SNX-2112 (PF-04928473)

製品コードS2639

SNX-2112 (PF-04928473)化学構造

分子量(MW):464.48

SNX-2112 (PF-04928473) selectively binds to the ATP pocket of HSP90α and HSP90β with Ka of 30 nM and 30 nM, uniformly more potent than 17-AAG.

サイズ 価格(税別)  
JPY 83000.00
JPY 44820.00
JPY 61420.00
JPY 161020.00

カスタマーフィードバック(1)

  • Mol Cell Biol 2013 33(12), 2375-87. SNX-2112 (PF-04928473) 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 SNX-2112 (PF-04928473) selectively binds to the ATP pocket of HSP90α and HSP90β with Ka of 30 nM and 30 nM, uniformly more potent than 17-AAG.
ターゲット
HSP90α [1]
(cell-free assay)
HSP90β [1]
(cell-free assay)
30 nM(Ka) 30 nM(Ka)
体外試験

Treatment of BT-474 cells with 1 μM SNX-2112 results in down-regulation of HER2 expression within 3 to 6 hours of drug exposure with near-complete loss of HER2 expression by 10 hours. Treatment with SNX-2112 also results in a decline in total Akt expression. SNX-2112 inhibits cell proliferation with IC50 values ranging from 10 to 50 nM, in BT474, SKBR-3, SKOV-3, MDA-468, MCF-7 and H1650 cancer cells. And these antiproliferative effects are associated with hypophosphorylation of Rb, arrest of G1 and modest levels of apotosis. [1] SNX-2112 competitively binds to the N-terminal adenosine triphosphate binding site of Hsp90. SNX-2112 induces apoptosis via caspase-8, -9, -3, and poly (ADPribose) polymerase cleavage. SNX-2112 inhibits cytokine-inducedAkt and extracellular signal-related kinase (ERK) activation and also overcomes the growth advantages conferred by interleukin-6, insulin-like growth factor-1, and bone marrow stromal cells. SNX-2112 inhibits tube formation by human umbilical vein endothelial cells via abrogation of eNOS/Akt pathway and markedly inhibits osteoclast formation via down-regulation of ERK/c-fos and PU.1. [2] Cell lines (eight cell lines from osteosarcoma, neuroblastoma, hepatoblastoma, and ymphoma) studied demonstrates sensitivity to SNX-2112 with IC50 values ranging from 10-100 nM. A higher dose (70 nM) exhibits a more prolonged inhibition and larger sub-G1 accumulation. Observed levels of Akt1 and C-Raf are markedly reduced over time along with an increase in PARP cleavage. [3] A recent research indicates NX-2112 induces autophagy in a time- and dose-dependent manner via Akt/mTOR/p70S6K inhibition. SNX-2112 induces significant apoptosis and utophagy in human melanoma A-375 cells, and may be an effective targeted therapy agent. [4]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A375 cells MUjGeY5kfGmxbjDhd5NigQ>? M1XublI1KGh? M2LwU2lvcGmkaYTpc44hd2ZiSIPwPVAhcW5iaIXtZY4hSTN5NTDj[YxteyCjc4Pld5Nm\CCjczDwV|Yh\GWpcnHkZZRqd25iYX\0[ZIhOjRiaILzJIJ6KGirZ3igZ49vfGWwdDDzZ5Jm\W6rbnesJGlEPTB;MD6wNFEh|ryP MWGxPVU2OjR|Mx?=
LNCAP cells NYrze2toWHKxbHnm[ZJifGmxbjDhd5NigQ>? MkP5O|IuOTR2IHi= MmXzRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCOTlPBVEBk\WyuczDh[pRmeiB5MjD0c{AyPDRiaILzJIJ6KGO7cYXhcpQhTE6DIHT5[UBu\XSqb3SsJGlEPTB;MD6wNFMh|ryP NUnYd3dpOTl3NUK0N|M>
human SW620 cells NF3ZXFJRem:uaX\ldoF1cW:wIHHzd4F6 M1jHW|czNTF2NDDo NV7DXGt7SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDTW|YzOCClZXzsd{Bi\nSncjC3NkB1dyBzNESgbJJ{KGK7IHP5dZVidnRiRF7BJIR6\SCvZYToc4QtKEmFNUC9NE4xODNizszN M4nLcVE6PTV{NEOz
HT-29 cells NHToV4dRem:uaX\ldoF1cW:wIHHzd4F6 MYK3Nk0yPDRiaB?= NWDyXlVSSW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC3NkB1dyBzNESgbJJ{KGK7IHP5dZVidnRiRF7BJIR6\SCvZYToc4QtKEmFNUC9NE4xODNizszN M175R|E6PTV{NEOz
human SK-MEL-5 cells NGHJc49Rem:uaX\ldoF1cW:wIHHzd4F6 NILCPVU4Oi1zNESgbC=> MYjBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFONLV3FUE02KGOnbHzzJIFnfGW{IEeyJJRwKDF2NDDodpMh[nliY4nxeYFvfCCGTlGg[JlmKG2ndHjv[EwhUUN3ME2wMlAxPiEQvF2= NYqwN|Z5OTl3NUK0N|M>
sf9 cells M33OfWZ2dmO2aX;uJIF{e2G7 Mnz0N{Bp MX7CbY5lcW6pIHHm[olvcXS7IITvJIh2dWGwIF6teIVzdWmwYXygdI9tgUircz30ZYdo\WRiSGPQPVBj\XSjIDjEPUB1dyCHMkO2LUBmgHC{ZYPz[YQhcW5iaX7z[YN1KHOoOTDj[YxteyCjZoTldkA{KGi{czDifUBndHWxcnXzZ4Vv[2VicH;sZZJqgmG2aX;uJIF{e2G7LDDLbV0xNjByNjFOwG0> MXWyOFM{OjR6OB?=
K562 cells MVTQdo9tcW[ncnH0bY9vKGG|c3H5 M4G2TVczNTF2NDDo M3HZe2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iS{W2NkBk\WyuczDh[pRmeiB5MjD0c{AyPDRiaILzJIJ6KGO7cYXhcpQhTE6DIHT5[UBu\XSqb3SsJGlEPTB;MD6wNFYh|ryP NF[xd|YyQTV3MkSzNy=>
MDA-MB-231 cells MX;Qdo9tcW[ncnH0bY9vKGG|c3H5 NH[2S3k4Oi1zNESgbC=> NGnKTY5CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3ERU1OSi1{M{GgZ4VtdHNiYX\0[ZIhPzJidH:gNVQ1KGi{czDifUBkgXG3YX70JGRPSSCmeXWgcYV1cG:mLDDJR|UxRTBwMEC2JO69VQ>? NYHBRYh4OTl3NUK0N|M>
PC3 cells M{PldHBzd2yrZnXyZZRqd25iYYPzZZk> MlvGO|IuOTR2IHi= Mlm1RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCSQ{OgZ4VtdHNiYX\0[ZIhPzJidH:gNVQ1KGi{czDifUBkgXG3YX70JGRPSSCmeXWgcYV1cG:mLDDJR|UxRTBwMEG3JO69VQ>? MVuxPVU2OjR|Mx?=
NCI-H460 cells MXvQdo9tcW[ncnH0bY9vKGG|c3H5 NVLMd5lIPzJvMUS0JIg> MmjuRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCQQ1mtTFQ3OCClZXzsd{Bi\nSncjC3NkB1dyBzNESgbJJ{KGK7IHP5dZVidnRiRF7BJIR6\SCvZYToc4QtKEmFNUC9NE4xOThizszN M3f1flE6PTV{NEOz
MCF7 cells MVzGeY5kfGmxbjDhd5NigQ>? NVXXNXFuUW6qaXLpeIlwdiCxZjDIV3A6OGGucHjhJIlvKGi3bXHuJG1ETjdiY3XscJMh[XO|ZYPz[YQh[XNiZHXndoFl[XSrb36gc4YhUGW{LUKsJGVEPTB;MD6wNVkh|ryP MV6yNlk{QDB|MB?=
AU565 cells M1XtbGZ2dmO2aX;uJIF{e2G7 NYTqU2k6OjRiaB?= Mnz6TY5pcWKrdHnvckBw\iCKc4C5NEBqdiCqdX3hckBCXTV4NTDj[YxteyCjc4Pld5Nm\CCjczDwSXJMKGSnZ4Lh[IF1cW:wIHHmeIVzKDJ2IHjyd{BjgSCqaXfoJINwdnSnboSgd4Nz\WWwaX7nMEBKSzVyPUCuNFQyKM7:TR?= MVKxPVU2OjR|Mx?=
HCT15 cells MoXYVJJwdGmoZYLheIlwdiCjc4PhfS=> M3LuflczNTF2NDDo M13Vb2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVUh[2WubIOgZYZ1\XJiN{KgeI8hOTR2IHjyd{BjgSCleYH1ZY51KESQQTDkfYUhdWW2aH;kMEBKSzVyPUCuNFUzKM7:TR?= MXKxPVU2OjR|Mx?=
MRC5 cells NID3e4VEgXSxdH;4bYNqfHliYYPzZZk> NWrkVFVqPDhiaB?= M3fCOWN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG1TSzViY3XscJMh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfUwhS0N3ME2yNU4{PCEQvF2= Mn7jNlI4ODR6OUC=

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 SNX-2112, delivered by its prodrug SNX-5422, inhibits MM cell growth and prolongs survival in a xenograft murine model and blockade of Hsp90 by SNX-2112 not only inhibits MM cell growth but also acts in the bone marrow microenvironment to block angiogenesis and osteoclastogenesis. [2]

お薦めの試験操作(参考用のみ)

キナーゼ試験:[1]
+ 展開

ATP Displacement Assay:

For the protein affinity-displacement assay, a purine-based affinity resin is generated by incubating ATP-linked Sepharose with Jurkat cell lysate (flash frozen and homogenized in saline) at 4 °C. This is then incubated with SNX-2112 for 90 minutes. Proteins eluted by drug are then resolved by SDS-PAGE, visualized with silver staining, and excised from the gel for MS-based identification. Briefly, after destaining and trypsin digestion, peptides are extracted with μC18 ZipTips and then eluted and spotted directly to a conventional stainless steel matrix-assisted laser desorption/ionization target with a saturated solution of α-cyano-4- hydroxycinnamic acid in 50% acetonitrile, 0.15% formic acid. Mass spectra are then acquired using a MALDI-TOF/TOF 4700 Proteomics Analyzer. MS spectra are acquired (1,000 shots per spectrum), and the three peaks from each with the greatest signal-to-noise ratio are automatically submitted for tandem MS analysis (3000 shots per spectrum). The collision energy is 1keV. Air is used as the collision gas. Protein identification is done from the MS and tandem MS data using GPS Explorer software with the integrated Mascot database search engine.
細胞試験: [1]
+ 展開
  • 細胞株: BT474, SKBR-3, SKOV-3, MDA-468, MCF-7 and H1650 cancer cells
  • 濃度: 0-500 nM
  • 反応時間: 24 hours
  • 実験の流れ: Cell viability is determined by seeding 2-5 × 103 cells per well in 96- well plates and treating with SNX-2112 24 hours after plating in complete medium (200 μL). Each drug concentration is tested in eight wells. Cells are assayed using the Alamar blue viability test after a 96-h incubation. Flow cytometry is done using nuclei stained with ethidium bromide and isolated via the Nusse protocol
    (参考用のみ)
動物試験:[2]
+ 展開
  • 動物モデル: 5 × 106 MM.1S cells are inoculated subcutaneously in the Fox Chase SCID mice (6-7 weeks old).
  • 製剤: SNX-5422 is dissolved in 1% carboxy methylcellulose/0.5% Tween 80 at 10 mg/mL and stored at 4 °C for in vivo stud
  • 投薬量: 20 or 40 mg/kg
  • 投与方法: SNX-5422 is administered orally 3 times per week, total 3 weeks.
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 93 mg/mL (200.22 mM)
Ethanol 1 mg/mL (2.15 mM)
Water 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):
0.5% CMC+0.25% 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 464.48
化学式

C23H27F3N4O3

CAS No. 908112-43-6
保管
in solvent
別名 N/A

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

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