Alvespimycin (17-DMAG) HCl

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.

サイズ 価格(税別)  
JPY 22742.00
JPY 24900.00
JPY 61420.00
JPY 94620.00

カスタマーフィードバック(6)

  • H2228/Vec or H2228/HGF cells were treated with or without alectinib (0.3 μmol/L) for 2 h or 17-DMAG (0.3 μmol/L) for 24 h and then stimulated with or without HGF (50 ng/mL) for 10 minutes. The resultant cells were lysed, and the indicated proteins were detected by immunoblotting.

    Oncotarget, 2014, 5(13): 4920-28 . Alvespimycin (17-DMAG) HCl purchased from Selleck.

    H2228 cells were treated with or without alectinib (0.3 μmol/L) for 2 h or 17-DMAG (0.3 μmol/L) for 24 h, and then stimulated with or without EGF (100 ng/mL), HB-EGF (10 ng/mL), and TGF-α (100 ng/mL) for 10 min. The resultant cells were lysed, and the indicated proteins were detected by immunoblotting.

    Oncotarget, 2014, 5(13): 4920-28 . Alvespimycin (17-DMAG) HCl purchased from Selleck.

  • 17-DMAG suppresses EGF and Met protein expression and phosphorylation even in the presence of HGF. PC-9, Ma-1, Ma-1/Vec, and Ma-1/HGF tumor cells were treated with or without erlotinib (0.3 umol/l) or 17-DMAG (0.3 umol/l) for 24 hours, and then stimulated with or without HGF (20 ng/ml) for 10 minutes. The resultant cells were lysed, and the indicated proteins were detected by immunoblotting. EGF, epidermal growth factor; HGF, hepatocyte growth factor.

    J Thorac Oncol 2012 7(7), 1078-85. Alvespimycin (17-DMAG) HCl purchased from Selleck.

    17-DMAG overcomes HGF-induced erlotinib resistance in vivo. Ma-1/Vec or Ma-1/HGF cells (5 x 106 each) were inoculated subcutaneously into SCID mice on day 0. Mice received oral erlotinib (20 mg/kg/day) or intraperitoneal 17-DMAG (10 mg/kg/day), starting on day 7. Tumor size was measured twice a week and tumor volumes were calculated as described in Materials and Methods. Macroscopic appearances of representative tumors harvested on day 21. *p < 0.01 compared with the control group (Student’s t test). 17-DMAG, 17-Dimethylaminoethylamino-17-demethoxygeldanamycin; HGF, hepatocyte growth factor; SCID, severe combined immunodeficiency.

    J Thorac Oncol 2012 7(7), 1078-85. Alvespimycin (17-DMAG) HCl purchased from Selleck.

  • Mol Oncol 2013 7(6), 1093-102. Alvespimycin (17-DMAG) HCl purchased from Selleck.

    (D) H&E staining and immunohistochemistry staining of CHIP and CD166 in consecutive sections of Cal27 xenografts in DMSO and 17-DMAG treated mice; bar=100 µm.

    Experimental Cell Research, 2017, 353(1):46-53. Alvespimycin (17-DMAG) HCl purchased from Selleck.

製品安全説明書

HSP (e.g. 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 M1vKeWN6fG:2b4jpZ:Kh[XO|YYm= NH;zfplEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBCOjB3ODDj[YxteyCkeTDNWHQh[XO|YYmsJGlEPTB;Mj6xJI5O NYfWcGRsOTh7Mkm0PFY>
human AGS cells Mny2SpVv[3Srb36gZZN{[Xl? NXjKXJZXUW6qaXLpeIlwdiCxZjDofZBwgGmjLXnu[JVk\WRiSFnGNUBi[3SrdnH0bY9vKGmwIHj1cYFvKEGJUzDj[YxteyCkeTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBKSzVyPUOuOkBvVQ>? NW\ZUm5WOTh|NUm2N|E>
SKBR3 cells MWnGeY5kfGmxbjDhd5NigQ>? NGHBOFVWeHKnZ4XsZZRqd25ib3[gTJNxPzBiaX6gV2tDWjNiY3XscJMtKEWFNUC9OEBvVQ>? M{PXclE3QDV2ME[2
human MDA-MB-231 cells MkPiSpVv[3Srb36gZZN{[Xl? M1fYVWlvcGmkaYTpc44hd2ZiSIPwPVAhcW5iaIXtZY4hVUSDLV3CMVI{OSClZXzsd{Bie3Onc4Pl[EBieyCqZYKyJIRm\3KjZHH0bY9vNCCLQ{WwQVQvPSCwTR?= NInTdWkyQDl{OUS4Oi=>
human MDA-MB-231 cells M4C4RWN6fG:2b4jpZ:Kh[XO|YYm= NGDtc4FEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBOTEFvTVKtNlMyKGOnbHzzJIJ6KE2WVDDhd5NigSxiSVO1NF02Njhibl2= MW[xPFkzQTR6Nh?=
human A2058 cells Mn6ySpVv[3Srb36gZZN{[Xl? MYTJcohq[mm2aX;uJI9nKEi|cEmwJIlvKGi3bXHuJGEzODV6IHPlcIx{NCCHQ{WwQVcvQSCwTR?= NVv3XI1VOTh7Mkm0PFY>
SKOV3 cells MXfGeY5kfGmxbjDhd5NigQ>? NWDHTWt3XXC{ZXf1cIF1cW:wIH;mJGh{eDdyIHnuJHNMV1Z|IHPlcIx{NCCHQ{WwQVE1KG6P NVr2c5pEOTZ6NUSwOlY>
SKBr3 cells MofPR5l1d3SxeHnjxsBie3OjeR?= MlrQR5l1d3SxeHnjbZR6KGGpYXnud5QhW0uEckOgZ4VtdHNuIFnDOVA:OjRibl2= NUC4SHB1OTZzNkWzOVQ>
human AGS cells MXzGeY5kfGmxbjDhd5NigQ>? NU\WUXM2OTZiaB?= M2joZ2lvcGmkaYTpc44hd2ZiSFnGNUBi[3SrdnH0bY9vKGmwIHj1cYFvKEGJUzDj[YxteyCjc4Pld5Nm\CCjczDpcohq[mm2aX;uJI9nKGi7cH;4bYEucW6mdXPl[EBtfWOrZnXyZZNmKGW6cILld5Nqd25iYX\0[ZIhOTZiaILzJIJ6KHKncH;yeIVzKGG|c3H5MEBKSzVyPUO2JI5O NILiRZEyPzV6M{m1NC=>
human HCT116 cells NFnnTZJEgXSxdH;4bYPDqGG|c3H5 M4PhNGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCkeTDBcIFu[XJiYnz1[UBie3OjeTygTWM2OD13MDDuUS=> MWWyNFY3OjV|NB?=
human Hep3B cells NUPKeVJbTnWwY4Tpc44h[XO|YYm= M332NlEzKGh? Mn\XTY5pcWKrdHnvckBw\iCqeYDvfIliNWmwZIXj[YQhUEmIMXHsdIhiKHC{b4TlbY4h[WOldX31cIF1cW:wIHnuJIh2dWGwIFjldFNDKGOnbHzzJJRz\WG2ZXSg[o9zKDNyIH3pcpMhdWWjc4Xy[YQh[W[2ZYKgNVIhcHK|IHL5JHdme3Sncn6gZoxwfCCjbnHsfZNqeyxiSVO1NF02PyCwTR?= M33Dd|IxPDZ7OEi3
human A549 cells NGHUOpJEgXSxdH;4bYPDqGG|c3H5 NFjTcJo4OiCq M1nlSWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGE2PDliY3XscJMh[W[2ZYKgO|IhcHK|IHL5JINmdGy2aYTldk1odG9iYYPzZZktKEmFNUC9Olghdk1? MUGxPVQxPTV{OB?=
human MCF7 cells M{G1UWN6fG:2b4jpZ:Kh[XO|YYm= NWXvNY42PzJiaB?= M3vlWmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1ETjdiY3XscJMh[W[2ZYKgO|IhcHK|LDDJR|UxRTdzIH7N M2rU[FE6OjNzOE[0
human NCI-H1299 cells NWHNWWlFTnWwY4Tpc44h[XO|YYm= MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGhUWDlyIHnuJIh2dWGwIF7DTU1JOTJ7OTDj[YxteyCjc4Pld5Nm\CCjczDBb5Qh\GWpcnHkZZRqd25iYX\0[ZIhOjRiaILzJIJ6KGy3bXnu[Zgh[XO|YYmsJGlEPTB;MD6xJO69VQ>? MmrFNlE1Ozh3NEG=
human HeLa cells M1mxZWZ2dmO2aX;uJIF{e2G7 NGO1UoFKdmirYnn0bY9vKG:oIGTOSk1idHCqYT3pcoR2[2WmIF7GMYtieHCjQjDhZ5RqfmG2aX;uJIlvKGi3bXHuJGhmVGFiY3XscJMtKEmFNUC9NE4yPSEQvF2= Mm[2NVg{PTl4M{G=
human A231 cells MlzhVJJwdGmoZYLheIlwdiCjc4PhfS=> NHHQPZU1QCCq NEHv[FZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFGyN|Eh[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkG3JO69VQ>? NY[5OJJxOjR5NkOyOlE>
human CCRF-CEM cells NWrvOZI4S3m2b4TvfIlkyqCjc4PhfS=> M4\QNlczKGh? NF;zcVNEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBES1KILVPFUUBk\WyuczDh[pRmeiB5MjDodpMh[nliY3XscJRqfGW{LUm2JIFyfWWxdYOgc45mKHOxbIX0bY9vKGG|c3H5MEBKSzVyPUCuOVQh|ryP M4rnT|E6PDB3NUK4
human NCI-H596 cells NHS3bXlEgXSxdH;4bYPDqGG|c3H5 M1\wblczKGh? MWrDfZRwfG:6aXPpeJkh[WejaX7zeEBPWTBzLXTl[olkcWWwdDDoeY1idiCQQ1mtTFU6PiClZXzsd{Bi\nSncjC3NkBpenNuIFnDOVA:OS5zIN88US=> MUWxPVI{OTh4NB?=
human HCT116 cells M2jiN3Bzd2yrZnXyZZRqd25iYYPzZZk> MXW0PEBp M4TnNGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MT6yNUDPxE1? M3:3O|I1PzZ|Mk[x
human MDA468 cells NHWwfoZEgXSxdH;4bYPDqGG|c3H5 Mn21O|IhcA>? MVTDfZRwfG:6aXPpeJkh[WejaX7zeEBPWTBzLXTl[olkcWWwdDDoeY1idiCPRFG0Olgh[2WubIOgZYZ1\XJiN{KgbJJ{NCCLQ{WwQVEvPiEQvF2= MUCxPVI{OTh4NB?=
human AGS cells NYLt[ZQzS3m2b4TvfIlkyqCjc4PhfS=> MVLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDBS3Mh[2WubIOgZpkhVVSWIHHzd4F6NCCLQ{WwQVE3KM7:TR?= NIC4bmIyQDN3OU[zNS=>
human LN229-Lux cells NX\D[VFQTnWwY4Tpc44h[XO|YYm= NH\BbGwzNjVvMUCg{txO MkfwNUBp NITiXIFKdmirYnn0bY9vKG:oIHz1Z4ln\XKjc3WgZYN1cX[rdImgbY4hcHWvYX6gUG4zOjlvTIX4JINmdGy|IHH0JFIvPSC2bzCxNEB2VSCrbnP1ZoF1\WRiZn;yJFEhcHJidX7k[ZIhdm:{bX;4bYEh\m:ubH;3[YQh[nliMkSgbJJ{KHWwZHXyJIh6eG:6aXGgZpkhemWyb4L0[ZIh\2WwZTDhd5NigQ>? Mnv2NlI4PDZ{N{S=
human NCI-H1299 cells M{CwWmZ2dmO2aX;uJIF{e2G7 Mke1NVIhcA>? MY\S[YR2[3Srb36gbY4hd3i7Z3XuJINwdnO3bYD0bY9vKHKjdHWgbY4hcHWvYX6gUmNKNUhzMkm5JINmdGy|IHnuZ5Vj[XSnZDDmc5IhOTJiaILz MWGyOVM5OzlzNR?=
human NCI-H526 cells NWLEVpg1TnWwY4Tpc44h[XO|YYm= MnOzNUDPxE1? MnGwNlQhcA>? MoXLRolv\GmwZzDh[oZqdmm2eTD0c{BJW1B7MDDpckBpfW2jbjDOR2kuUDV{NjDj[YxteyCjdDCxJJVOKGGodHXyJFI1KGi{czDifUBndHWxcnXzZ4Vv[2VicH;sZZJqgmG2aX;uJIF{e2G7 M1LrelE4PjB|NUSw

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

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]
+ 展開

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]
+ 展開
  • 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]
+ 展開
  • 動物モデル: SCID mice engrafted with TCL1 leukemia cells
  • 製剤: Dissolved in DMSO
  • 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
保管
in solvent
別名 NSC 707545,BMS 826476 HCl,KOS 1022

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 (g) = 濃度 (mol/L) x 体積 (L) 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

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01126502 Terminated B-cell Chronic Lymphocytic Leukemia|Prolymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia National Cancer Institute (NCI) May 2010 Phase 1
NCT01126502 Terminated B-cell Chronic Lymphocytic Leukemia|Prolymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia National Cancer Institute (NCI) May 2010 Phase 1
NCT00780000 Terminated Breast Cancer Bristol-Myers Squibb April 2008 Phase 2
NCT00780000 Terminated Breast Cancer Bristol-Myers Squibb April 2008 Phase 2
NCT00803556 Completed Solid Tumor|Breast Cancer Bristol-Myers Squibb January 2006 Phase 1
NCT00803556 Completed Solid Tumor|Breast Cancer Bristol-Myers Squibb January 2006 Phase 1

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

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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