Tanespimycin (17-AAG)

Name: Tanespimycin (17-AAG)
Brand: Selleck Chemicals
SKU: S1141
Rating: 5 (84 reviews)

For research use only.

Catalog No.S1141 Synonyms: CP127374, NSC-330507, KOS 953

84 publications

Tanespimycin (17-AAG) Chemical Structure

CAS No. 75747-14-7

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.

Selleck's Tanespimycin (17-AAG) has been cited by 84 publications

Cell, 2019, 36(2):179-193

PubMed: 28162770 ( click the link to review the publication )

Cancer Cell, 2019, 36(2):179-193

PubMed: 31378681 ( click the link to review the publication )

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

PubMed: 33439458 ( click the link to review the publication )

Cell Rep, 2021, 34(6):108726

PubMed: 33567287 ( click the link to review the publication )

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

PubMed: 32350249 ( click the link to review the publication )

Cell Rep, 2020, 33(7):108397

PubMed: 33207204 ( click the link to review the publication )

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

PubMed: 32272809 ( click the link to review the publication )

Mol Cell Biol, 2020,

PubMed: 32868290 ( click the link to review the publication )

Mol Cell Biol, 2020, MCB.00473-20

PubMed: 33139492 ( click the link to review the publication )

Phytomedicine, 2020,

PubMed: 32896707 ( click the link to review the publication )

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

PubMed: 33388604 ( click the link to review the publication )

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

PubMed: 33149557 ( click the link to review the publication )

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

PubMed: 32265286 ( click the link to review the publication )

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

PubMed: 31302001 ( click the link to review the publication )

Nat Commun, 2019, 10(1):5043

PubMed: 31695040 ( click the link to review the publication )

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

PubMed: 30797775 ( click the link to review the publication )

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

PubMed: 31189115 ( click the link to review the publication )

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

PubMed: 31570706 ( click the link to review the publication )

Cells, 2019, 8(8)

PubMed: 31370342 ( click the link to review the publication )

Front Cell Dev Biol, 2019, 7:204

PubMed: 31608279 ( click the link to review the publication )

Oxid Med Cell Longev, 2019, 2019:2050183

PubMed: 31178953 ( click the link to review the publication )

J Cell Physiol, 2019, 10.1002/jcp.29283

PubMed: 31595984 ( click the link to review the publication )

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

PubMed: 31516744 ( click the link to review the publication )

Sci Rep, 2019, 9(1):5637

PubMed: 30948782 ( click the link to review the publication )
Int J Biol Sci, 2019, 15(2):312-324

PubMed: 30745823 ( click the link to review the publication )

Toxicol Appl Pharmacol, 2019, 371:63-73

PubMed: 30953615 ( click the link to review the publication )

BMC Cancer, 2019, 19(1):102

PubMed: 30678647 ( click the link to review the publication )

Exp Eye Res, 2019, 189:107821

PubMed: 31589841 ( click the link to review the publication )

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

PubMed: 30455251 ( click the link to review the publication )

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

PubMed: 29202196 ( click the link to review the publication )

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

PubMed: 30237504 ( click the link to review the publication )

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

PubMed: 29975948 ( click the link to review the publication )

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

PubMed: 29440291 ( click the link to review the publication )

Mol Oncol, 2018,

PubMed: 29797762 ( click the link to review the publication )

J Cell Biochem, 2018, 10.1002/jcb.27397

PubMed: 30378153 ( click the link to review the publication )

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

PubMed: 29998564 ( click the link to review the publication )

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

PubMed: 30243156 ( click the link to review the publication )

F1000Res, 2018, 7:1906

PubMed: 30881689 ( click the link to review the publication )

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

PubMed: 28093501 ( click the link to review the publication )

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

PubMed: 29805987 ( click the link to review the publication )

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

PubMed: 28052321 ( click the link to review the publication )

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

PubMed: 27592300 ( click the link to review the publication )

Mol Cancer Ther, 2017,

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

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

PubMed: 28973376 ( click the link to review the publication )

Sci Rep, 2017, 7(1):4546

PubMed: 28674407 ( click the link to review the publication )

Toxicol Appl Pharmacol, 2017, 329:282-292

PubMed: 28624441 ( click the link to review the publication )

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

PubMed: 29218092 ( click the link to review the publication )

Onco Targets Ther, 2017, 10:2219-2226

PubMed: 28458565 ( click the link to review the publication )
SLAS Discov, 2017, 22(5):507-515

PubMed: 28324660 ( click the link to review the publication )

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

PubMed: 28823557 ( click the link to review the publication )

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

PubMed: 28670440 ( click the link to review the publication )

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

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

Nat Commun, 2016, 7:13122

PubMed: 27959342 ( click the link to review the publication )

Cancer Res, 2016, 76(4):965-73

PubMed: 26676744 ( click the link to review the publication )

Oncogene, 2016,

PubMed: 26804171 ( click the link to review the publication )

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

PubMed: 26657151 ( click the link to review the publication )

Cell Death Dis, 2016, 7:e2089

PubMed: 26866270 ( click the link to review the publication )

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

PubMed: 27653969 ( click the link to review the publication )

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

PubMed: 27059856 ( click the link to review the publication )

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

PubMed: ( click the link to review the publication )

Stem Cells, 2015, 33(9):2738-47

PubMed: 26077647 ( click the link to review the publication )

Cancer Biol Ther, 2015,

PubMed: 25692408 ( click the link to review the publication )

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

PubMed: 26142707 ( click the link to review the publication )

Oncotarget, 2015, 51: S659-S660

PubMed: ( click the link to review the publication )

Mol Cancer, 2014, 15:30

PubMed: 24927996 ( click the link to review the publication )

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

PubMed: 25140805 ( click the link to review the publication )

Exp Gerontol, 2014, 52:55-69

PubMed: 24486130 ( click the link to review the publication )

PLoS One, 2014, 9(10):e111146

PubMed: 25343454 ( click the link to review the publication )

Insect Mol Biol, 2014, 23(6):720-32

PubMed: 25060629 ( click the link to review the publication )

Julius Maximilians Universit, 2014, Kumari G

PubMed: ( click the link to review the publication )

Oncotarget, 2014, 5(12):4269-82

PubMed: 24962213 ( click the link to review the publication )

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

PubMed: 25506801 ( click the link to review the publication )
Mol Cell, 2013, 50(3):368-78

PubMed: 23583076 ( click the link to review the publication )

Biochim Biophys Acta, 2013, 1830(11):5184-92

PubMed: 23850472 ( click the link to review the publication )

Mol Cell Biol, 2013, 33(12):2375-87

PubMed: 23572559 ( click the link to review the publication )

Am J Respir Cell Mol Biol, 2013, 10.1165/rcmb.2013-0214OC

PubMed: 24303801 ( click the link to review the publication )

Sci Transl Med, 2012, 4(120):120ra17

PubMed: 22277784 ( click the link to review the publication )

J Exp Med, 2012, 209(2):259-73

PubMed: 22271575 ( click the link to review the publication )

Biochim Biophys Acta, 2012, 1823(4):911-9

PubMed: 22306003 ( click the link to review the publication )

J Biol Chem, 2012, 287(53):44109-20

PubMed: 23144451 ( click the link to review the publication )

Eukaryot Cell, 2012, 11(11):1324-32

PubMed: 22822234 ( click the link to review the publication )

Age (Dordr), 2012, 35(3):549-62

PubMed: 22252435 ( click the link to review the publication )

P Natl Acad Sci USA, 2011, 108(18):7535-40

PubMed: 21502504 ( click the link to review the publication )

J Nat Prod, 2011, 74(6):1491-9

PubMed: 21553813 ( click the link to review the publication )

Purity & Quality Control

Choose Selective HSP (HSP90) Inhibitors

Biological Activity

Description

Features

Displays very low toxicity toward normal cells.

Targets

HSP90 ^[1]
(Cell-free assay)

5 nM

In vitro

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]

Cell Data

Cell Lines	Assay Type	Activity Description	PMID
A549	NUfMd4ZFT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M4HybWlEPTB;MD6wNFA{ODNizszN	NIjJbWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK\|5USU6JRWK8M4E,
IST-MEL1	MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MnG3TWM2OD1yLkCwNFQxPyEQvF2=	NHH3V2w9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK\|5USU6JRWK8M4E,
NCI-SNU-1	M2nsXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M4La[GlEPTB;MD6wNFIxPyEQvF2=	NYK0W\|hORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
FADU	NWDTTGtPT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MXzJR\|UxRTBwMECyNFkh\|ryP	M4H4O\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
C32	MlHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NGXycVlKSzVyPUCuNFA{ODRizszN	NYXxVpZqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
D-566MG	MlH1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NWe4NoNxUUN3ME2wMlAxOzlizszN	M3;6elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
LXF-289	NVS2[XFRT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NXLYPZN6UUN3ME2wMlAxPDF7IN88US=>	NIfCTJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK\|5USU6JRWK8M4E,
HGC-27	MomxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MUPJR\|UxRTBwMEC1NUDPxE1?	MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
RPMI-7951	NGjhcGNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	M4faVWlEPTB;MD6wNFcyPyEQvF2=	NF\UU2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK\|5USU6JRWK8M4E,
HSC-3	NHLKc5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MULJR\|UxRTBwMEC5Nlkh\|ryP	M3fKfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
MIA-PaCa-2	NVzyc3Y1T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NGL4RopKSzVyPUCuNFExODlizszN	Ml21QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
KS-1	NXjBUpRbT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MlvRTWM2OD1yLkCxN\|U2KM7:TR?=	NWHaeItqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
CAL-51	MoeyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NXfzZXFEUUN3ME2wMlAyPDB3IN88US=>	NV;3eIdwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
MDA-MB-361	MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NWPtVJZsUUN3ME2wMlAyPDl3IN88US=>	NF65ZoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK\|5USU6JRWK8M4E,
TI-73	MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M1iwb2lEPTB;MD6wNVc6PiEQvF2=	MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
AGS	M{PibWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MnK3TWM2OD1yLkCxPVM5KM7:TR?=	MoTnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
NCI-H460	MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	NHfqUHJKSzVyPUCuNFE6PzRizszN	M3jwWlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
A204	M{\jSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NH\ZfXZKSzVyPUCuNFIzPDlizszN	M4S3ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
CHL-1	M4r3N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M4[wU2lEPTB;MD6wNlI2OSEQvF2=	NGL1R3Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK\|5USU6JRWK8M4E,
DU-4475	NFToZ5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MWLJR\|UxRTBwMEKyOlEh\|ryP	MlrCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
CGTH-W-1	M4njdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NIfzWGJKSzVyPUCuNFI{PDlizszN	Mn\UQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
HCC2218	MlrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NWjPSZVUUUN3ME2wMlAzPDl2IN88US=>	M2nZTFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
A2780	MlHhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MlzqTWM2OD1yLkCyOVMyKM7:TR?=	MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
NCI-H720	NXGySmlPT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NIexXWVKSzVyPUCuNFI2PDZizszN	MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
NCI-N87	NEXK[YNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MnvUTWM2OD1yLkCyOVk{KM7:TR?=	MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
CHP-212	M4Lrdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NHPNSYNKSzVyPUCuNFI3OjhizszN	M3;YbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
NCI-H23	NGLwd5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MV7JR\|UxRTBwMEK2OlUh\|ryP	NHrZ[HU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK\|5USU6JRWK8M4E,
D-263MG	MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MXzJR\|UxRTBwMEK3PFYh\|ryP	MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
ME-180	NV:ybYNnT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NFjGVWlKSzVyPUCuNFI5QTFizszN	NV;NTWQ6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
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Ramos-2G6-4C10	M3iz[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NWTxfVVLUUN3ME2xOU4xPThzIN88US=>	M17lU\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
NCI-H2342	NFPuNoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Mk\xTWM2OD1zNT6yNFQ1KM7:TR?=	M4LGNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
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RPMI-8866	MmHXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NGfuWY9KSzVyPUG2Mlg1QTZizszN	M4XJXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
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KYSE-140	NU\NcJVKT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVX0T3E3UUN3ME2xO{4zODJ6IN88US=>	NF;UN3g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK\|5USU6JRWK8M4E,
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BALL-1	NVPIO4M5T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NE\aRXhKSzVyPUG5MlM{QTlizszN	M17RR\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
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MOLT-13	MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MWTJR\|UxRTJ5LkO1NVYh\|ryP	NXi2dWx6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
COLO-741	M37tdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	M{DrPWlEPTB;M{GuN\|M{OyEQvF2=	MkHqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
NB6	MkGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	M2PrPGlEPTB;M{KuNlg4PiEQvF2=	M1XoT\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
MOLT-16	NEe2VpBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NE[3UHlKSzVyPUOzMlAxPTVizszN	M3;ZUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
IST-MES1	NWnzRZUxT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M4Pmb2lEPTB;M{SuNFU1OSEQvF2=	NYj1dZdYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
A4-Fuk	M1HZcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MoX0TWM2OD1\|NT6wOlYh\|ryP	NVnGWHZWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
CAL-85-1	NXnrcpR3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M{HwcGlEPTB;M{WuNlgyPyEQvF2=	NIDvTVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK\|5USU6JRWK8M4E,
CCRF-CEM	MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	M3nLOWlEPTB;M{euNVU{PiEQvF2=	NI\3Z489[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK\|5USU6JRWK8M4E,
HAL-01	NH\GTGRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MYDJR\|UxRTN6LkS4PFkh\|ryP	NHKwPGo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK\|5USU6JRWK8M4E,
HEL	NEK1XotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MnH1TWM2OD12Mz6zOFA6KM7:TR?=	NWHmcppTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
EW-1	MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?	MWXJR\|UxRTR\|LkS3Olgh\|ryP	Ml7rQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>
MDA-MB-231	Mne0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	NXPIWIpvUUN3ME20OU4yOTl7IN88US=>	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:5d4eu[YJqNmGlLoXrM4Np\W2kbD;jc41xd3WwZG;y[ZBwenShY3Hy[E9EUEWPQlyxNFk1QDBxJ{7TRW5ITVJ:L3G+
ABC-1	NEHufW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	MkTJTWM2OD12Nj64OVM5KM7:TR?=	M3HJdFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFExQTR6MD:nQnNCVkeHUkyvZV4>
NCI-H446	NUPGd41HT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	MmTvTWM2OD12OD61NFU5KM7:TR?=	NG\OPFA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;3e5cv\WKrLnHjMpVsN2OqZX3icE9kd22yb4Xu[H9z\XCxcoTfZ4Fz\C:FSFXNRmwyODl2OECvK\|5USU6JRWK8M4E,
MHH-PREB-1	NETE[XlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	NFXkdllKSzVyPUS5MlYxODdizszN	NX;oblhIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
DOHH-2	NIrjcVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?=	Mm[1TWM2OD12OT62OlU3KM7:TR?=	NUTaS4RzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:ve5d4NmWkaT7hZ{52cy:laHXtZoww[2:vcH;1coRgemWyb4L0Y4NiemRxQ1jFUWJNOTB7NEiwM{c,W0GQR1XSQE9iRg>?
GCT	NWfWSGNKT3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	NVHM[Yd7UUN3ME20PU43QTd4IN88US=>	MlXkQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xd4f3MoVjcS6jYz71b{9kcGWvYnyvZ49ueG:3bnTfdoVxd3K2X3PhdoQwS0iHTVLMNVA6PDhyLze+V2FPT0WUPD;hQi=>

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	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. 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. pAKT / pMAPK / pRb; PubMed: 18682579 Neuro Oncol The phosphorylated states of signaling proteins involved in glioma growth are also affected by 17-AAG treatment. 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. 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.	20090920 18682579 18827603 25712415
Immunofluorescence	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. 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). 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.	27279418 25290150
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

In vivo

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]

Protocol

Kinase Assay:^[1]	- Collapse 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.
Cell Research:^[1]	- Collapse Cell lines: BT474, SKBR3, N87, SKOV3, MCF7, MDA468, Hs578T, Hs578Bst, A549, HT29, U87, SKMG3, HT1080, RPTEC, NDF, HMVEC, HMEC, HUVEC, and PBMC cells Concentrations: Dissolved in DMSO, final concentrations ~10 μM Incubation Time: 5 days Method: 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. (Only for Reference)
Animal Research:^[2]	- Collapse Animal Models: 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 Dosages: ~50 mg/kg Administration: Injection i.p. (Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	100 mg/mL (170.73 mM)
	Water	Insoluble
	Ethanol	''5 mg/mL
In vivo	Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 5%DMSO+corn oil For best results, use promptly after mixing.	10mg/mL

* 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.

Chemical Information Download Tanespimycin (17-AAG) SDF

Molecular Weight	585.69
Formula	C₃₁H₄₃N₃O₈
CAS No.	75747-14-7
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	CP127374, NSC-330507, KOS 953
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

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Working concentration： mg/ml；

Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2021-01-06)

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

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Frequently Asked Questions

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

Selective HSP90 Inhibitor

NVP-BEP800 : HSP90β-selective, IC50=58 nM.
Most Potent HSP90 Inhibitor

KW-2478 : HSP90, IC50=3.8 nM.
HSP90 Inhibitor in Clinical Trial

17-DMAG (Alvespimycin) HCl : Phase II for Kidney Cancer.
Newest HSP90 Inhibitor

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

Related HSP (HSP90) Products

PU-H71 ^New

PU-H71 (NSC 750424) is a potent and selective inhibitor of HSP90 with IC50 of 51 nM. Phase 1.
KNK437 ^New

KNK437 is a pan-HSP inhibitor, which inhibits the synthesis of inducible HSPs, including HSP105, HSP72, and HSP40.
VER155008 ^New

VER155008 (C07) is a potent Hsp70 family inhibitor with IC50 of 0.5 μM, 2.6 μM, and 2.6 μM in cell-free assays for HSP70, HSC70, and GRP78 (HSPA5, Bip), respectively, >100-fold selectivity over HSP90. VER155008 inhibits autophagy and causes reduced levels of HSP90 client proteins.
Luminespib (NVP-AUY922)

Luminespib (AUY-922, NVP-AUY922, VER-52296) is a highly potent HSP90 inhibitor for HSP90α/β with IC50 of 13 nM /21 nM in cell-free assays, weaker potency against the HSP90 family members GRP94 and TRAP-1, exhibits the tightest binding of any small-molecule HSP90 ligand. Luminespib (AUY-922, NVP-AUY922) effectively downregulates and destabilizes the IGF-1Rβ protein and results in growth inhibition, autophagy and apoptosis. Phase 2.
Ganetespib (STA-9090)

Ganetespib (STA-9090) is an HSP90 inhibitor with IC50 of 4 nM in OSA 8 cells, induces apoptosis of OSA cells while normal osteoblasts are not affected; active metabolite of STA-1474. Phase 3.
Alvespimycin (17-DMAG) HCl

Alvespimycin (17-DMAG, NSC 707545, BMS 826476, KOS 1022) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. Phase 2.

Features:A synthetic derivative Geldanamycin, with lower hepatotoxicity than parent antibiotic & higher potency and bioavailability than the similar derivative 17-AAG.
Geldanamycin

Geldanamycin (NSC 122750) is a natural existing HSP90 inhibitor with K_d of 1.2 μM, specifically disrupts glucocorticoid receptor (GR)/HSP association. Geldanamycin attenuates virus infection-induced ALI (acute lung injury)/ARDS (acute respiratory distress syndrome) by reducing the host's inflammatory responses.
HSP990 (NVP-HSP990)

HSP990 (NVP-HSP990) is a novel, potent and selective HSP90 inhibitor for HSP90α/β with IC50 of 0.6 nM/0.8 nM. NVP-HSP990 induces cell cycle arrest and apoptosis.

Features:NVP-HSP990 is an orally available HSP90 inhibitor and is structurally distinct from other clinical HSP90 inhibitors.
Elesclomol (STA-4783)

Elesclomol (STA-4783) is a novel potent oxidative stress inducer that elicits pro-apoptosis events among tumor cells. Phase 3.
Onalespib (AT13387)

Onalespib (AT13387) is a selective potent Hsp90 inhibitor with IC50 of 18 nM in A375 cells, displays a long duration of anti-tumor activity. Phase 2.

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Tanespimycin (17-AAG)