ABT-263 (Navitoclax) 化学構造
分子量: 974.61

高品質保証

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Quality Control & MSDS

製品説明

  • Compare Bcl-2 Inhibitors
    Bcl-2製品生物活性の比較
  • 研究分野

製品の説明

生物活性

製品説明 ABT-263(Navitoclax)は、 Bcl-xLBcl-2Bcl-w の強力な阻害剤で、Kiがそれぞれ ≤ 0.5 nM、≤1 nM 、≤ 1 nMです。
ターゲット

Bcl-xL

Bcl-2

Bcl-w

IC50

≤ 0.5 nM (Ki)

≤1 nM (Ki)

≤ 1 nM (Ki)[1]

In vitro試験 ABT-263 is structurally related to ABT-737; it is a disruptor of Bcl-2/Bcl-xL interactions with pro-apoptotic proteins. Overexpression of the prosurvival Bcl-2 family members is commonly associated with tumor maintenance, progression, and chemoresistance. [1] ABT-263 displays the protection afforded by overexpression of Bcl-2 or Bcl-xL with EC50 values of 60 nM and 20 nM, respectively. [1] A wide range of cellular activity is observed with ABT-263 having a 50% growth inhibition (EC50) of 110 nM against the most sensitive line (H146), whereas its activity in the least sensitive line (H82) results in an EC50 at 22 μM. All four cell lines with EC50 values of <400 nM (H146, H889, H1963, and H1417) are also highly sensitive to ABT-737, and the two most resistant lines (H1048 and H82) are similarly resistant to ABT-263. [2]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
EoL-1-cell MojKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTBwMEC2Olkh|ryP M4XXWHNCVkeHUh?=
MV-4-11 M1nTc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTBwMEG1PFYh|ryP M2PoXHNCVkeHUh?=
NKM-1 Mn7HS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXns[mFNUUN3ME2wMlAyPjl7IN88US=> M{Xqc3NCVkeHUh?=
ML-2 NYjVeHl4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTBwMEG5PFMh|ryP MX;TRW5ITVJ?
BV-173 M3zufmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NE\qbVlKSzVyPUCuNFI{OTRizszN MXLTRW5ITVJ?
RS4-11 MoPKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTBwMEK1PFch|ryP NEe3O2RUSU6JRWK=
HL-60 MmDOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3nuTmlEPTB;MD6wNlkxQCEQvF2= NFXTPW5USU6JRWK=
KY821 M2fRVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHnTWM2OD1yLkCyPVc2KM7:TR?= NGfoRmRUSU6JRWK=
ECC10 NX\GZ|RuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEeyfVBKSzVyPUCuNFM4QTJizszN M3rNPXNCVkeHUh?=
NCI-H720 M2jUTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\ETWM2OD1yLkC0NFEyKM7:TR?= NIHxZXBUSU6JRWK=
QIMR-WIL M{HmbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVX6coQ2UUN3ME2wMlA1Ojh5IN88US=> MknlV2FPT0WU
KG-1 NVvOV|dST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEP3R3BKSzVyPUCuNFQ1QDZizszN NVLSZnRbW0GQR1XS
TGW M1jaUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TGTmlEPTB;MD6wOFY{OyEQvF2= MXfTRW5ITVJ?
ATN-1 NEDRVZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nKdWlEPTB;MD6wOFc{OyEQvF2= MXTTRW5ITVJ?
RH-18 NYDPfZBRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jzSWlEPTB;MD6wOlA1QCEQvF2= NEX6eXFUSU6JRWK=
EW-18 NGDwd4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTBwME[4OFEh|ryP NFriWFdUSU6JRWK=
NB17 NIn4fVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXFbI4zUUN3ME2wMlA4OTJ2IN88US=> MkHKV2FPT0WU
SK-NEP-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHOXYVKSzVyPUCuNFczOTNizszN MoTsV2FPT0WU
P12-ICHIKAWA MlTmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFPkPHJKSzVyPUCuNFc4PzhizszN MWPTRW5ITVJ?
KARPAS-45 M3XEU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XHTWlEPTB;MD6wO|gyPSEQvF2= NEf6RVVUSU6JRWK=
EW-3 NFvkUmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoHjTWM2OD1yLkC4NFU{KM7:TR?= MnLrV2FPT0WU
NB13 NXvWcmI3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4q2e2lEPTB;MD6wPFIxOyEQvF2= M4Dk[XNCVkeHUh?=
NCI-H209 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmiwTWM2OD1yLkC4O|A1KM7:TR?= M4HwSHNCVkeHUh?=
NCI-H1092 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTBwMUCyO|Uh|ryP NIHoZppUSU6JRWK=
NH-12 M4\re2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HjVWlEPTB;MD6xNFc1PCEQvF2= M4njU3NCVkeHUh?=
697 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYPu[nlkUUN3ME2wMlExQDN7IN88US=> NIXNepRUSU6JRWK=
KE-37 NVTU[3d1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\hXGlEPTB;MD6xNVM4KM7:TR?= NUTRbG1wW0GQR1XS
MOLT-4 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTUTWM2OD1yLkG1NVY6KM7:TR?= Mn3PV2FPT0WU
CHP-134 NU\lTHFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jqcGlEPTB;MD6xOlMxPiEQvF2= M{\nSnNCVkeHUh?=
D-283MED NXfPOmtOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILWRW9KSzVyPUCuNVc3QDZizszN M{frU3NCVkeHUh?=
LU-135 NVzMU5JqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXrfIpKSzVyPUCuNVg2PTJizszN NIHFNm5USU6JRWK=
LU-134-A NEixOllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH3qUG1KSzVyPUCuNVg3PzFizszN NHftR|VUSU6JRWK=
EM-2 NUfrXpFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIKwU5pKSzVyPUCuNVk6OThizszN MmXIV2FPT0WU
LU-139 NX\vb5BmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\1N2FEUUN3ME2wMlIxPDl6IN88US=> NG\uSoRUSU6JRWK=
ALL-PO MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml32TWM2OD1yLkKxPVg5KM7:TR?= Mm\HV2FPT0WU
NB12 MonES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\OTWM2OD1yLkKzNVE2KM7:TR?= M4XEeXNCVkeHUh?=
KP-N-YN M{POWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fMUGlEPTB;MD6yN|U4OyEQvF2= Ml7RV2FPT0WU
BEN MlrpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTBwMkO5Olgh|ryP M1\3cnNCVkeHUh?=
HCC1569 M4m2XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjHT|lKSzVyPUCuNlUyODZizszN M1f1W3NCVkeHUh?=
HuO9 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWfqWW14UUN3ME2wMlI3PzF3IN88US=> NGTueGhUSU6JRWK=
WM-115 M3HXeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTBwMke3N|gh|ryP NVe1PXVFW0GQR1XS
CCRF-CEM Mnz5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\MTWM2OD1yLkOzOVI6KM7:TR?= MUXTRW5ITVJ?
IST-SL1 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF70ZmhKSzVyPUCuN|U{PDNizszN MlG5V2FPT0WU
BE-13 MmGyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDiSZRDUUN3ME2wMlM3PDV7IN88US=> NWq2[3QxW0GQR1XS
COR-L88 M3zSemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIiwU25KSzVyPUCuN|Y2PCEQvF2= MV;TRW5ITVJ?
DOHH-2 Mo\ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVvJR|UxRTBwNEGwNlMh|ryP MUnTRW5ITVJ?
A704 MlvoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTBwNEK2O{DPxE1? NUDCZlg6W0GQR1XS
KNS-81-FD NWLpelEzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml7qTWM2OD1yLkS0NFE4KM7:TR?= MWfTRW5ITVJ?
RPMI-8226 MoDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTBwNEW2OVIh|ryP NU[2cZUzW0GQR1XS
TGBC24TKB NW\UflZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGr0WZpKSzVyPUCuOFU4PzhizszN M4HHZXNCVkeHUh?=
NCI-H1304 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnQTWM2OD1yLkS2NVU4KM7:TR?= NGS5TW5USU6JRWK=
MOLT-13 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlj3TWM2OD1yLkS2OlE{KM7:TR?= MWDTRW5ITVJ?
EW-22 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTBwNE[2O|Eh|ryP Mle1V2FPT0WU
MS-1 M1vrWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWPMU4VqUUN3ME2wMlQ3QTN|IN88US=> MVjTRW5ITVJ?
RMG-I M4XqVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIG2bmpKSzVyPUCuOFk1PjRizszN NE\2NlhUSU6JRWK=
NTERA-S-cl-D1 MmrmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTBwNUCwNVkh|ryP NWC1Wm4yW0GQR1XS
NCI-H1048 NGLP[5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTBwNUC5OVMh|ryP M3\uS3NCVkeHUh?=
SW1417 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTBwNUW0N|gh|ryP NW\kNVNMW0GQR1XS
DB MmrXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;nTWM2OD1yLkW3NFgh|ryP NFTXdWZUSU6JRWK=
MEG-01 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTBwNUizNkDPxE1? NWTXV4s2W0GQR1XS
EW-13 NHq2Z4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33Cb2lEPTB;MD61PFM1OSEQvF2= NIrSNHlUSU6JRWK=
LAMA-84 MkDES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYXJR|UxRTBwNUmyNFch|ryP NFfXV3VUSU6JRWK=
J-RT3-T3-5 NGfQc4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYHJR|UxRTBwNkC4NFgh|ryP NHzoW3JUSU6JRWK=
MOLT-16 NYixXFVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUi3WnprUUN3ME2wMlY2OjZ2IN88US=> MYjTRW5ITVJ?
DU-4475 M4nxZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnzoTWM2OD1yLk[1OFI4KM7:TR?= M2\pPXNCVkeHUh?=
HAL-01 M2Hm[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTBwN{K1OFkh|ryP NHnD[5FUSU6JRWK=
RD Mn[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEL0SHdKSzVyPUCuO|U5QTlizszN MmTtV2FPT0WU
OAW-28 NWPKVJF7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DQUWlEPTB;MD63PFM4KM7:TR?= M3vxOXNCVkeHUh?=
HCC38 NW\WVlJUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XLemlEPTB;MD64NFE6KM7:TR?= M3XUVHNCVkeHUh?=
NMC-G1 M1TmXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fjSWlEPTB;MD64NVEzOSEQvF2= MUTTRW5ITVJ?
EW-16 NUHWenZnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUX3OIlFUUN3ME2wMlgyOzJ6IN88US=> MVrTRW5ITVJ?
DU-145 MnKxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTBwOEm5NlMh|ryP M3zDbHNCVkeHUh?=
HPAF-II MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3zSnZKSzVyPUCuPVI3OjhizszN MWXTRW5ITVJ?
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PA-1 NY\aTpBGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rVUWlEPTB;MD65OVY1OiEQvF2= NXjU[lIzW0GQR1XS
OAW-42 NYq5Smw{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTBwOU[xOFYh|ryP NUjTS|VVW0GQR1XS
L-428 M3zLeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2nvNmlEPTB;MT6wNVI2KM7:TR?= NVK1OVJQW0GQR1XS
COLO-824 NUTjN3ZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTFwMEG3NFgh|ryP MWnTRW5ITVJ?
P30-OHK NULOZmdLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2OxcWlEPTB;MT6wOFY5QCEQvF2= NI\udIZUSU6JRWK=
NCI-H2170 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGnXdXlKSzVyPUGuNFYzOyEQvF2= NFPzOFNUSU6JRWK=
HCC2998 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYTtT3Y{UUN3ME2xMlA4OTN3IN88US=> NWrrV4NwW0GQR1XS
NB14 MlzTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkW3TWM2OD1zLkGzO|Q5KM7:TR?= NFGyZm5USU6JRWK=
TGBC1TKB Mmj6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnH1TWM2OD1zLkG0NVUzKM7:TR?= MmXQV2FPT0WU
KP-N-YS NEn6em1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPwOIpRUUN3ME2xMlE3OjN4IN88US=> NXzweVg4W0GQR1XS
CAL-120 M4HoWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWLJR|UxRTFwMU[0Nlkh|ryP M2njR3NCVkeHUh?=
SBC-1 MkXaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1j4dWlEPTB;MT6xPVA2OyEQvF2= NWj6boRQW0GQR1XS
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HCC2157 NIf5RWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTFwMUm0PVQh|ryP NIXSc4xUSU6JRWK=
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HEL NGXST4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HsO2lEPTB;MT6zNVAzQSEQvF2= NIKxTlVUSU6JRWK=
ES4 NITybYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjROJN[UUN3ME2xMlM1QTl6IN88US=> M1PQR3NCVkeHUh?=
NCI-SNU-1 NUHE[ndYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEHRfWtKSzVyPUGuN|Y2PTVizszN NUntPZlGW0GQR1XS
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NCI-H2342 M2X2PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3y3VGlEPTB;MT60NFI3QSEQvF2= MU\TRW5ITVJ?
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MLMA Mof6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYq2VWl[UUN3ME2xMlk3Pjd5IN88US=> MkHPV2FPT0WU
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HuO-3N1 M1ywbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\PNmlEPTB;Mj60PFc5KM7:TR?= M2fKVnNCVkeHUh?=
MHH-NB-11 M3jWWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofhTWM2OD1{LkWxNVU5KM7:TR?= MWrTRW5ITVJ?
TGBC11TKB MlK2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLGTWM2OD1{LkW3OlgyKM7:TR?= MYHTRW5ITVJ?
HOP-92 NVS1dWVoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fITmlEPTB;Mj61PFc1OyEQvF2= M{jWdnNCVkeHUh?=
IGR-1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLQTWM2OD1{Lk[yNFM2KM7:TR?= NFXqb5VUSU6JRWK=
GOTO MmnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3jO2hKSzVyPUKuOlU{PzdizszN NGjJO4hUSU6JRWK=
NCI-H1650 NHTSempIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTJwN{KyNVUh|ryP NEfhO2JUSU6JRWK=
NCI-H1581 NWW3b2d{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTJwN{m2PFEh|ryP NEixUHhUSU6JRWK=
NCI-H2405 MkXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDPWZJKSzVyPUKuPFI4QDJizszN NITlW2dUSU6JRWK=
U-118-MG MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEC2TFVKSzVyPUKuPVY1QTFizszN M2LCd3NCVkeHUh?=
DoTc2-4510 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofkTWM2OD1|LkCxOFE4KM7:TR?= Ml\NV2FPT0WU
NCI-H596 NHf6V3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTNwMES5PVch|ryP MljFV2FPT0WU
MPP-89 M2TjfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX7JR|UxRTNwMEW2OlYh|ryP NETmRYVUSU6JRWK=
GCIY NFHkcY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXXscJljUUN3ME2zMlIxPDlzIN88US=> MoDKV2FPT0WU
SW626 MnLLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4rYUmlEPTB;Mz6yOFU1OyEQvF2= M{DvdHNCVkeHUh?=
OCI-AML2 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEXwT5JKSzVyPUOuN|EzPzJizszN MlPhV2FPT0WU
NBsusSR M{nBeWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTNwM{S5N|gh|ryP MmL1V2FPT0WU
AN3-CA NVXYR3lPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH;kdVZKSzVyPUOuOFQzOzhizszN NYW3[JJsW0GQR1XS
EFM-19 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXXyc2RZUUN3ME2zMlQ5OzN7IN88US=> MmSzV2FPT0WU
RVH-421 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2T1TWlEPTB;Mz61Olg4PyEQvF2= MYrTRW5ITVJ?
5637 MnjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTFeGljUUN3ME2zMlYyOTB|IN88US=> NGHYW|lUSU6JRWK=
PANC-08-13 MkPXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIHRdllKSzVyPUOuOlM1PzJizszN NFPMfXdUSU6JRWK=
H9 MonFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrOTWM2OD1|Lk[3NVQ1KM7:TR?= NGKwfWVUSU6JRWK=
KARPAS-299 NXXxcXB4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPDU2hKSzVyPUOuOlc{PjFizszN NYHTVXZYW0GQR1XS
TE-5 MlfHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13UVWlEPTB;Mz63NFcxQSEQvF2= M3:5d3NCVkeHUh?=
NOS-1 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlzFTWM2OD1|Lke5PFM1KM7:TR?= M4HqVHNCVkeHUh?=
HH NGDKboJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUflVnk1UUN3ME2zMlg{QDZ6IN88US=> MlvJV2FPT0WU
769-P NFK1boFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTNwOEm1NUDPxE1? M4mydHNCVkeHUh?=
CHP-212 NE\YXFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M135XmlEPTB;Mz65NlU1QSEQvF2= MoHvV2FPT0WU
NCI-H82 MnzqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGSyXnlKSzVyPUOuPVU6OzZizszN NVOxOFVwW0GQR1XS
Mo-T NF\i[pFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTRwMESzNVIh|ryP MnfGV2FPT0WU
BB65-RCC NVLaSWRyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zuVmlEPTB;ND6wOFM6QSEQvF2= M1\BV3NCVkeHUh?=
SW1990 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTRwMEW5NFgh|ryP NUm0TnJEW0GQR1XS
LK-2 M2jHXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfWU25IUUN3ME20MlEyOjl|IN88US=> M3HxU3NCVkeHUh?=
ES5 M4\C[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfDZ5Q4UUN3ME20MlE{QTh3IN88US=> NF3UZWZUSU6JRWK=
JVM-3 NV2yZ2VGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoOzTWM2OD12LkG4NlIzKM7:TR?= MV\TRW5ITVJ?
RPMI-7951 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkfvTWM2OD12LkKyOFE{KM7:TR?= M4fHfXNCVkeHUh?=
Calu-6 NIqy[WNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPaTWM2OD12LkK3PFgyKM7:TR?= MV;TRW5ITVJ?
LC-2-ad MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{C5VmlEPTB;ND6yPVU3QCEQvF2= NHP4ZpFUSU6JRWK=
SW954 M4f0Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoK2TWM2OD12LkK5OlYh|ryP NHuzS|dUSU6JRWK=
H-EMC-SS M{PXV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfoUJdiUUN3ME20MlMyQDNzIN88US=> MoD5V2FPT0WU
ES3 MojZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmXxTWM2OD12LkO1OFQyKM7:TR?= NIL3VVJUSU6JRWK=
no-11 MnuzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LWVWlEPTB;ND6zOVU2PCEQvF2= MUPTRW5ITVJ?
LAN-6 M{\VOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTRwNEWxPFkh|ryP MV\TRW5ITVJ?
FTC-133 NWD1d4tpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1TOWGlEPTB;ND61N|k2KM7:TR?= MVrTRW5ITVJ?
8505C MoS3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrpTWM2OD12LkW0NlMh|ryP M1;4d3NCVkeHUh?=
SW620 NInQephIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXGeYJKSzVyPUSuOVcxPTdizszN MlewV2FPT0WU
BCPAP MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXr[2VFUUN3ME20MlY{PDhzIN88US=> M2P0ZXNCVkeHUh?=
SK-LU-1 MmrtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1ToRmlEPTB;ND62OlA5QSEQvF2= NHGzXHhUSU6JRWK=
NCI-H1623 NFKwTmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mo[yTWM2OD12LkewNlI5KM7:TR?= MXHTRW5ITVJ?
C2BBe1 MkThS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPSeoo6UUN3ME20Mlc1ODB6IN88US=> M1X3dnNCVkeHUh?=
GP5d MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVrWO2xpUUN3ME20Mlc5Ozh6IN88US=> M4XzfXNCVkeHUh?=
NB6 NUX5ZXFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTRwOE[yNFQh|ryP M2HsVnNCVkeHUh?=
MDA-MB-157 MonYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvNTWM2OD12Lki4O|Yh|ryP Ml\3V2FPT0WU
UMC-11 MoPoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYm0PYxuUUN3ME20Mlg5QTZ2IN88US=> M2jISnNCVkeHUh?=
HCC1419 MnTzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3XKWGlEPTB;ND65NFA3OyEQvF2= M3HYc3NCVkeHUh?=
NCI-H2029 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn\OTWM2OD12Lkm0NVg2KM7:TR?= MmHyV2FPT0WU
LXF-289 NFrvdpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1PtcWlEPTB;NT6wN|cyQSEQvF2= M3LkOHNCVkeHUh?=
KINGS-1 M3S2Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTVwMEe3OFQh|ryP NIf3blVUSU6JRWK=
HD-MY-Z NIjqRo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILDfHFKSzVyPUWuNlM6PjlizszN MmHyV2FPT0WU
ESS-1 NVnQRYJtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTVwMkW1PVch|ryP MmHxV2FPT0WU
GI-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XHZmlEPTB;NT6yO|kzPiEQvF2= MmTlV2FPT0WU
RPMI-2650 NYXZT4RmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTVwM{[xOkDPxE1? MWDTRW5ITVJ?
IA-LM NI\PdnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTVwM{m4O|Eh|ryP MWDTRW5ITVJ?
KP-4 NEDyU|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LnUmlEPTB;NT60OlM{PCEQvF2= NW\0PGNIW0GQR1XS
G-402 NVuxXYFbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWKwWlltUUN3ME21MlUyQDZ3IN88US=> NX\wW|dLW0GQR1XS
OS-RC-2 NH\zXFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVe0dGNrUUN3ME21MlUzPjB2IN88US=> NInTTGlUSU6JRWK=
NCI-H1155 NEX5W5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{H6RWlEPTB;NT61OFk2PSEQvF2= MXnTRW5ITVJ?
OE19 NGfkeJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2XFVGlEPTB;NT62PFYzPCEQvF2= MUnTRW5ITVJ?
U-2-OS NGfyS4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHQbIpWUUN3ME21Mlg6ODF|IN88US=> MX\TRW5ITVJ?
SCC-15 M1rjdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTVwOUO2OlIh|ryP MUTTRW5ITVJ?
NCI-H630 NYfuZZhPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTVwOUm0NFQh|ryP MVTTRW5ITVJ?
PFSK-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTZwMEWyOVkh|ryP NXu0RpBWW0GQR1XS
NCI-H1770 MkjxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTZwMkC4O|Qh|ryP NWPDNGVLW0GQR1XS
SK-MEL-3 NHO0RVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmX0TWM2OD14LkSyPVE2KM7:TR?= M3q0bnNCVkeHUh?=
LB1047-RCC M{jMVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPk[pVKSzVyPU[uOFc3OjVizszN MmS4V2FPT0WU
NCI-H446 NITHSphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTZwNkK5NlUh|ryP Mkf1V2FPT0WU
SW780 MnrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vhbWlEPTB;Nj63NFE5PSEQvF2= MlPUV2FPT0WU
NEC8 NUPlWZI4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkLUTWM2OD14Lke2OlMh|ryP Mo[3V2FPT0WU
NOMO-1 MlzDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLjTWM2OD14Lke4NVEyKM7:TR?= NV3hWGNoW0GQR1XS
COLO-668 NGfCRmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYf3OYM4UUN3ME22Mlg1Ozh5IN88US=> MVzTRW5ITVJ?
MC116 M3fEfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfqNJJKSzVyPU[uPVM5QTdizszN MV7TRW5ITVJ?
HCC1937 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn[3TWM2OD14Lkm5NlUyKM7:TR?= NG\sZ|VUSU6JRWK=
NCI-N87 NGD3SWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzReGpDUUN3ME23MlE6Ojl|IN88US=> MXTTRW5ITVJ?
COLO-320-HSR Mmn4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\pTWM2OD15LkKyO|M5KM7:TR?= MkO0V2FPT0WU
HCC1806 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUW5XlhmUUN3ME23MlI3ODR2IN88US=> NEj1NXJUSU6JRWK=
OVCAR-3 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTdwM{OwN|gh|ryP M33iNXNCVkeHUh?=
NUGC-3 M1\Cfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWfPeZFoUUN3ME23MlM6Pjl2IN88US=> MXTTRW5ITVJ?
SW1783 NEHn[5NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTdwNEOxO|Uh|ryP MlP3V2FPT0WU
GCT Mlq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3rObmlEPTB;Nz61OlkxPiEQvF2= MXLTRW5ITVJ?
NCI-H2126 NHj1NHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVW4S5p{UUN3ME23Mlc{PjJ3IN88US=> MlT5V2FPT0WU
MEL-HO MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoG5TWM2OD15Lke3NFU1KM7:TR?= NITybVlUSU6JRWK=
CAPAN-1 NXrYVpZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{fBe2lEPTB;Nz63O|M2PyEQvF2= NIf2UGpUSU6JRWK=
SW756 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjDTWM2OD15Lke4N|M{KM7:TR?= M2TPTXNCVkeHUh?=
SKG-IIIa NYjRV4lbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mon2TWM2OD15LkixPFkzKM7:TR?= NWXmRYpmW0GQR1XS
HCE-T MlvvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoSwTWM2OD15Lki3O|g{KM7:TR?= MlOwV2FPT0WU
Ca-Ski NHnvWYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY\JR|UxRTdwOUmzPFMh|ryP NIPofWNUSU6JRWK=
COLO-684 M3XRUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRThwMEG4NVgh|ryP M3TibnNCVkeHUh?=
KYSE-70 Mn;kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRThwMEe3Nlkh|ryP Mm\vV2FPT0WU
TI-73 NWfzSVhVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV;JR|UxRThwMkW4OVEh|ryP MoD4V2FPT0WU
BT-20 M3r3V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWmwVnNLUUN3ME24MlI3ODV{IN88US=> MWnTRW5ITVJ?
MHH-ES-1 NV3uOXdQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XxbGlEPTB;OD61NVg{PCEQvF2= NYX0SIxyW0GQR1XS
TE-12 NGfsVWhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvhOHI3UUN3ME24MlU6QTNzIN88US=> NVqxSZl4W0GQR1XS
YH-13 NFq5XGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRThwNkGwNFgh|ryP M3vxbHNCVkeHUh?=
SF126 NGCzU29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXOVJRFUUN3ME24Mlg{QDZ3IN88US=> NXfwOVdDW0GQR1XS
J82 MlvsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIP2dmZKSzVyPUiuPVAxOzhizszN NXzRelRZW0GQR1XS
RCC10RGB NFnZNmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRThwOUm1OlEh|ryP M3\0b3NCVkeHUh?=
SK-UT-1 NFLJVpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTlwMES5OFUh|ryP M1j6SXNCVkeHUh?=
LB2241-RCC NGXMSldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3LtbmlEPTB;OT6xPVE{PyEQvF2= MVfTRW5ITVJ?
LB996-RCC MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrhXnJKSzVyPUmuNVk5QSEQvF2= MmLiV2FPT0WU
EPLC-272H MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUPFOItmUUN3ME25MlM4PjV5IN88US=> M{DJW3NCVkeHUh?=
CTV-1 NIPNT4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHWTWM2OD17LkW2OVMzKM7:TR?= MX7TRW5ITVJ?
HSC-2 MnfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;FbGlEPTB;OT61O|U2KM7:TR?= M{\FSXNCVkeHUh?=
SK-MEL-28 NHrGOnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUXEbW45UUN3ME25MlYyQDl|IN88US=> MXXTRW5ITVJ?
MMAC-SF MkjLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHmyRYNKSzVyPUmuOlg4PSEQvF2= M2\jfnNCVkeHUh?=
CP50-MEL-B MlTDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;ve4oxUUN3ME25Mlc2Pzh{IN88US=> NWfIdox{W0GQR1XS
HT-1080 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7TcHhVUUN3ME25Mlc4PzN7IN88US=> NVXrSodTW0GQR1XS
HEC-1 M2[yeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXKTWM2OD1zMD6zN|UzKM7:TR?= MnLuV2FPT0WU
AGS M1T3VWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGfDZo9KSzVyPUGwMlM4PCEQvF2= M{\QWnNCVkeHUh?=
GAMG MnzjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1;4cGlEPTB;MUCuOVE3OiEQvF2= M{DnVXNCVkeHUh?=
SW48 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37NSGlEPTB;MUCuOVE5QSEQvF2= NGewdFhUSU6JRWK=
U031 M3vYWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoeyTWM2OD1zMD61PVA5KM7:TR?= M1TUO3NCVkeHUh?=
OVCAR-5 MmDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTFyLk[0Nlkh|ryP MXvTRW5ITVJ?
SF295 M1\uV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnaTWM2OD1zMD62O|A1KM7:TR?= MoLwV2FPT0WU
BHT-101 NYnOdYJ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3UdGJKSzVyPUGwMlcyPzdizszN NI\TNWxUSU6JRWK=
VMRC-RCZ NF71bo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7Oe5lrUUN3ME2xNU4{OjBzIN88US=> NHrOSHBUSU6JRWK=
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K5 NGLPT41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2raSGlEPTB;NEWuPVQxPSEQvF2= MWTTRW5ITVJ?
NCI-H358 M2fWPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlHaTWM2OD12Nz6yNVUh|ryP M4WxOnNCVkeHUh?=
NCI-H2030 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY[yVpBXUUN3ME20O{4zOzd2IN88US=> MWDTRW5ITVJ?
SW948 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILkXItKSzVyPUS3MlQ3PCEQvF2= MWnTRW5ITVJ?
BALL-1 M1LBVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\jTWM2OD12Nz62NVY5KM7:TR?= MXLTRW5ITVJ?
TE-9 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkC4TWM2OD12Nz65OVgyKM7:TR?= NIrRbHRUSU6JRWK=
SK-N-FI Mn\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDKTWM2OD12OD6wN|U5KM7:TR?= MkXDV2FPT0WU
KALS-1 NXr6WGg3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvuXmdQUUN3ME20PE4yOjh7IN88US=> MWjTRW5ITVJ?
HO-1-N-1 MkfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTR6Lke0OFUh|ryP M4myO3NCVkeHUh?=
NCI-H2452 NFXP[FJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3u1dGlEPTB;NEmuNVE2OiEQvF2= M2\nZ3NCVkeHUh?=
OC-314 NHX2W|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\LNWtlUUN3ME20PU43QDN2IN88US=> NXHPR4R4W0GQR1XS

... Click to View More Cell Line Experimental Data

In vivo試験 When ABT-263 is administered at 100 mg/kg/day in the H345 xenograft model, significant antitumor efficacy is observed with 80% TGI and 20% of treated tumors indicating at least a 50% reduction in tumor volume. [2] Oral administration of ABT-263 alone causes complete tumor regressions in xenograft models of small-cell lung cancer and acute lymphoblastic leukemia. In xenograft models of aggressive B-cell lymphoma and multiple myeloma where ABT-263 displays modest or no single agent activity, it significantly enhances the efficacy of clinically relevant therapeutic regimens. [2]
臨床試験 ABT-263 is currently in Phase II clinical trial for the treatments of chronic lymphocytic leukemia.
特集

プロトコル (参考用のみ)

キナーゼアッセイ:

[1]

Affinity determination Binding affinities (Ki or IC50) of ABT-263 against different isoforms of Bcl-2 family are determined with competitive fluorescence polarization assays. The following peptide probe/protein pairs are used: f-bad (1 nM) and Bcl-xL (6 nM), f-Bax (1 nM) and Bcl-2 (10 nM), f-Bax (1 nM) and Bcl-w (40 nM), f-Noxa (2 nM) and Mcl-1 (40 nM), and f-Bax (1 nM) and Bcl-2-A1 (15 nM). Binding affinities for Bcl-xL are also determined using a time-resolved fluorescence resonance energy transfer assay. Bcl-xL (1 nM, His tagged) is mixed with 200 nM f-Bak, 1 nM Tb-labeled anti-His antibody, and ABT-263 at room temperature for 30 min. Fluorescence is measured on an Envision plate reader using a 340/35 nm excitation filter and 520/525 (f-Bak) and 495/510 nm (Tb-labeled anti-His antibody) emission filters.

細胞アッセイ:

[1]

細胞株 SCLC cell lines
濃度 0-1 μM
反応時間 48 hours
実験の流れ

Human tumor cell lines SCLC cell lines are maintained at 37 °C containing 5% CO2. SCLC cell lines are cultured in RPMI 1640 with 10% fetal bovine serum (FBS), 1% sodium pyruvate, 25 mM HEPES, 4.5 g/L glucose, and 1% penicillin/streptomycin. Leukemia and lymphoma cell lines are cultured in RPMI 1640 supplemented with 10% FBS and 1% penicillin/streptomycin. Cells (1-5×10 4) are treated by ABT-263 for 48 hours in 96-well culture plates in a final volume of 100 μL and cytotoxicity is assessed with the CellTiter Glo assay. In vitro cyto toxicity of ABT-263 is assayed.

動物実験:

[1]

動物モデル C.B.-17 scid-bg or C.B.-17 scid mice
製剤 Formulated in 10% ethanol, 30% polyethylene glycol 400, and 60% Phosal 50 PG
投薬量 100 mg/kg/d
投与方法 Administered via p.o.

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 ABT-263 (Navitoclax) SDF
分子量 974.61
化学式

C47H55ClF3N5O6S3

CAS No. 923564-51-6
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 100 mg/mL (102.6 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo
* <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 4-​[4-​[[2-​(4-​chlorophenyl)​-​5,​5-​dimethyl-​1-​cyclohexen-​1-​yl]​methyl]​-​1-​piperazinyl]​-​N-​[[4-​[[(1R)​-​3-​(4-​morpholinyl)​-​1-​[(phenylthio)​methyl]​propyl]​amino]​-​3-​[(trifluoromethyl)​sulfonyl]​phenyl]​sulfonyl]​-benzamide

文献中の引用 (36)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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