Alvespimycin (17-DMAG) HCl

For research use only. Not for use in humans.

製品コードS1142 別名:NSC 707545,BMS 826476 HCl,KOS 1022

Alvespimycin (17-DMAG) HCl化学構造

分子量(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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バルク問合せ

文献中Selleckの製品使用例(36)

製品安全説明書

HSP (HSP90)阻害剤の選択性比較

生物活性

製品説明 Alvespimycin (17-DMAG) HCl is a potent HSP90 inhibitor with IC50 of 62 nM in a cell-free assay. Phase 2.
特性 A synthetic derivative Geldanamycin, with lower hepatotoxicity than parent antibiotic & higher potency and bioavailability than the similar derivative 17-AAG.
ターゲット
HSP90 [1]
(Cell-free assay)
62 nM
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human A2058 cells MXLDfZRwfG:6aXRCpIF{e2G7 M2r0[mN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGEzODV6IHPlcIx{KGK7IF3UWEBie3OjeTygTWM2OD1{LkGgcm0> NUjIPGEzOTh7Mkm0PFY>
human AGS cells MXrGeY5kfGmxbjDhd5NigQ>? NIfiSXFKdmirYnn0bY9vKG:oIHj5dI95cWFvaX7keYNm\CCKSV[xJIFkfGm4YYTpc44hcW5iaIXtZY4hSUeVIHPlcIx{KGK7IILldI9zfGW{IHflcoUh[XO|YYmsJGlEPTB;Mz62JI5O M3fUU|E5OzV7NkOx
SKBR3 cells NEjKPIdHfW6ldHnvckBie3OjeR?= M2j6d3VxemWpdXzheIlwdiCxZjDId5A4OCCrbjDTT2JTOyClZXzsd{whTUN3ME20JI5O M1jmbFE3QDV2ME[2
human MDA-MB-231 cells M1TTV2Z2dmO2aX;uJIF{e2G7 MYnJcohq[mm2aX;uJI9nKEi|cEmwJIlvKGi3bXHuJG1FSS2PQj2yN|Eh[2WubIOgZZN{\XO|ZXSgZZMhcGW{MjDk[Ydz[WSjdHnvckwhUUN3ME20MlUhdk1? MmLzNVg6Ojl2OE[=
human MDA-MB-231 cells NETjUopEgXSxdH;4bYPDqGG|c3H5 NVXZV2tWS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUSDLV3CMVI{OSClZXzsd{BjgSCPVGSgZZN{[XluIFnDOVA:PS56IH7N NUDk[IpxOTh7Mkm0PFY>
human A2058 cells MkjkSpVv[3Srb36gZZN{[Xl? M4\UdWlvcGmkaYTpc44hd2ZiSIPwPVAhcW5iaIXtZY4hSTJyNUigZ4VtdHNuIFXDOVA:Py57IH7N NUToWZZtOTh7Mkm0PFY>
SKOV3 cells MUTGeY5kfGmxbjDhd5NigQ>? MmWxWZBz\We3bHH0bY9vKG:oIFjzdFcxKGmwIGPLU3Y{KGOnbHzzMEBGSzVyPUG0JI5O MlPzNVY5PTRyNk[=
SKBr3 cells NGjIZVZEgXSxdH;4bYPDqGG|c3H5 NVq2VnhnS3m2b4TvfIlkcXS7IHHnZYlve3RiU1vCdlMh[2WubIOsJGlEPTB;MkSgcm0> MknSNVYyPjV|NUS=
human AGS cells NXfnRpNVTnWwY4Tpc44h[XO|YYm= M3XkNFE3KGh? NEfZVFVKdmirYnn0bY9vKG:oIFjJSlEh[WO2aY\heIlwdiCrbjDoeY1idiCDR2OgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCqeYDvfIliNWmwZIXj[YQhdHWlaX\ldoF{\SCneIDy[ZN{cW:wIHHmeIVzKDF4IHjyd{BjgSC{ZYDvdpRmeiCjc4PhfUwhUUN3ME2zOkBvVQ>? M{\MO|E4PTh|OUWw
human HCT116 cells NWLLUY8zS3m2b4TvfIlkyqCjc4PhfS=> MoTpR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGK7IFHsZY1ieiCkbIXlJIF{e2G7LDDJR|UxRTVyIH7N M1TacVIxPjZ{NUO0
human Hep3B cells MWnGeY5kfGmxbjDhd5NigQ>? NVjIOndXOTJiaB?= MUnJcohq[mm2aX;uJI9nKGi7cH;4bYEucW6mdXPl[EBJUUZzYXzwbIEheHKxdHXpckBi[2O3bYXsZZRqd25iaX6gbJVu[W5iSHXwN2Ih[2WubIOgeJJm[XSnZDDmc5IhOzBibXnud{Bu\WG|dYLl[EBi\nSncjCxNkBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{NCCLQ{WwQVU4KG6P MWSyNFQ3QTh6Nx?=
human A549 cells NVL5ZZhlS3m2b4TvfIlkyqCjc4PhfS=> MXe3NkBp NFWx[GdEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCPTR7IHPlcIx{KGGodHXyJFczKGi{czDifUBk\WyudHn0[ZIu\2yxIHHzd4F6NCCLQ{WwQVY5KG6P NFm4epAyQTRyNUWyPC=>
human MCF7 cells MXXDfZRwfG:6aXRCpIF{e2G7 MV63NkBp M4jhVmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgO|IhcHK|LDDJR|UxRTdzIH7N NH73NYUyQTJ|MUi2OC=>
human NCI-H1299 cells MYjGeY5kfGmxbjDhd5NigQ>? NIHNN3JKdmirYnn0bY9vKG:oIHj1cYFvKEiVUEmwJIlvKGi3bXHuJG5EUS2KMUK5PUBk\WyuczDhd5Nme3OnZDDhd{BCc3RiZHXndoFl[XSrb36gZYZ1\XJiMkSgbJJ{KGK7IHz1cYlv\XhiYYPzZZktKEmFNUC9NE4yKM7:TR?= NFnnV4kzOTR|OEW0NS=>
human HeLa cells M1XLfGZ2dmO2aX;uJIF{e2G7 MW\Jcohq[mm2aX;uJI9nKFSQRj3hcJBp[S2rbnT1Z4VlKE6ILXvhdJBiSiCjY4TpeoF1cW:wIHnuJIh2dWGwIFjlUIEh[2WubIOsJGlEPTB;MD6xOUDPxE1? Mm[1NVg{PTl4M{G=
human A231 cells NIrvdWhRem:uaX\ldoF1cW:wIHHzd4F6 NEThdms1QCCq NYrMOFVrSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlMyKGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6xO{DPxE1? MWCyOFc3OzJ4MR?=
human CCRF-CEM cells NIe5VJJEgXSxdH;4bYPDqGG|c3H5 NULmNJlTPzJiaB?= M3X1OWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGNEWkZvQ1XNJINmdGy|IHHmeIVzKDd{IHjyd{BjgSClZXzseIl1\XJvOU[gZZF2\W:3czDvcoUhe2:udYTpc44h[XO|YYmsJGlEPTB;MD61OEDPxE1? NGS3[3UyQTRyNUWyPC=>
human NCI-H596 cells Mn\OR5l1d3SxeHnjxsBie3OjeR?= NXTYbXdVPzJiaB?= M2nKZmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KE6TMEGt[IVncWOrZX70JIh2dWGwIF7DTU1JPTl4IHPlcIx{KGGodHXyJFczKGi{czygTWM2OD1zLkGg{txO NIe3e2QyQTJ|MUi2OC=>
human HCT116 cells M1Hvc3Bzd2yrZnXyZZRqd25iYYPzZZk> NEDuNXk1QCCq MUnBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTFwMkGg{txO MlfPNlQ4PjN{NkG=
human MDA468 cells NVTjTJdGS3m2b4TvfIlkyqCjc4PhfS=> M3HjelczKGh? MoDPR5l1d3SxeHnjbZR6KGGpYXnud5QhVlFyMT3k[YZq[2mnboSgbJVu[W5iTVTBOFY5KGOnbHzzJIFnfGW{IEeyJIhzeyxiSVO1NF0yNjZizszN NETne2QyQTJ|MUi2OC=>
human AGS cells NETWSpVEgXSxdH;4bYPDqGG|c3H5 NYXEbW1TS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSUeVIHPlcIx{KGK7IF3UWEBie3OjeTygTWM2OD1zNjFOwG0> NHnFd4EyQDN3OU[zNS=>
human LN229-Lux cells NXLBSIZqTnWwY4Tpc44h[XO|YYm= MoX4Nk42NTFyIN88US=> MlS0NUBp M37PZ2lvcGmkaYTpc44hd2ZibIXjbYZmemG|ZTDhZ5Rqfmm2eTDpckBpfW2jbjDMUlIzQS2OdYigZ4VtdHNiYYSgNk42KHSxIEGwJJVOKGmwY4XiZZRm\CCob4KgNUBpeiC3bnTldkBvd3Kvb4jpZUBnd2yub4fl[EBjgSB{NDDodpMhfW6mZYKgbJlxd3irYTDifUBz\XCxcoTldkBo\W6nIHHzd4F6 NF3X[5IzOjd2NkK3OC=>
human NCI-H1299 cells NIOycWNHfW6ldHnvckBie3OjeR?= MXqxNkBp NYLocmhoWmWmdXP0bY9vKGmwIH;4fYdmdiClb37zeY1xfGmxbjDyZZRmKGmwIHj1cYFvKE6FST3INVI6QSClZXzsd{BqdmO3YnH0[YQh\m:{IEGyJIhzew>? Mn3oNlU{QDN7MUW=
human NCI-H526 cells MVLGeY5kfGmxbjDhd5NigQ>? MnrXNUDPxE1? MUmyOEBp NH74fWVDcW6maX7nJIFn\mmwaYT5JJRwKEiVUEmwJIlvKGi3bXHuJG5EUS2KNUK2JINmdGy|IHH0JFEhfU1iYX\0[ZIhOjRiaILzJIJ6KG[udX;y[ZNk\W6lZTDwc4xiemm8YYTpc44h[XO|YYm= MmPINVc3ODN3NEC=

他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

アッセイ
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
体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
- 合併

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.
細胞試験: [5]
- 合併
  • 細胞株: Chronic lymphocytic leukemia (CLL)
  • 濃度: Dissolved in DMSO, final concentrations ~1 μM
  • 反応時間: 24, or 48 hours
  • 実験の流れ: 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).
    (参考用のみ)
動物試験:[5]
- 合併
  • 動物モデル: SCID mice engrafted with TCL1 leukemia cells
  • 投薬量: 10 mg/kg
  • 投与方法: Intraperitoneal injection 5 times per week
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 131 mg/mL (200.54 mM)
Water Insoluble
Ethanol Insoluble
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):
1% DMSO+30% polyethylene glycol+1% Tween 80
混合させたのち直ちに使用することを推奨します。
30 mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 653.21
化学式

C32H48N4O8•HCl

CAS No. 467214-21-7
Storage powder
in solvent
別名 NSC 707545,BMS 826476 HCl,KOS 1022
Smiles Cl.COC1CC(C)CC2=C(NCCN(C)C)C(=O)C=C(NC(=O)C(=C\C=C/C(OC)C(OC(N)=O)/C(=C/C(C)C1O)C)\C)C2=O

投与溶媒組成計算器(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)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
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
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

HSP (HSP90)シグナル伝達経路

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID