Alvespimycin (17-DMAG) HCl

Catalog No.S1142 Synonyms: NSC 707545,BMS 826476 HCl,KOS 1022

Alvespimycin (17-DMAG) HCl Chemical Structure

Molecular Weight(MW): 653.21

Alvespimycin (17-DMAG) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. Phase 2.

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Cited by 21 Publications

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Biological Activity

Description Alvespimycin (17-DMAG) 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.
Targets
HSP90 [1]
(Cell-free assay)
62 nM
In vitro

17-DMAG displays ~2 times potency against human Hsp90 than 17-AAG, with IC50 of 62 nM versus 119 nM. In SKBR3 and SKOV3 cells which over-express Hsp90 client protein Her2, 17-DMAG causes down-regulation of Her2 with EC50 of 8 nM and 46 nM, respectively, as well as induction of Hsp70 with EC50 of 4 nM and 14 nM, respectively, leading to significant cytotoxicity with GI50 of 29 nM and 32 nM, respectively, consistent with Hsp90 inhibition. [1] 17-DMAG in combination with vorinostat synergistically induces apoptosis of the cultured MCL cells as well as primary MCL cells, more potently than either agent alone, by markedly attenuating the levels of cyclin D1 and CDK4, as well as of c-Myc, c-RAF and Akt. [3] In contrast to 17-AAG which is only active for IKKβ in chronic lymphocytic leukemia (CLL) cells, 17-DMAG treatment effectively leads to depletion of the Hsp90 client protein, resulting in diminished NF-κB p50/p65 DNA binding, decreased NF-κB target gene transcription, and caspase-dependent apoptosis. By targeting the NF-κB family, 17-DMAG selectively mediates dose- and time-dependent cytotoxicity against CLL cells, but not normal T cells or NK cells important for immune surveillance. [5]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human A2058 cells MXTDfZRwfG:6aXRCpIF{e2G7 Mk\tR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRVIxPThiY3XscJMh[nliTWTUJIF{e2G7LDDJR|UxRTJwMTDuUS=> MUOxPFkzQTR6Nh?=
human AGS cells NFn1O29HfW6ldHnvckBie3OjeR?= NVe0ZopbUW6qaXLpeIlwdiCxZjDofZBwgGmjLXnu[JVk\WRiSFnGNUBi[3SrdnH0bY9vKGmwIHj1cYFvKEGJUzDj[YxteyCkeTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBKSzVyPUOuOkBvVQ>? M1jkWVE5OzV7NkOx
SKBR3 cells M2nFWmZ2dmO2aX;uJIF{e2G7 MXjVdJJm\3WuYYTpc44hd2ZiSIPwO|AhcW5iU1vCVlMh[2WubIOsJGVEPTB;NDDuUS=> M{S0OFE3QDV2ME[2
human MDA-MB-231 cells M3\Z[WZ2dmO2aX;uJIF{e2G7 NUTwZVNuUW6qaXLpeIlwdiCxZjDId5A6OCCrbjDoeY1idiCPRFGtUWIuOjNzIHPlcIx{KGG|c3Xzd4VlKGG|IHjldlIh\GWpcnHkZZRqd25uIFnDOVA:PC53IH7N MkLxNVg6Ojl2OE[=
human MDA-MB-231 cells NHj2VlREgXSxdH;4bYPDqGG|c3H5 MmKxR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUWRCNU2ELUKzNUBk\WyuczDifUBOXFRiYYPzZZktKEmFNUC9OU45KG6P M3PVflE5QTJ7NEi2
human A2058 cells NIO4SJJHfW6ldHnvckBie3OjeR?= M{C5cWlvcGmkaYTpc44hd2ZiSIPwPVAhcW5iaIXtZY4hSTJyNUigZ4VtdHNuIFXDOVA:Py57IH7N NWPYOZZGOTh7Mkm0PFY>
SKOV3 cells NW\uS5ZNTnWwY4Tpc44h[XO|YYm= NUCwb4dzXXC{ZXf1cIF1cW:wIH;mJGh{eDdyIHnuJHNMV1Z|IHPlcIx{NCCHQ{WwQVE1KG6P NYT3PYVuOTZ6NUSwOlY>
SKBr3 cells MVHDfZRwfG:6aXRCpIF{e2G7 NHv0[I9EgXSxdH;4bYNqfHliYXfhbY5{fCCVS1LyN{Bk\WyuczygTWM2OD1{NDDuUS=> M3vqOlE3OTZ3M{W0
human AGS cells NECwW49HfW6ldHnvckBie3OjeR?= M{DuUFE3KGh? Mn31TY5pcWKrdHnvckBw\iCKSV[xJIFkfGm4YYTpc44hcW5iaIXtZY4hSUeVIHPlcIx{KGG|c3Xzd4VlKGG|IHnubIljcXSrb36gc4YhcHmyb4jpZU1qdmS3Y3XkJIx2[2moZYLhd4Uh\XiycnXzd4lwdiCjZoTldkAyPiCqcoOgZpkhemWyb4L0[ZIh[XO|YYmsJGlEPTB;M{[gcm0> M2rYelE4PTh|OUWw
human HCT116 cells M1PFPWN6fG:2b4jpZ:Kh[XO|YYm= MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[nliQXzhcYFzKGKudXWgZZN{[XluIFnDOVA:PTBibl2= NWP5WW1NOjB4NkK1N|Q>
human Hep3B cells NG\SNpRHfW6ldHnvckBie3OjeR?= NICz[VIyOiCq NFTj[HdKdmirYnn0bY9vKG:oIHj5dI95cWFvaX7keYNm\CCKSV[xZYxxcGFicILveIVqdiCjY3P1cZVt[XSrb36gbY4hcHWvYX6gTIVxO0JiY3XscJMhfHKnYYTl[EBnd3JiM{CgcYlveyCvZXHzeZJm\CCjZoTldkAyOiCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m|LDDJR|UxRTV5IH7N MYWyNFQ3QTh6Nx?=
human A549 cells MknaR5l1d3SxeHnjxsBie3OjeR?= M1P0ZVczKGh? M2K2TmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[W[2ZYKgO|IhcHK|IHL5JINmdGy2aYTldk1odG9iYYPzZZktKEmFNUC9Olghdk1? NETPfnEyQTRyNUWyPC=>
human MCF7 cells MVTDfZRwfG:6aXRCpIF{e2G7 M2m5OlczKGh? NV\GVXdNS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCjZoTldkA4OiCqcoOsJGlEPTB;N{Ggcm0> MWWxPVI{OTh4NB?=
human NCI-H1299 cells MluzSpVv[3Srb36gZZN{[Xl? MWnJcohq[mm2aX;uJI9nKGi3bXHuJGhUWDlyIHnuJIh2dWGwIF7DTU1JOTJ7OTDj[YxteyCjc4Pld5Nm\CCjczDBb5Qh\GWpcnHkZZRqd25iYX\0[ZIhOjRiaILzJIJ6KGy3bXnu[Zgh[XO|YYmsJGlEPTB;MD6xJO69VQ>? MmLmNlE1Ozh3NEG=
human HeLa cells NH3XVI9HfW6ldHnvckBie3OjeR?= NXvvN4cyUW6qaXLpeIlwdiCxZjDUUmYu[WyyaHGtbY5lfWOnZDDOSk1s[XCyYVKgZYN1cX[jdHnvckBqdiCqdX3hckBJ\UyjIHPlcIx{NCCLQ{WwQVAvOTVizszN NHu4XWkyQDN3OU[zNS=>
human A231 cells MUjQdo9tcW[ncnH0bY9vKGG|c3H5 M2DJNVQ5KGh? MX\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF{M{GgZ4VtdHNiYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjF5IN88US=> M3r1dVI1PzZ|Mk[x
human CCRF-CEM cells NHvzd3hEgXSxdH;4bYPDqGG|c3H5 NV3sbZA3PzJiaB?= NV7RcYM{S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hS0OURj3DSW0h[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IHPlcIx1cXSncj25OkBieXWnb4XzJI9v\SC|b3z1eIlwdiCjc4PhfUwhUUN3ME2wMlU1KM7:TR?= MWqxPVQxPTV{OB?=
human NCI-H596 cells MX3DfZRwfG:6aXRCpIF{e2G7 NXTNb5ZlPzJiaB?= MXTDfZRwfG:6aXPpeJkh[WejaX7zeEBPWTBzLXTl[olkcWWwdDDoeY1idiCQQ1mtTFU6PiClZXzsd{Bi\nSncjC3NkBpenNuIFnDOVA:OS5zIN88US=> NHjDTnEyQTJ|MUi2OC=>
human HCT116 cells NFvQ[XdRem:uaX\ldoF1cW:wIHHzd4F6 NH\hcGw1QCCq M{n4U2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MT6yNUDPxE1? M3K2UlI1PzZ|Mk[x
human MDA468 cells NX\tdFJGS3m2b4TvfIlkyqCjc4PhfS=> NFHTTJU4OiCq NWO1NWN7S3m2b4TvfIlkcXS7IHHnZYlve3RiTmGwNU1l\W[rY3nlcpQhcHWvYX6gUWRCPDZ6IHPlcIx{KGGodHXyJFczKGi{czygTWM2OD1zLk[g{txO MXmxPVI{OTh4NB?=
human AGS cells M1H3bGN6fG:2b4jpZ:Kh[XO|YYm= MWPDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBS3Mh[2WubIOgZpkhVVSWIHHzd4F6NCCLQ{WwQVE3KM7:TR?= NVTZZoQ{OTh|NUm2N|E>
human LN229-Lux cells M1\IcWZ2dmO2aX;uJIF{e2G7 MVWyMlUuOTBizszN MWOxJIg> NVrZcYFpUW6qaXLpeIlwdiCxZjDseYNq\mW{YYPlJIFkfGm4aYT5JIlvKGi3bXHuJGxPOjJ7LVz1fEBk\WyuczDheEAzNjVidH:gNVAhfU1iaX7jeYJifGWmIH\vdkAyKGi{IIXu[IVzKG6xcn3vfIliKG[xbHzve4VlKGK7IEK0JIhzeyC3bnTldkBpgXCxeHnhJIJ6KHKncH;yeIVzKGenbnWgZZN{[Xl? M13tUVIzPzR4Mke0
human NCI-H1299 cells MoHGSpVv[3Srb36gZZN{[Xl? NXXOZnl2OTJiaB?= NGfVRZJT\WS3Y4Tpc44hcW5ib4j5[4VvKGOxboP1cZB1cW:wIILheIUhcW5iaIXtZY4hVkOLLVixNlk6KGOnbHzzJIlv[3WkYYTl[EBnd3JiMUKgbJJ{ NFjGRXgzPTN6M{mxOS=>
human NCI-H526 cells MkXsSpVv[3Srb36gZZN{[Xl? MofINUDPxE1? M1KwW|I1KGh? MUfCbY5lcW6pIHHm[olvcXS7IITvJGhUWDlyIHnuJIh2dWGwIF7DTU1JPTJ4IHPlcIx{KGG2IEGgeW0h[W[2ZYKgNlQhcHK|IHL5JIZtfW:{ZYPj[Y5k\SCyb3zhdol7[XSrb36gZZN{[Xl? Mn3JNVc3ODN3NEC=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
HSP90 / HSP70 ; 

PubMed: 28915605     


Western blot analysis showing dose-dependent elevation of Hsp70 and HSP90 levels in AGS cells by 17-DMAG.

p-Akt / Survivin / MMP2 ; 

PubMed: 28915605     


Western blot analysis showing the dose-dependent reduction of the expression of HSP90 client proteins, such as p-Akt, survivin, and MMP2 by 17-DMAG.

PARP / Cleaved caspase-3 / Cleaved caspase-8 / Cleaved caspase-9 / PUMA ; 

PubMed: 28915605     


(C-D) 17-DMAG effects on the expression of apoptotic proteins (PARP, c-caspase 3, c-caspase-8, c-caspase-9, and PUMA) in AGS cells. Western blot analyses indicate that 17-DMAG significantly increased the expression of apoptotic proteins in AGS cells in a dose- (C) and time- (D) dependent manner (P < 0.05).

p-ALK / ALK / p-Akt / Akt / p-ERK / ERK ; 

PubMed: 26219569     


Modulation of ALK signaling in parental and 17-DMAG-resistant cells. Cells were treated with the indicated concentrations of 17-DMAG or AUY922 for 6 h. The molecules of ALK-related signaling activity were detected by western blot analysis.

α-Tax / α-IKKα / α-IKKβ/ α-NEMO / α-TBK1 / α-p65 / α-p50 ; 

PubMed: 24109220     


C8166, MT-2, and MT-4 cells were treated with 17-DMAG as indicated, and cell lysates were subjected to immunoblotting with the indicated antibodies.

28915605 26219569 24109220
Growth inhibition assay
Cell proliferation ; 

PubMed: 28915605     


Proliferation assay of AGS cells treated with graded concentrations of 17-DMAG for 24 h or 48 h. 17-DMAG resulted in significant dose- and time-dependent reduction of AGS cell proliferation (P < 0.05)

28915605
In vivo 17-DMAG treatment at 5 mg/kg or 25 mg/kg thrice per week significantly reduces tumor growth of TMK-1 xenografts, by significantly reducing vessel area and numbers of proliferating tumor cells in sections. [2] Consistent the inhibition of FAK signaling in vivo, 17-DMAG treatment at 25 mg/kg three times a week significantly suppresses tumor growth, and metastasis of ME180 and SiHa xenografts in mice. [4] Administration of 17-DMAG at 10 mg/kg for 16 days significantly decreases the white blood cell count and prolongs the survival in a TCL1-SCID transplant mouse model. [5]

Protocol

Kinase Assay:[1]
+ Expand

Fluorescence polarization (FP)-based competition binding assay:

This assay utilizes a boron difluoride dipyrromethene (BODIPY) labeled geldanamycin analogue (BODIPY-AG) as a probe and measured fluorescence polarization upon binding of the probe to a protein. Native human Hsp90 protein (α + β isoforms) is isolated from HeLa cells. BODIPY-AG solution is freshly prepared in FP assay buffer (20 mM HEPES-KOH, pH 7.3, 1.0 mM EDTA, 100 mM KCl, 5.0 mM MgCl2, 0.01% NP-40, 0.1 mg/mL fresh bovine γ-globulin (BGG), 1.0 mM fresh DTT, and protease inhibitor from stock solution in DMSO. Competition curves are obtained by mixing 10 μL each of a solution containing BODIPY-AG and Hsp90, and a serial dilution of 17-DMAG freshly prepared in FP assay buffer from stock solution in DMSO. Final concentrations are 10 nM BODIPY-AG, 40 or 60 nM Hsp90, varying concentration of 17-DMAG (0.10 nM-10 μM), and ≤0.25% DMSO in a 384-well microplate. After 3 hours incubation at 30 °C, fluorescence anisotropy (γEx = 485 nm, γEm = 535 nm) is measured on an EnVision 2100 multilabel plate reader. IC50 value of 17-DMAG is obtained from the competition curves.
Cell Research:[5]
+ Expand
  • Cell lines: Chronic lymphocytic leukemia (CLL)
  • Concentrations: Dissolved in DMSO, final concentrations ~1 μM
  • Incubation Time: 24, or 48 hours
  • Method: Cells are exposed to various concentrations of 17-DMAG for 24, or 48 hours. For the assessment of cytotoxicity, MTT reagent is then added, and plates are incubated for an additional 24 hours before spectrophotometric measurement. Apoptosis is determined by staining with annexin V-fluorescein isothiocyanate and propidium iodide (PI).
    (Only for Reference)
Animal Research:[5]
+ Expand
  • Animal Models: SCID mice engrafted with TCL1 leukemia cells
  • Formulation: Dissolved in DMSO
  • Dosages: 10 mg/kg
  • Administration: Intraperitoneal injection 5 times per week
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 131 mg/mL (200.54 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
30 mg/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

Molecular Weight 653.21
Formula

C32H48N4O8•HCl

CAS No. 467214-21-7
Storage powder
in solvent
Synonyms NSC 707545,BMS 826476 HCl,KOS 1022

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID