Tanespimycin (17-AAG)

For research use only. Not for use in humans.

目录号：S1141 别名： CP127374, NSC-330507, KOS 953 中文名称：坦螺旋霉素

Tanespimycin (17-AAG) Chemical Structure

CAS No. 75747-14-7

Tanespimycin (17-AAG, CP127374, NSC-330507, KOS 953) 是一种有效的HSP90抑制剂，无细胞试验中IC50为5 nM，作用于来自肿瘤细胞的HSP90比作用于来自正常细胞HSP90结合亲和力高100倍。Tanespimycin (17-AAG)可诱导细胞凋亡、坏死、自噬和线粒体自噬。Phase 3。

规格

价格

库存

购买数量

10mM (1mL in DMSO)	RMB 2350.91	现货
5mg	RMB 795.18	现货
25mg	RMB 2432.97	现货
100mg	RMB 6527.43	现货
200mg	RMB 10950.03	现货
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客户使用Selleck生产的Tanespimycin (17-AAG)发表文献109篇：

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Blood Cancer J, 2022, 12(3):39

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ACS Appl Mater Interfaces, 2022, 10.1021/acsami.1c22138

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J Cell Mol Med, 2022, 10.1111/jcmm.17210

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Hepatol Commun, 2022, 10.1002/hep4.1928

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SLAS Discov, 2022, 27(3):175-184

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Mol Cell, 2021, 81(6):1170-1186.e10

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EMBO Rep, 2021, e51740

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Elife, 2021, 10e64977

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Cancer Lett, 2021, 512:28-37

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Front Microbiol, 2021, 12:797279

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Mol Ther Nucleic Acids, 2021, 26:208-221

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Int J Mol Sci, 2021, 22(5)2538

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Sci Rep, 2021, 11(1):18003

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Int J Pharm, 2021, 607:120988

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Sci China Life Sci, 2021, 10.1007/s11427-020-1860-2

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Vet Microbiol, 2021, 265:109316

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Cell Rep, 2021, 34(6):108726

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Nat Commun, 2020, 29;11(1):2086

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Cell Rep, 2020, 33(7):108397

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Cancers (Basel), 2020, 7;12(4)

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Mol Cell Biol, 2020, MCB.00473-20

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Mol Cell Biol, 2020,

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Phytomedicine, 2020,

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Eur J Cell Biol, 2020, 100(1):151148

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Drug Des Devel Ther, 2020, 14:4605-4612

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G3 (Bethesda), 2020, 4;10(5):1585-1597

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Mol Cell, 2019, 75(4):823-834

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Nat Commun, 2019, 10(1):5043

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Cell Syst, 2019, 8(2):97-108

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Cell Rep, 2019, 27(11):3331-3344

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Cell Death Dis, 2019, 10(10):737

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Cells, 2019, 8(8)

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Front Cell Dev Biol, 2019, 7:204

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Oxid Med Cell Longev, 2019, 2019:2050183

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J Cell Physiol, 2019, 10.1002/jcp.29283

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Cancer Biol Med, 2019, 16(2):220-233

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Sci Rep, 2019, 9(1):5637

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Int J Biol Sci, 2019, 15(2):312-324

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Toxicol Appl Pharmacol, 2019, 371:63-73

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BMC Cancer, 2019, 19(1):102

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Exp Eye Res, 2019, 189:107821

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Mol Cell Biol, 2019, 39(4)e00375-18

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J Natl Cancer Inst, 2018, 110(4):390-399

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Cell Death Dis, 2018, 9(10):944

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Cell Physiol Biochem, 2018, 47(6):2199-2215

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Mol Cancer Ther, 2018, 17(5):1051-1060

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Mol Oncol, 2018,

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J Cell Biochem, 2018, 10.1002/jcb.27397

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Eur J Med Chem, 2018, 158:548-558

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F1000Res, 2018, 7:1906

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Mycoses, 2018, 61(11):853-856

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EMBO J, 2017, 36(5):646-663

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ACS Photonics, 2017, 5(2):487-494

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Br J Pharmacol, 2017, 174(5):409-423

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Cell Mol Life Sci, 2017, 74(3):543-554

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J Invest Dermatol, 2017, 137(2):341-349

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Mol Cancer Ther, 2017,

PubMed: 28619760 ( click the link to review the publication )

Hum Mol Genet, 2017, 26(22):4465-4480

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Sci Rep, 2017, 7(1):4546

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Toxicol Appl Pharmacol, 2017, 329:282-292

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Am J Transl Res, 2017, 9(11):4945-4953

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Onco Targets Ther, 2017, 10:2219-2226

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SLAS Discov, 2017, 22(5):507-515

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Oncotarget, 2017, 8(38):64651

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Oncotarget, 2017, 8(62):105372-105382

PubMed: 29285257 ( click the link to review the publication )

Medchemcomm, 2017, 8(1):88-95

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Cell, 2017, 170(5):845-859

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Nat Commun, 2016, 7:13122

PubMed: 27959342 ( click the link to review the publication )
Cancer Res, 2016, 76(4):965-73

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Oncogene, 2016, 35(28):3681-91

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Oncogene, 2016, 35(3):333-43

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Oncogene, 2016,

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Oncogene, 2016, 35(29):3854-3865

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Cell Death Dis, 2016, 7:e2089

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Mol Pharm, 2016, 13(11):3724-3735

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Am J Physiol Lung Cell Mol Physiol, 2016, 310(10):L964-74

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Biochem J, 2016, 473(12):1733-44

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Medicinal Chemistry Research, 2016, 10.1007/s00044-016-1553-7

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Oncotarget, 2016, 7(2):1323-40

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Mol Cancer Res, 2015, 13(5):923-33

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Cancer Biol Ther, 2015,

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Oncotarget, 2015, 6(22):19228-45

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Oncotarget, 2015, 6(17):14796-813

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Mol Cancer, 2014, 15:30

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ACS Chem Biol, 2014, 9(10):2237-41

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Exp Gerontol, 2014, 52:55-69

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PLoS One, 2014, 9(10):e111146

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Assay Drug Dev Technol, 2014, 12(9-10):514-26

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Julius Maximilians Universit, 2014, Kumari G

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Mol Cell, 2013, 50(3):368-78

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产品安全说明书

HSP (HSP90)抑制剂选择性比较

生物活性

产品描述

特性

17-AAG对正常细胞的毒性很小。

靶点

HSP90 ^[1]
(Cell-free assay)

5 nM

体外研究

17-AAG是格尔德霉素类似物, 但是与过量表达HER-2的癌细胞 (BT474, N87, SKOV3 和SKBR3)或BT474乳腺细胞衍生的Hsp90亲和力高100多倍，IC50为5-6 nM, 而作用于正常人类原代细胞时，IC50为400-943 nM, 因为肿瘤Hsp90 处于多伴复合体状态，具有高ATP酶活性，而正常细胞Hsp90 处于潜在未结合状态, 且直接与那些细胞中17-AAG毒性相关。^[1]17-AAG 引起HER2, HER3, Akt，突变和野生型雄激素受体(AR)降解，导致前列腺细胞如LNCaP, LAPC-4, DU-145,和PC-3中RB依赖的 G1 期生长停顿，IC50为25-45 nM。^[2]除了诱导改变野生型BCR-ABL的Ba/F3细胞凋亡, IC50为5.2 μM, 17-AAG还通过诱导野生型和突变型 BCR-ABL蛋白降解，而诱导改变抗 Imatinib Mesylate的 T315I和 E255K BCR-ABL突变型细胞生长，IC50分别为2.3 μM 和 1.0 μM。^[3]

Cell Data

Cell Lines	Assay Type	Activity Description	PMID
A549	MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1TqcWlEPTB;MD6wNFA{ODNizszN	MoKzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
IST-MEL1	MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NXnCRnVmUUN3ME2wMlAxODRyNzFOwG0>	MlLiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
NCI-SNU-1	NHvnV4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NEDHOXNKSzVyPUCuNFAzODdizszN	NYXrepcyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
FADU	NF7HWWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MmHzTWM2OD1yLkCwNlA6KM7:TR?=	NF[3PG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK\|5USU6JRWK8M4E,
C32	MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M4LwfmlEPTB;MD6wNFMxPCEQvF2=	MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
D-566MG	NX3G[2tXT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NEXaUHpKSzVyPUCuNFA{QSEQvF2=	NXi2bZFzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
LXF-289	NFewR4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NHP6[2xKSzVyPUCuNFA1OTlizszN	NGPpU5k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK\|5USU6JRWK8M4E,
HGC-27	NHjZfYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NXzWdXhYUUN3ME2wMlAxPTFizszN	MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
RPMI-7951	NUHBb4ZYT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3fKNWlEPTB;MD6wNFcyPyEQvF2=	NFW2fGU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK\|5USU6JRWK8M4E,
HSC-3	M1XNS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M{LGWmlEPTB;MD6wNFkzQSEQvF2=	MoS0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
MIA-PaCa-2	NYixNG9sT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NV;Gd\|dTUUN3ME2wMlAyODB7IN88US=>	M2PIW\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
KS-1	NUm4dJRwT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NXrPXJFQUUN3ME2wMlAyOzV3IN88US=>	MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
CAL-51	NIfLdlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M2HmcWlEPTB;MD6wNVQxPSEQvF2=	M1:2TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
MDA-MB-361	NVvsOJJqT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3fWUGlEPTB;MD6wNVQ6PSEQvF2=	MXi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
TI-73	MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MVPJR\|UxRTBwMEG3PVYh\|ryP	NU\qUZdwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
AGS	MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M3K1OGlEPTB;MD6wNVk{QCEQvF2=	NWjUOFM3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
NCI-H460	MkfKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	Mn7pTWM2OD1yLkCxPVc1KM7:TR?=	MkTZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
A204	M4O1Tmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M1zoUGlEPTB;MD6wNlI1QSEQvF2=	MmfzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
CHL-1	M33RfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M4\ROWlEPTB;MD6wNlI2OSEQvF2=	MlXSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
DU-4475	MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NUDpbWxqUUN3ME2wMlAzOjZzIN88US=>	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
CGTH-W-1	NFTZ[45Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NGO5UWRKSzVyPUCuNFI{PDlizszN	NE[5PHQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK\|5USU6JRWK8M4E,
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IA-LM	NWj0SYRIT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVH2e3VlUUN3ME2yN{4zPDl\|IN88US=>	NIjyfWI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK\|5USU6JRWK8M4E,
SW1463	M3S2[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NVrkXZNvUUN3ME2yN{44QSEQvF2=	MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
JAR	Ml;LS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NXH5PZVyUUN3ME2yOE4{Ojl\|IN88US=>	Mnz2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
HT	NHrSRXFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NFf6XVVKSzVyPUK0MlQ4PTNizszN	MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
LCLC-103H	MnrQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NXfaRXpNUUN3ME2yOE45PDR7IN88US=>	MoC5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
SNU-449	MmLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NXvlTWdRUUN3ME2yOE45PzRzIN88US=>	MoXoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
KE-37	NF\Qd41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NWjpOnV7UUN3ME2yOU4xQTJ6IN88US=>	NF\5T5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK\|5USU6JRWK8M4E,
NCI-H1623	MorDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NFPPeVhKSzVyPUK3MlE{ODNizszN	NXWwPHg{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
MOLT-13	NHHp[IVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M1zoSGlEPTB;MkeuN\|UyPiEQvF2=	Ml[5QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
COLO-741	MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NITIR5dKSzVyPUOxMlM{OzNizszN	NHqwVYM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK\|5USU6JRWK8M4E,
NB6	NEW0[GJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYHJR\|UxRTN{LkK4O\|Yh\|ryP	NU[yS5VLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
MOLT-16	M3O2b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MVfJR\|UxRTN\|LkCwOVUh\|ryP	NYSyZ4FERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
IST-MES1	M3jrOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MnHPTWM2OD1\|ND6wOVQyKM7:TR?=	M2W2RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
A4-Fuk	NVTZSpBrT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MWPJR\|UxRTN3LkC2OkDPxE1?	M{LjUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
CAL-85-1	M3vqXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NF;TOZlKSzVyPUO1MlI5OTdizszN	M1\uNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
CCRF-CEM	NV3Kd\|BJT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NUTPXXF3UUN3ME2zO{4yPTN4IN88US=>	MoexQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
HAL-01	M3zxTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	Mm\PTWM2OD1\|OD60PFg6KM7:TR?=	MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
HEL	MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MVzJR\|UxRTR\|LkO0NFkh\|ryP	MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
EW-1	M1W2WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NWLz[FM3UUN3ME20N{41PzZ6IN88US=>	NYP5NXRmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
MDA-MB-231	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NGXqV4pKSzVyPUS1MlEyQTlizszN	MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
ABC-1	M4riV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MYTJR\|UxRTR4Lki1N\|gh\|ryP	M2XReVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
NCI-H446	MonTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M1XiSmlEPTB;NEiuOVA2QCEQvF2=	NXTSeFMxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
MHH-PREB-1	NXvEfo9LT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MkLrTWM2OD12OT62NFA4KM7:TR?=	M2TIbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
DOHH-2	NFuwbHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NYHrSpF[UUN3ME20PU43PjV4IN88US=>	MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
GCT	M{\zSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MWjJR\|UxRTR7Lk[5O\|Yh\|ryP	MkWyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	LATS1 / p-LATS1 / YAP / CTGF; PubMed: 25712415 J Cell Mol Med Effects of 17-AAG on the expression of LATS1, p-LATS1, YAP and CTGF. The expression levels of YAP and CTGF proteins, indicated by Western blot assay, were down-regulated, while LATS1 was upregulated in a dose-dependent manner in 17-AAG treated groups compared to the untreated group. Cleaved PARP / Survivin; PubMed: 18827603 J Thorac Oncol Western analysis of expression levels of cleaved PARP and Survivin in MM cell lines. β-Actin served as loading control. pAKT / pMAPK / pRb; PubMed: 18682579 Neuro Oncol The phosphorylated states of signaling proteins involved in glioma growth are also affected by 17-AAG treatment. EGFR / PDGFR / AKT / MAPK / c-RAS; PubMed: 18682579 Neuro Oncol 17-AAG promotes the degradation of HSP90 client proteins that are involved in the pathology of glioblastoma multiforme (GBM). Glioma cell lines were treated with increasing concentrations of 17-AAG for 48 h, and protein lysates were run on Western blots. HSP90 client proteins known to be involved in gliomagenesis showed degradation while nonclient proteins remained unaffected by 17-AAG treatment. α-Synuclein / HSP90 / HSP70 / HSP32 / αB-Crystallin; PubMed: 20090920 PLoS One Immunoblot analysis of heat shock protein induction. Cells were treated with 17-AAG (1–200 nM, 24 h), or subjected to heat shock (HS: 44°C, 30 min, 24 h recovery) or to MG-132 (MG: 1 µM, 24 h). Cell lysates were prepared and immunoblot analysis was carried out with antibodies against the individual proteins as indicated on the right. Co, untreated control.	25712415 18827603 18682579 20090920
Immunofluorescence	β-catenin / E-cadherin; PubMed: 25290150 PLoS One Co-localization of β-catenin (Red) and E-cadherin (Green) was observed at the cell-cell junctions (white arrows) both in siCtrl and siCTGF cells after 17-AAG treatment. Scale bar is 20 µm. YAP / TAZ; PubMed: 25290150 PLoS One Reduction in cytoplasmic distribution accompanied by increased nuclear localization of YAP/TAZ was more apparent in cells treated with 45 nM 17-AAG (red channel for YAP/TAZ and blue channel for nucleus). Statistical comparisons were performed using one-way Kruskal-Wallis multiple comparison, ***p<0.001 compared with control (0 nM). STAT3; PubMed: 27279418 Mol Med Rep Effects of 17-AAG on STAT3 expression of H446 cells. (A) Control group; (B) 3.125 mg/l; (C) 6.25 mg/l. 17-AAG, 17-allylamino-17-demethoxygel-danamycin; STAT3, signal transducer and activator of transcription 3; DAPI, 4′,6-diamidino-2-phenylindole.	25290150 27279418
Growth inhibition assay	Cell viability; PubMed: 18682579 Neuro Oncol 17-AAG inhibits the growth of human glioma cell lines. Human glioma cell lines and a nontumorigenic fibroblast cell line were treated with increasing concentrations of 17-AAG for 4 days, and the effect on cell growth was assessed by a 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt (MTS) assay. The 50% inhibitory concentration (IC50) of all glioma cell lines ranged from 0.05 to 0.5 μM 17-AAG, as compared to 1.5 μM for the nontumorigenic cells.	18682579

体内研究

17-AAG作用于携带3T3-src, B16或CT26移植瘤裸鼠，与Hsp90结合具有高亲和力，IC50为8-35 nM，而作用于正常组织时，IC50为200-600 nM。^[1] 17-AAG按50 mg/kg左右剂量处理，引起AR, HER2, HER3, 和 Akt表达明显降低，降低达50%以上，这种作用存在剂量依赖性，结果导致雄激素依赖型 (CWR22)和非依赖型(CWR22R 和CWRSA6) 前列腺移植瘤生长受抑制，抑制率分别为67%, 80%和 68%。^[2]

激酶实验：^[1]	- 合并 Hsp90结合实验: 纯化的Hsp90蛋白或过量表达HER-2的癌细胞(BT474, N87, SKOV3 和 SKBR3) 裂解物或BT474乳腺癌细胞溶于溶解buffer(20 mM HEPES, pH 7.3, 1 mM EDTA, 5 mM MgCl₂, 100 mM KCl) ，与不同浓度17-AAG在4^oC下温育30分钟，然后和生物素-GM链接的BioMag链霉亲和素磁珠在4^oC下温育1小时。试管放置于磁架上,除去未结合的上清液。在溶解buffer中清洗三次磁珠，然后在SDS–PAGE 样本缓冲液中在95^oC下加热5分钟。在SDS蛋白凝胶上进行样本分析,使用特点抗体进行Western Blotting。使用Bio-rad Fluor-S 多重图像测量Western Blot条带，计算抑制Hsp90与生物素-GM结合的百分数。测定IC50。
细胞实验：^[1]	- 合并 Cell lines: BT474, SKBR3, N87, SKOV3, MCF7, MDA468, Hs578T, Hs578Bst, A549, HT29, U87, SKMG3, HT1080, RPTEC, NDF, HMVEC, HMEC, HUVEC, 和 PBMC Concentrations: 溶于DMSO, 终浓度为10 μM 左右 Incubation Time: 5天 Method: 细胞按每孔2000个接种在96孔板上，终培养体积为100 μL，培养24小时，然后加入浓度不断增高的17-AAG，温育5天。使用 Celltiter 96 AQueous 非放射性细胞增殖检测试剂盒测定存活细胞数。测定IC50。 (Only for Reference)
动物实验：^[2]	- 合并 Animal Models: 皮下注射雄激素依赖性CWR22移植瘤的雄性 nu/nu 无胸腺小鼠，皮下注射雄激素非依赖性的CWR22R和CWRSA6移植瘤的雌性nu/nu 无胸腺小鼠。 Dosages: 50 mg/kg 左右 Administration: 腹膜注射 (Only for Reference)

参考文献

溶解度 (25°C)

体外	DMSO	100 mg/mL (170.73 mM)
	Water	Insoluble
	Ethanol	''5 mg/mL
体内	从左到右依次将纯溶剂加入产品，现配现用(数据来自Selleck实验检测而非文献)： 5%DMSO+corn oil	10mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据 Download Tanespimycin (17-AAG) SDF

分子量	585.69
化学式	C₃₁H₄₃N₃O₈
CAS号	75747-14-7
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	CP127374, NSC-330507, KOS 953

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

每只动物给药体积

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % ddH₂O

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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操作手册

如果有其他问题，请给我们留言。

常见问题及建议解决方法

问题 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

HSP (HSP90) Signaling Pathway Map

HSP (HSP90) Inhibitors with Unique Features

选择性强的HSP90抑制剂

NVP-BEP800 : HSP90β-selective, IC50=58 nM.
活性最高的HSP90抑制剂

KW-2478 : HSP90, IC50=3.8 nM.
用于临床的HSP90抑制剂

17-DMAG (Alvespimycin) HCl : Phase II for Kidney Cancer.
最新的HSP90抑制剂

XL888 : ATP-competitive inhibitor of HSP90 with IC50 of 24 nM.

研究领域

产品类型

定制您的化合物库

Tanespimycin (17-AAG)

客户使用Selleck生产的Tanespimycin (17-AAG)发表文献109篇：

产品安全说明书

HSP (HSP90)抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download Tanespimycin (17-AAG) SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2022-01-17)

技术支持

常见问题及建议解决方法

HSP (HSP90) Signaling Pathway Map

HSP (HSP90) Inhibitors with Unique Features

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