Tanespimycin (17-AAG)

製品コード:S1141 別名:CP127374, NSC-330507, KOS 953

For research use only.

Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3.

Tanespimycin (17-AAG)化学構造

CAS No. 75747-14-7

サイズ 価格(税別)
10mM (1mL in DMSO) JPY 43300
JPY 15900
JPY 44700
JPY 116800

代表番号: 03-5615-9297|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(115)

製品安全説明書

HSP (HSP90)阻害剤の選択性比較

相関HSP (HSP90)製品

生物活性

製品説明 Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) is a potent HSP90 inhibitor with IC50 of 5 nM in a cell-free assay, having a 100-fold higher binding affinity for HSP90 derived from tumour cells than HSP90 from normal cells. Tanespimycin (17-AAG) induces apoptosis, necrosis, autophagy and mitophagy. Phase 3.
特性 Displays very low toxicity toward normal cells.
ターゲット
HSP90 [1]
(Cell-free assay)
5 nM
体外試験

17-AAG, an analog of geldanamycin, exhibits greater than 100 times higher binding affinity for Hsp90 derived from HER-2-overexpressing cancer cells (BT474, N87, SKOV3 and SKBR3) or BT474 breast carcinoma cells with IC50 values of 5-6 nM. [1] 17-AAG causes the degradation of HER2, HER3, Akt, and both mutant and wild-type androgen receptor (AR), leading to the RB-dependent G1 growth arrest of prostate cancer cells such as LNCaP, LAPC-4, DU-145, and PC-3 with IC50 values of 25-45 nM. [2] In addition to inducing apoptosis of Ba/F3 cells transformed with wild-type BCR-ABL with an IC50 of 5.2 μM, 17-AAG has the ability to induce apoptosis of cells transformed with imatinib mesylate-resistant T315I and E255K BCR-ABL mutants with IC50 values of 2.3 μM and 1.0 μM, respectively, by inducing the degradation of both wild-type BCR-ABL protein and mutants. [3]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A549 NELZV2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPITWM2OD1yLkCwNFMxOyEQvF2= MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
IST-MEL1 NH;6bpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPwTWM2OD1yLkCwNFQxPyEQvF2= MkfyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
NCI-SNU-1 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljGTWM2OD1yLkCwNlA4KM7:TR?= NWq4TJp4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
FADU Ml;LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYDVXHZqUUN3ME2wMlAxOjB7IN88US=> NInm[Yg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
C32 MknDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mk\5TWM2OD1yLkCwN|A1KM7:TR?= MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
D-566MG MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3GbVg5UUN3ME2wMlAxOzlizszN M1uzSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
LXF-289 NF7iPYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\Yd2lEPTB;MD6wNFQyQSEQvF2= Mn;VQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
HGC-27 M{faV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\6T2lEPTB;MD6wNFUyKM7:TR?= MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
RPMI-7951 M2LUXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1;rcGlEPTB;MD6wNFcyPyEQvF2= M2DMdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
HSC-3 NHrHTYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojtTWM2OD1yLkCwPVI6KM7:TR?= NFnSe3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
MIA-PaCa-2 MmrUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEX1T5dKSzVyPUCuNFExODlizszN NVP3S5c4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
KS-1 MnnJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFrqU5FKSzVyPUCuNFE{PTVizszN NEK1O2k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
CAL-51 NVGzb4VJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlLRTWM2OD1yLkCxOFA2KM7:TR?= NY\ON5dFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
MDA-MB-361 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEWwVW5KSzVyPUCuNFE1QTVizszN NX34eGRQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
TI-73 MkX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX\GU49xUUN3ME2wMlAyPzl4IN88US=> NGTwXFU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
AGS M2Pve2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\kb5p{UUN3ME2wMlAyQTN6IN88US=> NXfZVG9ZRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
NCI-H460 MnPIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTBwMEG5O|Qh|ryP NFT3TGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
A204 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jZbGlEPTB;MD6wNlI1QSEQvF2= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
CHL-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\yUWlEPTB;MD6wNlI2OSEQvF2= MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
DU-4475 M3;wfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXtTWM2OD1yLkCyNlYyKM7:TR?= MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
CGTH-W-1 MlfvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;PT|VUUUN3ME2wMlAzOzR7IN88US=> MoX2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
HCC2218 NInmbItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWnJR|UxRTBwMEK0PVQh|ryP NG\x[|k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
A2780 M1f1bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTBwMEK1N|Eh|ryP NUTIdJh5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
NCI-H720 MnPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml3CTWM2OD1yLkCyOVQ3KM7:TR?= NFHqOoU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
NCI-N87 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTBwMEK1PVMh|ryP NXXBXJRpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
CHP-212 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWnrVnlEUUN3ME2wMlAzPjJ6IN88US=> MlvOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
NCI-H23 NF;wVVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;CZ294UUN3ME2wMlAzPjZ3IN88US=> MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
D-263MG NFjhSGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjNSWxKSzVyPUCuNFI4QDZizszN NGjKZ2Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
ME-180 M{L4W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;G[m1KSzVyPUCuNFI5QTFizszN M{\XNFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
SW982 NYnKPFZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVL2fHYyUUN3ME2wMlAzQTl7IN88US=> NHj5UIY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK|5USU6JRWK8M4E,
OE19 M{TQ[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fOeGlEPTB;MD6wN|A4PyEQvF2= MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
SK-LU-1 NXL5OVV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXn6TlBJUUN3ME2wMlA{ODh{IN88US=> MlGwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
H4 NH;RWotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfrWWRKSzVyPUCuNFMxQSEQvF2= MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
HT-144 Mmm1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XVbmlEPTB;MD6wN|A6OyEQvF2= M3e2[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
SK-UT-1 MkDtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHabI1sUUN3ME2wMlA{OTd6IN88US=> M4q1UVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
D-336MG Mn;xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTBwMEOzNFkh|ryP MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
MDA-MB-175-VII M375V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV7JR|UxRTBwMEOzOVQh|ryP MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
GAMG NF2xUZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlr2TWM2OD1yLkCzOFM2KM7:TR?= M1TMUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
CP50-MEL-B NF3BPFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXT4bGd[UUN3ME2wMlA{PDVizszN NXe5T29xRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
OVCAR-5 M4nG[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M17M[2lEPTB;MD6wN|Q5KM7:TR?= NXPUS|FoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
SK-MES-1 NIfkeohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{OwVmlEPTB;MD6wN|YxPiEQvF2= M2HiV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
VM-CUB-1 NG\SVJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnLWlRbUUN3ME2wMlA{PjV5IN88US=> Mk\IQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
WM-115 NFXOVW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTBwMEO3OlIh|ryP MmnOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
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MDA-MB-231 M{fJOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWjJR|UxRTR3LkGxPVkh|ryP MmDvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
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アッセイ
Methods Test Index PMID
Western blot LATS1 / p-LATS1 / YAP / CTGF ; Cleaved PARP / Survivin ; pAKT / pMAPK / pRb ; EGFR / PDGFR / AKT / MAPK / c-RAS ; α-Synuclein / HSP90 / HSP70 / HSP32 / αB-Crystallin 25712415 18827603 18682579 20090920
Immunofluorescence β-catenin / E-cadherin ; YAP / TAZ ; STAT3 25290150 27279418
Growth inhibition assay Cell viability 18682579
体内試験 17-AAG displays significantly higher binding affinity for Hsp90 from 3T3-src, B16 or CT26 xenografts in nude mice with IC50 values of 8-35 nM as compared with that from the normal tissues with IC50 values of 200-600 nM. [1] Administration of 17-AAG (~50 mg/kg) causes significant decline in AR, HER2, HER3, and Akt expression in a dose-dependent manner with >50% decline at dose of 50 mg/kg, resulting in the dose-dependent inhibition of androgen-dependent (CWR22) and -independent (CWR22R and CWRSA6) prostate cancer xenografts growth by 67%, 80% and 68% at dose of 50 mg/kg, respectively. [2]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
  • Hsp90 binding assays:

    Purified native Hsp90 protein or cell lysates from HER-2-overexpressing cancer cells (BT474, N87, SKOV3 and SKBR3) or BT474 breast carcinoma cells in lysis buffer (20 mM HEPES, pH 7.3, 1 mM EDTA, 5 mM MgCl2, 100 mM KCl) are incubated with various concentrations of 17-AAG for 30 minutes at 4 °C, and then incubated with biotin-GM linked to BioMag streptavidin magnetic beads for 1 hour at 4 °C. Tubes are placed on a magnetic rack, and the unbound supernatant removed. The magnetic beads are washed three times in lysis buffer and heated for 5 minutes at 95 °C in SDS–PAGE sample buffer. Samples are analysed on SDS protein gels, and western blots done using indicated antibodies. Bands in the western blots are quantified using the Bio-rad Fluor-S MultiImager, and the percentage inhibition of binding of Hsp90 to the biotin-GM is calculated. The IC50 reported is the concentration of 17-AAG needed to cause half-maximal inhibition of binding.

細胞試験:[1]
  • 細胞株:BT474, SKBR3, N87, SKOV3, MCF7, MDA468, Hs578T, Hs578Bst, A549, HT29, U87, SKMG3, HT1080, RPTEC, NDF, HMVEC, HMEC, HUVEC, and PBMC cells
  • 濃度: Dissolved in DMSO, final concentrations ~10 μM
  • 反応時間:5 days
  • 実験の流れ:Cells are seeded in 96-well plates at 2,000 cells per well in a final culture volume of 100 μL for 24 hours before the addition of increasing concentrations of 17-AAG that is incubated for 5 days. Viable cell number is determined using the Celltiter 96 AQueous Nonradioactive Cell Proliferation Assay. The value of the background absorbance at 490 nm (A490) of wells not containing cells is subtracted. Percentage of viable cells = (A490 of 17-AAG treated sample/A490 untreated cells) × 100. The IC50 is defined as the concentration that gave rise to 50% viable cell number.
動物試験:[2]
  • 動物モデル:Male nu/nu athymic mice inoculated s.c. with androgen-dependent CWR22 xenograft, and female nu/nu athymic mice inoculated s.c. with androgen-independent xenografts CWR22R and CWRSA6
  • 投薬量:~50 mg/kg
  • 投与方法:Injection i.p.

溶解度 (25°C)

体外

体内

左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
5%DMSO+corn oil
混合させたのち直ちに使用することを推奨します。

10mg/mL

化学情報

分子量 585.69
化学式

C31H43N3O8

CAS No. 75747-14-7
Storage 3年 -20°C
2年 -80°C in solvent
Smiles CC1CC(C(C(C=C(C(C(C=CC=C(C(=O)NC2=CC(=O)C(=C(C1)C2=O)NCC=C)C)OC)OC(=O)N)C)C)O)OC

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00103272 Terminated Drug: tanespimycin|Drug: bortezomib Adult Acute Basophilic Leukemia|Adult Acute Eosinophilic Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult T-cell Leukemia/Lymphoma|Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Mycosis Fungoides/Sezary Syndrome|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Small Intestine Lymphoma|Splenic Marginal Zone Lymphoma|Waldenström Macroglobulinemia National Cancer Institute (NCI) April 2005 Phase 1
NCT00098488 Terminated Drug: tanespimycin|Biological: rituximab B-cell Chronic Lymphocytic Leukemia|Prolymphocytic Leukemia|Refractory Chronic Lymphocytic Leukemia National Cancer Institute (NCI) April 2005 Phase 1
NCT00118248 Completed Drug: tanespimycin Recurrent Thyroid Cancer|Stage IV Follicular Thyroid Cancer|Stage IV Papillary Thyroid Cancer|Thyroid Gland Medullary Carcinoma National Cancer Institute (NCI) December 2004 Phase 2
NCT00098423 Completed Drug: tanespimycin|Drug: cytarabine Accelerated Phase Chronic Myelogenous Leukemia|Adult Acute Basophilic Leukemia|Adult Acute Eosinophilic Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Blastic Phase Chronic Myelogenous Leukemia|Chronic Myelomonocytic Leukemia|de Novo Myelodysplastic Syndromes|Previously Treated Myelodysplastic Syndromes|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Refractory Anemia With Excess Blasts in Transformation|Relapsing Chronic Myelogenous Leukemia|Secondary Acute Myeloid Leukemia|Secondary Myelodysplastic Syndromes National Cancer Institute (NCI) November 2004 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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よくある質問(FAQ)

質問1:
What kind of subtypes does this compound inhibit? HSP90α or HSP90β ?

回答
17-AAG can inhibit both HSP90α and HSP90β, but it is unclear how much are they affected respectively. You should note that Hsp90 derived from tumor cells has a 100-fold higher binding affinity for 17-AAG than that from normal cells according to this paper. http://www.nature.com.ezp-prod1.hul.harvard.edu/nature/journal/v425/n6956/full/nature01913.html

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