stable and dissolve better than free base. But this compound (S1021) dissolves better in DMSO than hydrate one (S7782).

  • Question 2
    Can I give dasatinib to mice by oral gavage? If so, how to dissolve the drug?

    Answer: Our S1021 Dasatinib in 1% DMSO+30% PEG 300+1% Tween 80 at 30 mg/ml is a suspension which you can administrate to mice via oral gavage. If you want a clear solution, it can be dissolved in 4% DMSO+30% PEG 300+5% Tween 80+ddH2O at 5 mg/ml clearly.

技術サポート&よくある質問(FAQ)

ストックの作り方、阻害剤の保管する方法、細胞実験や動物実験に注意すべきな点を全部含めており、製品を取扱う時よくあった質問に対して取扱説明書でお答えいたします。

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    KX2-391は初めの臨床Src阻害剤(ペプチド模倣型)で、Srcのペプチド基質サイトに作用することです。KX2-391は癌細胞系にGI50値が9-60 nMです。臨床2期。

  • PP1

    PP1は一種の有効で、選択性的なSrc阻害剤で、Lck/Fynに作用する時のIC50値が5 nM/6 nMです。

  • PP2

    PP2は一種のSrc家族キナーゼ阻害剤で、無細胞試験でLck/Fynに作用する時のIC50値が4 nM/5 nMです。PP2は、Srcに作用する効果はEGFRに作用する効果より100倍が高くなりますが、ZAP-70、JAK2とPKAに活性を表しません。

最近チェックしたアイテム

Tags: Dasatinibを買う | Dasatinib供給者 | Dasatinibを購入する | Dasatinib費用 | Dasatinib生産者 | オーダーDasatinib | Dasatinib代理店
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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